World Academy of Science, Engineering and Technology
[Pharmacological and Pharmaceutical Sciences]
Online ISSN : 1307-6892
1271 Mechanistic Insight and In-Vitro Validation of Scoparone-Functionalized Zno Nanoparticles as Antioxidant and Antimicrobial Therapeutics Against Antimicrobial-Resistant E. Coli
Authors: Callistus I. Iheme, Chinwe S. Alisi, Obinna S. Nwabueze
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Antimicrobial resistance (AMR) poses a significant threat to the global health sector. Zinc oxide nanoparticles (ZnO NPs) were synthesized with aqueous crude extract of Azadirachta indica, and the phytochemical compositions were determined using Gas chromatography coupled to mass spectroscopy (GC-MS). They were further characterized using advanced spectroscopes and microscopes. The results showed arrays of ZnO NPs nanorods with maximal absorption wavelengths of 320 nm. The GC-MS revealed the presence of twenty volatile phytochemicals associated with the synthesized ZnO NPs. Among the volatile compounds, an in silico study revealed Scoparone as the most bioactive compound. The ZnO NPs were separately functionalized with Scoparone-rich portion of the extract (ZnO NPs-S), and Ampicillin (ZnO NPs-amp). Subsequently, the nanoparticles were assessed for their antioxidant and in vitro antimicrobial properties against antimicrobial-resistant Escherichia coli. An in vitro study assessed the colony counts (cfu) of the E. coli in the presence of the antimicrobials; dehydrogenase inhibitory properties of ZnO NPs-S, ZnONPs-amp, extract of A. indica, and Ampicillin (standard drug). At the concentration of 500 μm/mL, 57.89% and 89.74% of the enzyme activities were inhibited by ZnO NPs-S and ZnO NPs-amp, respectively. An in silico study revealed Scoparone component of ZnO NPs-S as the most viable competitor of nicotinamide adenine dinucleotide (NAD+) for E. coli malate and histidinol dehydrogenases binding pockets. Antioxidant analysis revealed that ZnO NPs exhibited poor antioxidant potential. Conclusively, ZnO NPs-S exhibited good antimicrobial properties against antimicrobial-resistant E. coli, and were enhanced through conjugation with Ampicillin. The application of the nanoparticles could ameliorate the increasing threat posed by AMR to the global health sector. Further toxicological, pharmacokinetic, and pharmacodynamic studies are encouraged on the nanoparticles.Keywords: antimicrobial resistance, antioxidant, enzyme activity, E. coli, zinc oxide nanoparticles
Procedia PDF Downloads 61270 Targeting Inflammation: Molecular Dynamic Simulation of Bioactive Polyphenols from Peanut (Arachis hypogaea) Leaves
Authors: Chinwe Sylvanus Alisi, Raymond Chigozie Ibeh, Godwin Sunday Aloh, Chinedu Paul Nwuke, Precious Ngozichinwe Alisi, Chinonyerem Jedidiah Ukweni, Gavin Chibundu Ikechukwu, Blessed Chigozirim Aniche, Israel Omekara
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The leaves of Arachis hypogea are being used to treat and/or manage many ailments, including inflammation. This study evaluated the relationship between the structure of the phenol-rich fraction of methanol leaf extract of Arachis the hypogea (MLEAH) in albino rats. Phytochemical profiling of the MLEAH revealed alkaloids, glycosides, tannins, flavonoids, saponins and phenols, which were most abundant. Column chromatographic fractionation and subsequent TLC of the fractions enabled the pooling together of five (5) fractions on the basis of similar RF values and termed for phenol-rich fraction of Arachis hypogea (PRFAH) leaves and used for the studies. A two-phase sub-acute toxicity evaluation revealed its LD50 to be above 1000mg/kg body weight (kg.bw). PRFAH was compared with 10mg/kgbw diclofenac-an NSAID- for ability to reverse egg-white-induced hind paw edema (HPO) in the rats. Overall, the PRFAH at 500 and at 1000mg/kg b.w respectively significantly (p < 0.05) reduced HPO by 77.9% and 83.30% when compared with the NSAID’s 90.84%. Anti-inflammatory effect of PRFAH at 500 and 1000mg/kg b.w. was pronounced as the fraction significantly (p<0.05) reduced the levels of tumor necrosis factor–α (TNF-α), nitric oxide (NO), interleukin -1β(IL-1β) and cyclo-oxygenase-2 (COX-2), more than the diclofenac for all parameters. PRFAH also restored the activities of antioxidant enzymes (superoxide dismutase (SOD) and catalase (CAT). Glutathione-reduced (GSH) concentration was restored while peroxidation (TBARS) was inhibited in the paw tissue. PRFAH at tested doses maintained the kidney and liver function markers in sub-acute toxicity studies, suggesting antioxidation as its mechanism of action. In silico studies strongly indicated that PRFAH exerted its action by binding favorably to the target enzymes, involved in inflammation, especially COX-2, as inferred from their binding scores of all the docking-identified phytochemicals, protocatechuic acid with a better binding efficiency of -94Kcal/mol than aspirin (-93kcal/mol), appeared to be the key anti-inflammatory component of PRFAH. The findings in this study strongly suggest that PRFAH exerts its anti-inflammatory action by down regulating cytokine signaling pathways.Keywords: arachis hypogea, phenol-rich fraction, anti-inflammatory, cyclo-oxygenase-2 (COX-2), phytochemical profiling
Procedia PDF Downloads 51269 Development and Characterization of a Konjac-Based Biodegradable Food-Packaging Film
Authors: Shaik Asha Begum, Sodagiri Revanth Sai
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The escalating ecological impact of single-use plastics has accelerated research into bio-based packaging materials. This study reports the formulation of an eco-friendly, edible, and compostable food-packaging film using konjac-derived glucomannan as the principal polymer, plasticised with glycerol and reinforced with gelatin, cellulose, and gum tragacanth. A water-based casting process produced transparent films in 8–10 h (45-55 °C) or 24–36 h (25 °C, 50 % RH). Qualitative assessments showed improved flexibility, tensile integrity, and moisture resistance compared with neat konjac films. The work demonstrates the technical feasibility of scaling konjac films as a circular-economy alternative to petro-chemical plastics.Keywords: konjac glucomannan, biodegradable film, bio-packaging, edible film, sustainable materials
Procedia PDF Downloads 81268 Medicinal Plants Used For Malaria Treatment In Ekiti State, South-western Nigeria: A Systematic Ethnobotanical Review
Authors: Afuwape Omotola Mary, Ajayi Bosede Helen, Abetuyi Olufunke, Agbalu Omowumi
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Malaria remains one of the most persistent public health concerns in Nigeria, particularly in rural and peri-urban communities where access to conventional healthcare is limited. In Ekiti State, South-Western Nigeria, traditional medicine continues to play a vital role in malaria management through the use of indigenous medicinal plants. This study presents a comprehensive ethnobotanical review of antimalarial plants commonly used in Ekiti State based on data collected via structured questionnaires administered to traditional healers, herbal vendors, students, and knowledgeable elders across selected local government areas. Information was collected by interviewing indigenous people using a semi-structured questionnaire.Respondents identified various plant species believed to possess antimalarial properties. A total of 100 respondents were interviewed, of whom 54% were females and 46% were males. This population comprisedherbal medicine sellers (9%), traditional doctors (6%), mothers (55%), and farmers (32%). Thirtyplant species used in the treatment of malaria, belonging to 9 families, were identified and compiled, detailing information such as common and local names, parts used, methods of preparation, and previous scientific reports. Among the plants identified during the survey, Entandrophragmacylindricum,Moringaoleifera, and Azadirachtaindicahave the highest reports of being used to treat malaria. Some of the reports show that some herbs were used together as a concoction. Despite the identification of numerous traditionally used plants for the treatment of malaria, scientific confirmation of the traditional claims of anti-malarial properties is crucial. In addition to helping to preserve this rich range of anti-malarial plants, this would position them for any potential future study into active principles and the potential creation of new, more affordable, and more potent anti-malarial medications.Keywords: malaria, concortion, ethnobotanical, herbal medicine
Procedia PDF Downloads 111267 Toxicity Assessment of Senna Occidentalis Seed Extract Using Drosophila Melanogaster Model
Authors: Joy J. Adeyemi, John O. Ayorinde, Amos O. Abolaji
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Research has shown that the seeds ofSenna occidentalis(S. occidentalis) (L.) Link have been found to result in various forms of intoxication. The toxicity of Senna seeds have been tested in animal models which includes rabbits, rats and cattle but have not been evaluated using Drosophila melanogaster models. Senna seeds were extracted using water and ethanol. The ethanol extract was fractionated using hexane, ethanol and ethylacetate into pure fractions. The quantitative and qualitative analysis of the seed extracts and fractions were carried out revealing the presence of bioactive compounds.For the survival study, 1-3 day old flies were exposed to different concentrations of the seed extract and fractions for 14 days. For the biochemical analysis, the flies were grouped into 5 with 50 flies per vial and were treated for 5 days. The flies were anaesthesized thereafter and processed to obtain supernatant solutions used to determine oxidative stress, neurological and inflammatory biomarkers.This study shows that Senna occidentalis seed extracts are toxic in Drosophila melanogaster models further affirming its toxicity as reported by previous literature. Both seed extracts and were proven to be toxic at the doses administered. They generated excess free radicals inducing oxidative stress owing to the reduction shown in most oxidative biomarkers except monoamine oxidase in the aqueous extract which shows its propensity for treating neurological disorders.Keywords: senna occidentalis, drosophila melanogaster, inflammatory biomarkers, oxidative stress, monoamine oxidase, neurological disorders
Procedia PDF Downloads 91266 Assessment of Pharmacists’ Adherence to Antibiotic Dispensing Guidelines in Benghazi, Libya
Authors: Mohammed Almukhtar Akhrees, Faris Mohammed Ali Abu Ihlayqah, Omar Saed Aboubakr, Mohamed Tarek jaouda, Ali Ateia Elmabsout, Salma Abdelkerim Bukhatwa
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The unsanctioned dispensing of antibiotics continues to pose a major global health challenge by accelerating the development of antimicrobial resistance (AMR). This study investigates the extent to which pharmacists in Benghazi, Libya, comply with established antibiotic dispensing protocols and examines their knowledge, attitudes, and routine practices. A cross-sectional survey was administered to 100 pharmacists working in various pharmaceutical settings—community, clinical, and hospital pharmacies—throughout Benghazi. A structured questionnaire was used to gather data on demographic profiles, professional background, awareness of guidelines, dispensing behavior, and perceived obstacles to compliance. The data presented in the study were descriptive analysis and person correlation was used for statistical significant differences. While 56% of participants indicated some awareness of national or international antibiotic guidelines, only 28% reported having undergone formal training in antimicrobial stewardship. Notably, 77% admitted to dispensing antibiotics without prescriptions, often driven by patient requests, assumptions about symptom severity, and limited enforcement of regulations. Only 30% regularly engaged in educating patients on appropriate antibiotic use. Furthermore, 71% reported facing moderate to significant difficulties in adhering to dispensing standards. Proposed solutions to improve compliance included specialized training (59%) and stronger regulatory enforcement (54%).Challenges prevent from following guidelines shown closest to significance (r = 0.178, p = 0.077), suggesting a weak trend that might warrant further study. This study reveals a significant discrepancy between pharmacists’ awareness and their actual dispensing practices in Benghazi. Addressing this issue requires reinforcing regulatory policies, expanding targeted educational programs, and fostering greater public understanding of antibiotic use to effectively combat the growing threat of AMR.Keywords: antibiotics, dispensing, knowledge, practices, pharmacy, pharmacists, guidelines
Procedia PDF Downloads 101265 Mesdopetam: A Selective D3 Antagonist Targeting Levodopa-Induced Dyskinesia
Authors: Munirah Alzafiri
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Levodopa-induced dyskinesia is a disabling complication of long-term Parkinson’s disease treatment, with limited therapeutic options currently available. This Phase 2b randomized, double-blind, placebo-controlled trial evaluated the safety and efficacy of mesdopetam, a selective dopamine D3 receptor antagonist at doses of 2.5 milligrams, 5 milligrams, and 7.5 milligrams twice daily over 12 weeks. Although mesdopetam did not meet the primary endpoint which is improvement in daily functional time without troublesome involuntary movements compared to placebo , patients receiving 7.5 milligrams twice daily showed notable improvement in secondary measures, including a 12.9-point reduction on the Unified Dyskinesia Rating Scale, with 71.4% achieving at least an eight-point drop, compared to 51.5% on placebo. Motor function remained stable and a dose-dependent reduction in motor OFF time was observed. Mesdopetam was well tolerated with no cognitive decline or hallucinations and most adverse events were mild. These findings suggest that mesdopetam is well tolerated and is a promising candidate for future clinical development.Keywords: D3 receptor antagonist, dyskinesia, mesdopetam, D3 Parkinson’s disease, receptor antagonist
Procedia PDF Downloads 111264 Evaluating the Anxiolytic Potential of Cannabidiol: A Critical Analysis of Efficacy
Authors: Munirah Alzafiri
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Anxiety disorders are among the most prevalent mental health conditions affecting millions worldwide. The search for effective treatments has led to increased interest in cannabidiol (CBD) as a potential anxiolytic agent. This study critically evaluates the efficacy, safety, and cognitive effects of CBD in the management of anxiety disorders, particularly social anxiety disorder (SAD). A meta-analysis, along with clinical trial data, suggests that CBD demonstrates significant anxiolytic properties with a favorable safety profile. However, variations in dosing, study designs, and treatment durations present challenges in drawing definitive conclusions. Compared to traditional pharmacological interventions such as SSRIs and benzodiazepines , CBD offers potential cognitive benefits while minimizing adverse effects. Despite promising findings, limitations such as small sample sizes, short treatment durations, and methodological heterogeneity highlight the need for further large-scale, long-term research. This analysis underscores the importance of refining CBD-based therapies to optimize their clinical application in anxiety management.Keywords: anxiety disorders, cannabidiol, cognitive effects, social anxiety disorder
Procedia PDF Downloads 91263 The Impact of Comorbid Conditions on Healthcare Expenditures Among Adults with Prostate Cancer Diagnosis in the United States
Authors: Isaiah Olumeko, Gladys Jacobs Dick
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Introduction: Prostate cancer continues to affect a growing number of men in the United States, raising serious public health concerns. It has been projected that by 2025, there will be around 313,780 new cases and 35,770 deaths linked to the disease. In 2021, the total national expenditure on prostate cancer care was approximately $22.3 billion. Updated research on how comorbid conditions drive healthcare spending among this unique population. As previous clinical data-based studies may be outdated. This study aims to use real-world data to examine the impact of comorbid conditions on healthcare expenditures among adults with prostate cancer. Methods: A retrospective cross-sectional study was conducted using the Medical Expenditure Panel Survey (MEPS) from adult men (≥ 18 years) with prostate cancer, categorized by comorbidities (≤1, 2, and 3+). Covariates included age, race, income, education, perceived health status, region, insurance, and smoking status. Measures of healthcare expenditure used in this study are the total healthcare expenditure, inpatients, prescription medicines, office-based visits, outpatients, and emergency visits. Weighted descriptive analyses were conducted to examine baseline characteristics across the three comorbidity groups. An adjusted linear regression model was employed using SAS version 9.4 to examine differences in healthcare expenditure estimates. Results: The cohort included 1,539 participants (weighted: 16,091,423). Among them, 25.60% had one or no comorbid condition, 24.17% had two, while 50.23% had three or more comorbid conditions. After adjusting for covariates, individuals with one or no comorbid condition incurred significantly lower total healthcare expenditures compared to those with 3+ comorbidities (%ΔEE: +221%, p < 0.0001). Outpatient expenditures were significantly lower among those with ≤1 comorbidity than those with 3+ (%ΔEE: +319%, p < 0.0001), and the same pattern held for inpatient services. For prescription medications, spending was lower among those with ≤1 comorbidity compared to individuals with 2+ (%ΔEE: +184%, p = 0.001) and those with 3+ comorbidities (+920%, p < 0.0001). In contrast, emergency department spending did not differ significantly across the groups. Conclusion: Comorbid conditions are linked to significantly higher healthcare expenditures among adults with prostate cancer. The obvious cost differences were observed in inpatient, outpatient, and prescription services. This underscores the importance of integrated care strategies aimed at managing comorbidities and reducing financial strain in this population.Keywords: prostate cancer, comorbid conditions, healthcare expenditures, healthcare utilization
Procedia PDF Downloads 191262 Mycotoxins Occurrence Algerian Wheat Collected from Two Climatic Regions in Algeria
Authors: Riba Amar, Hayat Khouni, Jalila Ben Salah-Abbès, Tiziri Badji
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In the current paper, a multi-mycotoxin analysis of twenty-two mycotoxins in 202 durum wheat samples collected in Algeria from 2019 to 2021 was performed by UHPLCMS/MS. Enniatins were present in 2 out of 45 wheat samples in the 2019 harvest. Whereas, in the harvest of 2020, 37.6% of wheat samples were found contaminated by ochratoxin A and/or beauvericin, deoxynivalenol(1076 µg/kg), fumonisin B1, enniatins and zearalenone (most prevalent in 2020 and 2021 harvest). Mycotoxin contamination increased from 37.6% in 2020 to 55.2% in 2021 harvests. The most frequently observed mycotoxin co-occurrence was the combination of enniatin A1, enniatin B and enniatin B1 (0.5- 126 µg/kg) and DON (1307 µg/kg). Finally, AFB1 (0.4-2.6 µg/kg) was detected in only one sample collected from the continental region. These results pointed to the necessity of frequent and rigorous wheat quality controls in order to better evaluate the risk regarding the Algerian population.Keywords: mycotoxins, co-occurrence, wheat, climatic change, Algeria
Procedia PDF Downloads 151261 Dermal Fibroblasts Secretomes as Bioactive Agents for Wound Healing: in vitro Performance Assessment
Authors: María F. Arraño, Ricardo Ceriani, Andrea Tapia-Bustos, Caroline Weinstein-Oppenheimer
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Chronic wounds present a significant clinical challenge due to their inability to heal spontaneously. These injuries affect approximately 1% of the global population, with higher prevalence among the elderly and individuals with chronic conditions such as diabetes. While various therapeutic approaches have been developed, their effectiveness remains limited. Among emerging strategies, secretomes derived from mesenchymal stem cells have garnered attention for their ability to accelerate wound healing through anti-inflammatory, anti-apoptotic, pro-angiogenic, and immunomodulatory properties. These secretomes, comprising a complex mixture of soluble factors and extracellular vesicles, enhance wound repair by promoting cell proliferation, migration, and the expression of key genes involved in tissue regeneration. Despite their promising regenerative potential, secretome particularly those derived from dermal fibroblasts remain an underexplored area of research. Investigating their biological effects could lead to novel therapeutic advancements, offering innovative solutions for treating chronic wounds. This study aimed to evaluate the effects of the secretome derived from human dermal fibroblasts on proliferation, migration, and the mRNA expression of VEGF, collagen type I, and collagen type III on human dermal fibroblasts. Cell proliferation was assessed using the CyQUANT™ assay, while migration was analyzed through in vitro wound healing assays. Transcript expression was measured via reverse transcription coupled with quantitative real-time PCR. The results demonstrated a significant increase in fibroblast proliferation, at secretomes concentrations of 100 and 1000 ng/mL, which was accompanied by enhanced migration, effectively reducing the wounded area at both concentrations. Additionally, key genes associated with tissue regeneration VEGF, implicated with new blood vessels formation, collagen type I, and collagen type III, related to extracellular matrix formation—showed increased expression on dermal fibroblasts exposed to secretomes at 10 to 1000 ng/mL. Cell proliferation is relevant to rebuild the dermal tissue during the wound healing process, as it is fibroblast migration and secretion of the evaluated molecules. These findings suggest that the fibroblast-derived secretome holds substantial promise as a therapeutic tool for tissue engineering. This study was funded by regular FONDECYT 1251144.Keywords: bioactivity, gene expression, medical device, secretomes.
Procedia PDF Downloads 161260 Famotidine/Diclofenac Sodium Novel Gastroretentive Bilayer Tablet Dosage Form: Formulation, Optimization and Characterization Studies
Authors: Sara Altamimi, Abdelkader Metwally, Abdelazim Zaghloul
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Background/objectives:Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed for the management of pain due to their analgesic and anti-inflammatory properties. Their long-term use is associated with numerous side effects, such as gastric bleeding and ulceration. These side effects can be reduced by using gastroprotective agent(s). The main objective of this study is to prepare and characterize a bilayer tablet containing famotidine (FA); a histamine H2 receptor antagonistand diclofenac sodium (DS); a NSAID in a single tablet dosage form. This combination is intended to reduce the gastrointestinal complications associated with the long-term use of DS, improve the bioavailability of both medications, and increase patient compliance.Methods: A gastric floating tablet was prepared by mixing 40 mg FA with 80 mg HPMC K15M, 20 mg sodium bicarbonate,and other excipients to reach 200 mg. The enteric tablet was prepared by mixing 100 mg DS, 37.5 mg Eudragit® L100-55, 37.5 mg HPMC K15M, and other excipients to reach 250 mg. The powder blend wasassessed for flowability and compressibility.FA and DS tablets werecompressed using a single punch tablet compression machine and were characterized for uniformity of weight,thickness, drug content, hardness, friability, and drug release in 0.1 N HCl for FA and phosphate buffer pH 6.8 for DS. As FA tablets are intended to remain in the stomach, they were evaluated forinvitro buoyancy.The bilayer tablet was prepared by stacking the sustained enteric layer,middle separating layer, andfloating gastroretentive layer in the die cavity of the compression machine. DSC and FTIR analysis wereperformed to determine the tablets’ physicochemical compatibility. The design of experiments (DOE) was applied to reach the optimized formulation. Results:The powder blend showed acceptable flowability and compressibility. The characterization results of the prepared tablets were within the pharmacopeial limits. The cumulative percentage of drugs released after 12 hours was95% for FA and 98% for DS. The bilayer tablet was separated into two tablets in few seconds after immersion in0.1N HCl. Conclusions: Formulating a bilayer tablet containing FA and DS is expected to yield significant outcomes that will enhance therapeutic efficacy, safety profile, and patient compliance.Keywords: famotidine, diclofenac sodium, gastroretentive drug delivery, bilayer tablets, formulation, optimization and characterization
Procedia PDF Downloads 131259 Examining the Association Between Quality of Life and Healthcare Expenditure Among Older Adults with Arthritis in the United States
Authors: Samuel C. Ofili, Paroma Arefin, Somtochukwu M. R. Nwajiobi, Sujit S. Sansgiry
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Arthritis is a major chronic condition that affects a significant portion of the population, especially among older adults. In the United States, more than 65 million people live with arthritis, which has emerged as a leading contributor to disability. This condition reduces mobility and daily functioning and substantially affects individuals' physical, mental, and emotional well-being. The financial burden is also considerable, with annual healthcare costs surpassing $600 billion, and those affected by arthritis spend approximately $1,000 more annually on healthcare compared to individuals without the condition. Despite the high healthcare utilization among this population, there is a notable gap in research exploring the connection between healthcare expenditures and quality of life, which could improve care strategies and guide future policy. Thus, this study aims to evaluate the association between perceived quality of life and healthcare expenditures and to identify factors associated with increased spending among older adults with arthritis in the United States. This retrospective cross-sectional study used data from the 2018–2022 Medical Expenditure Panel Survey (MEPS). The analysis included adults aged 65 years and older with a diagnosis of arthritis. Quality of life was measured using self-reported physical and mental health scores on a scale from 1 (poor) to 5 (excellent). Descriptive statistics summarized sample characteristics, and survey-weighted linear regression models were used to assess the association between quality of life and total annual healthcare expenditures, adjusting for relevant covariates. Analyses were performed using SAS V9.4. The study included 16,073 participants, representing a weighted population of 31.6 million older adults with arthritis. The sample was predominantly female (60.8%), aged 65–74 (55.2%), and non-Hispanic White (74.9%). Most were publicly insured (55%), held a high school diploma (51%), and were unemployed (82.4%). Unadjusted analyses indicated that individuals with poor physical and mental health had the highest mean annual healthcare expenditures, $32,985 (95% CI: $28,867–$37,101) and $22,397 (95% CI: $19,303–$25,489), respectively. In contrast, those reporting excellent physical and mental health had the lowest expenditures, $9,162 (95% CI: $8,251–$10,073) and $12,786 (95% CI: $11,964–$13,606), respectively. A clear inverse relationship was observed: healthcare expenditure decreased as perceived health status improved. This trend persisted after adjusting for confounders. Compared to those with poor health, individuals with excellent physical and mental health had 63% and 30% lower healthcare expenditures, respectively (both p < 0.0001). Similarly, those with good physical and mental health had 52% (p < 0.0001) and 24% (p = 0.04) lower expenditures, respectively. Additional factors significantly associated with higher healthcare costs included sex, age, race, insurance coverage, geographic region, number of chronic conditions, educational attainment, and employment status. Among older adults with arthritis, better self-reported quality of life, both physical and mental, was strongly associated with significantly lower healthcare expenditures. These findings highlight the economic burden of poor health status and underline the importance of interventions aimed at improving the quality of life in this population. Several sociodemographic and clinical factors were also identified as contributors to increased healthcare spending, offering potential targets for cost-reduction strategies.Keywords: arthritis, quality of life, united states, healthcare expenditure, older adults.
Procedia PDF Downloads 141258 Comprehensive Phyto Pharmacognostical Profiling, Isolation of Strophanthidin, HPTLC Method Development and Anticancer Evaluation of Corchorus aestuans L., Corchorus olitorius L., and Corchorus trilocularis L.
Authors: Carol P. Macwan, Tejal G. Soni, B. N. Suhagia
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The plants known as ‘Jute’ C. aestuans L., C. olitorius L., and C. trilocularis L. (Family - Tiliaceae) grow as weeds in India and other countries during the rainy season. Their cardiotonic and anticancer characteristics make them valuable in Ayurveda for treating diuresis, gonorrhoea, digestive disorders, urethritis, and pneumonia. This work established pharmacognostic and phytochemical characteristics, isolated the cardiotonic principle, and validated anticancer properties. The leaves of all three plants were examined for morphology, microscopy, and quantitative microscopy for stomatal index, veinislet number, vein termination number, and palisade ratio. Total ash, acid-insoluble ash, water-soluble ash, sulphated ash, alcohol-soluble extractive value, and water-soluble extractive value were measured. The powders of C. aestuans L., C. olitorius L., and C. trilocularis L. stems, roots, leaves, and seeds were also tested for phytochemical properties. Stems of all three species contained sugars, tannins, sterols, triterpenoids, flavonoid glycosides, saponins, and mucilage. Roots had sugars, tannins, sterols, triterpenoids, saponins, and mucilage. Leaves contained sugars, tannins, sterols, triterpenoids, flavonoid glycosides, saponins, and mucilage. C. olitorius L. leaves had cardiac glycosides, unlike the other two species. All three species' seeds contained sugars, tannins, sterols, triterpenoids, cardiac glycosides, saponins, and mucilage. For the first time, morphological, microscopic, powder characteristics, quantitative microscopic, physicochemical, and preliminary phytochemical screening parameters have been determined for C. aestuans L., C. olitorius L., and C. trilocularis L. stems, roots, leaves, and seeds. These parameters can be used to set standards for these Phytoconstituent isolated from C. aestuans L. seeds using column chromatography were identified as strophanthidin by UV, FT-IR, 1H-NMR, 13C-NMR, and MS/MS. A HPTLC method for strophanthidin measurement was developed and validated for linearity, precision, accuracy, specificity, detection limit, and quantification limit. The method was simple, linear, precise, accurate, specific, reproducible, and suitable for routine plant analysis and authentication, quantifying strophanthidin content in C. aestuans L. seeds, C. olitorius L. leaves, and C. trilocularis L. seeds. The plant's anticancer potential was tested against numerous cell lines, and the cytotoxicity test on normal cells showed that all samples were harmless. The A-375 malignant melanoma cell line was significantly cytotoxic by the methanol extract of C. olitorius L. and C. trilocularis L. seeds and leaves. Methanol extract of C. trilocularis L. leaves and C. aestuans L. seeds cytotoxic on K-562 chronic myelogenous leukaemia cells. The HEP-3B hepatocellular carcinoma cell line rejected all test samples. For a detailed mechanistic study, agarose gel electrophoresis showed that the methanol extract of C. trilocularis L. leaves and the seeds of C. olitorius L. and C. trilocularis L. showed a remarkable DNA fragmentation pattern, confirming apoptosis rather than necrosis.Keywords: corchorus, pharmacognosy, phytochemistry, anticancer
Procedia PDF Downloads 141257 Difference in Physical and Mental Health Status Across Racial Groups Among Elderly Patients Diagnosed with Prostate Cancer in the United States
Authors: Isaiah Olumeko, Gladys J. Dick, Somtochukwu M. R. Nwajiobi
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Introduction: Prostate cancer is the second most common cancer in men and the fifth leading cause of cancer death worldwide. Around 60% of cases occur in men aged ≥65, with an average diagnosis age of 66–67. Updated research on health-related quality of life (HRQOL), particularly physical and mental health in older adults, is essential for informing interventions. As prior studies based on clinical data may be outdated. This study aims to use real-world evidence to assess HRQOL differences across racial groups and identify factors associated with HRQOL among older adults with prostate cancer. Method: A retrospective cross-sectional study was conducted using data from the Medical Expenditure Panel Survey (MEPS) from 2018 to 2022. The study focused on adults aged ≥65 years who had a diagnosis of prostate cancer and reported scores for perceived physical and mental health. In MEPS, these scores were derived from single-item self-reports using a 5-point Likert scale (1 = Excellent, 2 = Very Good, 3 = Good, 4 = Fair, 5 = Poor). For analysis, the scores were reverse-coded so that higher values indicated better health-related quality of life (HRQOL). Descriptive, weighted analyses were conducted to examine patient characteristics across key racial/ethnic groups, including Non-Hispanic Whites (NHWs), Non-Hispanic Blacks (NHBs), and Hispanics. To evaluate differences in perceived physical and mental health status, linear regression models adjusted for covariates were employed using SAS version 9.4. Results: The cohort comprised 1,215 older adults (weighted n = 12,209,891) with prostate cancer. NHWs made up 73.90% of the sample, followed by NHBs (18.77%) and Hispanics (7.33%). NHWs reported significantly higher HRQOL scores for physical (3.35 ± 0.05) and mental health (3.76 ± 0.05) than Hispanics (3.24 ± 0.20; 3.61 ± 0.24) and NHBs (3.09 ± 0.09; 3.64 ± 0.12) (p < 0.001); these differences remained after covariate adjustment. Participants with ≥5 comorbidities had lower scores compared to those without comorbidity (physical: β = -1.07, p < 0.0001; mental: β = -0.71, p = 0.001). Compared to individuals without a degree, those with a master’s/doctorate had higher HRQOL (physical: β = 0.41, p = 0.024; mental: β = 0.60, p = 0.0001). Similarly, those with higher income showed better outcomes than lower-income groups (physical: β = 0.45, p = 0.001; mental: β = 0.32, p = 0.0163). Adults ≥80 years had significantly poorer mental health scores than those aged 65–79 (β = -0.31, p = 0.002). Conclusion: These findings highlight significant differences in physical and mental health-related quality of life among older adults with prostate cancer, particularly across racial/ethnic groups. Education, comorbidities, income, and advanced age are factors that can affect HRQOL.Keywords: prostate cancer diagnosis, mental health status, physical health status, racial groups
Procedia PDF Downloads 311256 Ethnobotanical Insight into Sickle Cell Disease Management: A Comprehensive Study of Traditional and Bioactive Components of Medicinal Plants Utilized in Ondo Local Government Area, Ondo-State, Nigeria
Authors: Olanipekun Mary Kehinde, Olanipekun Ayomide Damilola
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This research provided an in-depth ethnobotanical analysis of medicinal plants used in managing sickle cell disease in Ondo West Local Government Areas of Ondo State, Nigeria. Through the administration of semi-structured questionnaires, interviews and discussions data were collected from traditional healers, herb sellers, and knowledgeable locals. A total of 30 plant species belonging to 23 different families were identified and documented. The family of Fabaceae is the most represented with three medicinal plant species. Most of the plant species were Herbs (67%), followed by trees (19%) and shrubs (14%). The plant parts used were Leaves (57%), Fruits (27%), roots (12%), seed (6%), and whole plant (3%) respectively. The whole part of Aristolochia and Newbouldia laevis plants were used. The mode of preparation and administration ranges from decoction (60%), powder (13%), infusion (10%), maceration and juice (6.7%), and chewing (3.3%) respectively. The study identified and authenticated the properties and bioactive composition of the leaves of the commonly mentioned medicinal plants, Justicia carnea and Carica papaya. The Carica papaya contains more alkaloids 24.540±24.53 than Justicia carnea with 5.880±5.85. Also, the Flavonoids present in Justicia carnea amounted to 155.246±155.26 while Carica papaya had 36.232±36.25. The findings justified the importance and potential of botanical knowledge as an alternative or supplementary treatment for sickle cell disease. This study not only validates the ethnobotanical practices in the region but also offers a foundation for future pharmacological research.Keywords: ethnobotany, sickle cell disease, medicinal plants, alternative medicine, bioactive ingredients
Procedia PDF Downloads 211255 Inorganic Nanomaterial-Based Chemo-Photothermal Therapy for Cancer
Authors: Swati Biswas, Sneha Das, Tonmoy Banerjee
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Oral cancer, especially squamous cell carcinoma as its most common subtype, continues to pose a serious global health threat—impacting over 300,000 individuals and accounting for nearly 140,000 deaths each year. In recent years, advances in targeted drug delivery systems have opened new avenues in treatment, particularly through the integration of photothermal and photodynamic therapies alongside traditional chemotherapy. These approaches aim to localize therapeutic effects while minimizing systemic toxicity. Graphene has emerged as a promising material in this domain due to its excellent photothermal conversion properties. However, pristine graphene presents significant challenges: their hydrophobic nature and limited biocompatibility can trigger cytotoxic responses. To address these limitations, this study focused on engineering a biodegradable nanocarrier composed of graphene oxide (GO) and tannic acid (TA), leveraging π-π stacking interactions for stable assembly. GO was synthesized via a modified Hummers method, followed by non-covalent functionalization with TA to enhance biocompatibility and introduce drug-binding sites. A proteasomal inhibitor (PI) was subsequently conjugated to the TA-GO complex via ester bond formation, enabling controlled release under physiological conditions. Comprehensive characterization of the nanosheets was conducted through both physicochemical and biological assessments, including in-vitro and in-vivo models. The resulting nano platform demonstrated efficient drug encapsulation, time-dependent cellular uptake, and potent anticancer activity. In vivo studies in tumor-bearing mice revealed enhanced tumor targeting, high therapeutic payload delivery, and superior apoptosis induction, mediated by the dual-action mechanism of photothermal therapy and proteasome inhibition. This tailored delivery system not only improves the therapeutic index but also provides a foundation for the development of multifunctional nanomedicines in oral cancer treatment.Keywords: graphene oxide, drug delivery, nanomedicine, photothermal-chemotherapy
Procedia PDF Downloads 201254 A Comprehensive Analysis of Predictors for Drug-Related Problems Among Ambulatory Patients with Chronic Kidney Disease in a Nephrology Outpatient Setting
Authors: Khurshid Alam, Mahmood Basil A. Al Rawi, Amer Hayat Hayat Khan, Irfanullah Khan, Hira Naz
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Drug-related problems refer to any situation or event associated with drug therapy that could potentially disrupt or interfere with a patient’s intended clinical outcome. While numerous predictors of drug-related problems have been identified, further investigation is needed in outpatient settings for patients with chronic kidney disease (CKD). Therefore, this study aimed to conduct a comprehensive analysis of predictors for DRPs among ambulatory CKD patients attending outpatient nephrology clinics.A single-arm, pre- and post-intervention study design was employed. Adult patients diagnosed with CKD stages 1 to 5 who were receiving treatment and follow-up care at Khyber Teaching Hospital (KTH) and Medical Teaching Institution (DHQ), Khyber Pakhtunkhwa (KPK), Pakistan, were enrolled. The recruitment phase spanned from February to June 2022, with follow-up conducted between March and July 2022.Data were analyzed using SPSS version 26. A two-sided p-value of less than 0.05 was considered statistically significant. The study used multivariable logistic regression models to identify predictors of DRPs. Initially, simple binary logistic regression was applied to explore the associations of various sociodemographic and clinical variables, including gender, age, body mass index (BMI), employment status, education, income, number of medications, and CKD stages (measured by eGFR), with the occurrence of DRPs. Variables showing p-values <0.05 were included in the multiple logistic regression analysis.Key findings revealed that several variables significantly predicted different types of DRPs. Patients with CKD stage 3 (eGFR 45–59 ml/min) were 8.838 times more likely to receive wrong prescriptions compared to those with stage 1 CKD (eGFR >90 ml/min) (95% CI: 2.211–35.326, P=0.002). Similarly, patients prescribed 7 to 8 medications had 14.272 times higher odds of experiencing DRPs compared to those on 1 to 2 medications (95% CI: 2.650–76.871, P=0.002). Poor adherence was also significantly associated with polypharmacy; patients taking 7–8 medications were 5.175 times more likely to show poor adherence than those taking fewer medications (P=0.014).Unemployment within the household was associated with a 5.303-fold increased likelihood of receiving incorrect prescriptions (95% CI: 1.128–24.929, P=0.035). Income level was another significant factor. Patients earning PKR 30,000 to 50,000 had 6.004 times higher odd ratio of receiving duplicate prescriptions with similar effects (95% CI: 1.548–23.297, P=0.010) and a 3.096-fold increased likelihood of poor medication adherence (95% CI: 1.140–8.412, P=0.027).In terms of contraindicated medications, stage 3 CKD patients had a 7.132-fold increased risk of being prescribed such drugs (95% CI: 2.075–24.514, P=0.002). Moreover, patients with a BMI of 18.5–24.5 were 30 times more likely to receive subtherapeutic dosages (95% CI: 3.855–233.441, P<0.1). In conclusion, this study highlights multiple sociodemographic and clinical factors that significantly contribute to DRPs among ambulatory CKD patients. Stages of CKD, polypharmacy, employment status, income level, and BMI were all key predictors. These findings emphasized the importance of individualized patient assessment, targeted interventions, and multidisciplinary collaboration in reducing the burden of DRPs in this population. The insights gained can aid healthcare professionals in developing tailored strategies to enhance medication safety and therapeutic outcomes for CKD patients in outpatient settings.Keywords: chronic kidney disease, ambulatory patients, predictors, drug-related problems, outpatients, estimated glomerulus filtration
Procedia PDF Downloads 221253 Preformulation Studies and in vivo Testing of the Ethanolic Extract of Swietenia macrophylla Seeds as an Anti-Melanogenic Agent
Authors: Catherine Mae C. Cuya, Sofia Antonienne Allarde, Kent Vinzcent R., De Castro, Ma. Alysson C. Dedell, Amerah M. Maruhom, Marielle Jazmin A. Sebastian, Omar A. Villalobos, Irish Mhel C. Mitra, Mary Jho-Anne T. Corpuz
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The increasing demand for safer and eco-friendly dermatological treatments has driven interest in natural alternatives for skin disorders. This study explored the potential of ethanolic seed extract from Swietenia macrophylla as an anti-melanogenic agent, with the goal of developing a preformulated dosage form. The extract underwent physicochemical evaluation and organoleptic assessments to determine its stability and suitability for formulation. To confirm its anti-melanogenic activity, zebrafish (Danio rerio) embryos were used as an in vivo model, where imaging techniques assessed melanin inhibition. Additionally, toxicity classification, survival, and mortality rates, and ocular melanin content were analyzed across three replicates. Data were subjected to one-way analysis of variance (ANOVA) and post-hoc Tukey test, with results expressed as mean ± standard deviation. Furthermore, excipient compatibility and stability testing under controlled conditions were conducted to ensure the formulation’s stability and efficacy. The findings demonstrated the potential of S. macrophylla as a natural anti-melanogenic agent, paving the way for its application in cosmetic and dermatological formulations.Keywords: Swietenia macrophylla, anti-melanogenic, zebrafish, ethanolic extract, excipient compatibility, stability testing, cosmetic formulation
Procedia PDF Downloads 271252 The Impact of the Improved Pricing Regulations on Price Revision of Registered Pharmaceutical Products at Renewal Phase in Years 2019-2023
Authors: Sara Alhassan
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The Saudi Food and Drug Authority (SFDA) sets pricing rules for pharmaceutical products to promote fair pricing and ensure equitable access to essential drugs. The registration of pharmaceutical products is valid for five years for each concentration, medicinal formula, or package and the price is revised at the renewal phase based on the common pricing criteria outlined in the pricing guidelines. Revising the product price will determine the pricing department's recommendation if the product price will be reduced or remain at the same current price. The previous practice (2019-2021) for repricing medicines was based on reviewing all pharmaceutical products according to criteria specified in the previous pricing guidelines. After establishing the new pricing guidelines in the year 2021, which aimed to ensure fairness and equitable access to essential medicines by regulating the prices. The prices of pharmaceutical products should be set at an affordable level for all stakeholders, including patients, healthcare providers, and governments. This study aims to examine the impact of the new regulation of pharmaceutical pricing on the practice of the pharmaceutical renewal registration phase at SFDA. By Measuring and comparing different variables as the number of applications submitted for renewal reversion to the number of applications closed without price reductions versus the number of applications eligible for price reductions and the number of appeals to the approved prices after the revision. These findings will provide valuable insights into the effectiveness and efficiency of the new pricing practice established by the SFDA.Keywords: pricing regulations, price revision, pharmaceutical products, renewal phase
Procedia PDF Downloads 261251 The Effect of Artificial Intelligence on Pharmacology Development
Authors: Ramy Reda Morgan Kamel
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The idea of myocardial injury, despite the fact that first identified from animal studies, is now identified as a clinical phenomenon which can bring about microvascular harm, no-reflow phenomenon, myocardial lovely, myocardial hibernation and ischemic preconditioning. The final result of this occasion is left ventricular (LV) systolic disorder main to elevated morbidity and mortality. the standard scientific case of reperfusion damage takes place in acute myocardial infarction (MI) with ST segment elevation wherein an occlusion of a major epicardial coronary artery is accompanied through recanalization of the artery. this will arise either spontaneously or by thrombolysis and/or by means of number one percutaneous coronary intervention (PCI) with green platelet inhibition by using aspirin (acetylsalicylic acid), clopidogrel and glycoprotein IIb/IIIa inhibitors. In latest years, percutaneous coronary intervention (PCI) has emerge as a well-mounted approach for the remedy of coronary artery ailment. PCI improves symptoms in patients with coronary artery disorder and it's been increasing the safety of strategies. but, peri- and submit-procedural myocardial harm, including angiographical sluggish coronary float, microvascular embolization, and extended degrees of cardiac enzyme, along with creatine kinase and troponin-T and -I, has additionally been mentioned even in non-compulsory instances. moreover, myocardial reperfusion harm at the start of myocardial reperfusion, which reasons tissue damage and cardiac disorder, can also occur in cases of the acute coronary syndrome. due to the fact patients with myocardial damage is related to larger myocardial infarction and have a worse long-time period analysis than those without myocardial damage, it's far important to prevent myocardial harm throughout and/or after PCI in sufferers with coronary artery ailment. thus far, many studies have proven that adjunctive pharmacological treatment suppresses myocardial damage and increases coronary blood go with the flow throughout PCI strategies. in this evaluation, we spotlight the usefulness of pharmacological treatment in mixture with PCI in attenuating myocardial harm in sufferers with coronary artery disease.Keywords: electromagnetic solar system, nano-material, nano pharmacology, pharmacovigilance, quantum theoryclinical simulation, education, pharmacology, simulation, clinical pharmacology, pharmacometrics, career development pathways
Procedia PDF Downloads 201250 Locust Bean Gum and Chitosan on Metronidazole as Biopolymer Composite for Improved Colon Specific Drug Delivery
Authors: Titus Emmanuel Onugba, Joseph. C. Oguegbulu
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The reduced efficacy of metronidazole in the treatment of diarrheal diseases is mainly due to lower concentrations of the drug reaching the colonic site of action. Biopolymers like locust bean gum (LBG) and chitosan have been useful biopolymers in developing controlled-release matrices for drugs. In this work, efforts were made to develop a biopolymer composite of chitosan and LBG as coating films on metronidazole for improved colon-specific delivery of metronidazole. A ratio of 1:2 Chitoas/LBG was used to prepare four coating levels of biopolymer coating solution, F1, F2, F3, and F4, corresponding to 10%, 20%, 30%, and 40%, respectively, of average tablet weight. A dip-coating method was used to coat metronidazole tablets in triplicates. KH₂PO₄ and NaOH were used to prepare simulated colonic fluid USP (pH 6.8), while 0.1N HCl was used as simulated gastric fluid (pH 1.2) without enzyme. In vitro drug release studies showed that F4-coated tablets had the maximum drug release of 48% after I hr. in SGF. In SCF on the other hand, F4-coated tablets showed the lowest drug release of 60.3% after 30 minutes, with F3-coated tablets showing maximum drug release. Overall, our coated tablets show higher drug release in colonic medium compared to the gastric medium, suggesting that our developed pharmaceutical system may be capable of controlled release of metronidazole to the colonic site of action. These findings present an opportunity for modifications in the pharmaceutical formulation of metronidazole to improve its efficacy in the treatment of diarrheal infections, as well as larger implications for other drug formulations.Keywords: biopolymer composites, chitosan, dissolution studies, drug delivery, locust bean gum
Procedia PDF Downloads 251249 Knowledge of Antibiotics and Antibiotic Resistance Among Bangladesh Pharmacy Customers-a Study in Bangladesh
Authors: Md. Suman
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Objective: The main objective of this study was to evaluate the knowledge of antibiotic resistant among Bangladeshi pharmacy customers.Methods: Study was conducted among Bangladesh pharmacy customers different area in the Dhaka city. The questionnaire covered 1) Patients age-15 year to 50 years & sex are both male & female 2) knowledge of antibiotics and antibiotic resistance 3) Antibiotics use with or without registered doctor’s prescriptionResults: Among 524 participants, 60.4% (n=317) male & 39.5% (n=207) female, 40.2 %( n=211) had initial knowledge of antibiotics resistant in general and 59.7 %( n=313) had don’t have knowledge of antibiotic resistance. Simultaneously, more than 60.6 %( n=318) patient’s/Participant’s take antibiotics without doctor’s prescription from pharmacy as per dispenser advice they are always suggested antibiotics to the pharmacy customers when patient’s sufferer colds, influenza, cough & fever. Only 35.69% (n=187) patient’s take antibiotics with registered doctor’s prescription. Total number of participant 45.42% (n=238) patient’s take antibiotics Without registered doctor’s prescription as well as only 18.89% (n=99) take medicines without antibiotics. On the other hand prescription dispense by registered pharmacist 29.20 %( n=153) and prescription dispense by without pharmacist 70.80 %( n=371). Conclusions: High level of knowledge of antibiotics and antibiotic resistance among Bangladesh pharmacy customers, there are obvious knowledge gaps. We suggest that action is taken to increase the knowledge level, and particularly target people in vocational, male dominated occupations outside the health service.Keywords: antibiotics, antibiotics resistant, knowledge of antibiotics, miss use of antibiotics
Procedia PDF Downloads 261248 Chemical Synthesis of Antimicrobial Peptides and Studies of Their Enzymatic Stability
Authors: Olivier Ndogo Eteme, Victorine Ezami Meyomesse
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Objectives: Bacterial resistance to conventional antibiotics is a serious public health problem. Over the past decade, small proteins known as antimicrobial peptides (AMPs), natural compounds produced by all prokaryotic and eukaryotic cells, have shown promising results in overcoming the growing problems of antibiotic resistance. There are nowadays several cysteine-rich peptides of plant origin that have shown very good antimicrobial activities. The research of molecules with bactericidal activity with a lack of multi-resistance is always a current event. The present study was undertaken to investigate the in vitro antibacterial activities of four synthesized peptides obtained in 97% yield. Method: This reaction, by solid phase synthesis method was monitored by combining HPLC and LC/MS methods. The antibacterial test was performed using microdilution method. Results: The conformity and effectiveness of the synthesis of the peptides was carried out by LC/MS with an average yield of 97%. Both synthesized peptides were bactericidal on all tested strains, unless Neo1 which is bacteriostatic on E. coli ATCC 25922 strain. The biofilm eradication capacity test was carried out on two ATCC strains of S. epidermidis. Strain ATCC 35984 is a good biofilm-forming strain, while strain ATCC 12228 is considered a poor biofilm former. Comparison of the presence of biofilm between them showed a significant difference with p<0.05, showing that the controls used are significantly different in all cases. In addition, both synthesized peptides do not present hemolytic properties, therefore making them good drug candidates. Conclusion: Antimicrobial peptides are a good alternative today to fight against microbial resistance. So, new Neo synthesized peptides (Neo1, Neo2, Neo3 and Neo4) could serve as a basis for preclinical approaches to potential new active ingredients to combat certain microbial resistance.Keywords: solid phase synthesis, peptides, antibacterial activity, microbial resistance, protease stability
Procedia PDF Downloads 241247 An Approach to Develop Ionic Liquid Formulations for Enhanced Ibuprofen Delivery
Authors: Priyanka Shinde, Mukesh Bansal, Yeganeh Donyanavard, Sreekanth Pentlavalli, Adrian Kelly, Anant Paradkar
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This study aimed to investigate the feasibility of utilizing ionic liquid for the development of solid oral dosage forms of ibuprofen as conventional tablets. As Ionic liquids (ILs) are organic salts that contain anions and cations with melting points (Tm) and glass transition (Tg) below 100°C. Holding desirable properties such as high ionic conductivity, excellent solvents, low volatility, and thermal stability, for improving solubility and bioavailability of ibuprofen. Considering these properties, the research mainly focuses on creating a polymeric ionic mixture suitable for tablet production and investigating different formulation techniques to optimize the process. For preparation of Ibu-Ionic Liquid, API (Ibuprofen), Triethanolamine (Tea), Di iso propanolamine (Dipa) were used, followed by Polymers; PVA, PEO, PVP, HPMC-AS were used to create Polymeric Ionic liquid in various ratios such as (IL (TEA): HPMCA-AS 1:2.5, 1:3, 1:4, IL (TEA): PVA 1:2.5,1:3,1:4 and same with ionic liquid (DIPA) etc. The formed product then subjected to direct compression along with bulking agents and lubricant (Lactose, Calcium phosphate, Magnesium Stearate etc.) having varied concentration of each ingredient to optimize the formulation. Additionally, Different analytical tests were performed to support this finding such as thermal gravimetric analysis (TGA), Differential scanning colorimetry (DSC), Fourier transfer infra-red (FTIR), to check the composition of the formed Ionic Liquids and ILs polymeric mixture. The drug release profiles of the final formulations were assessed via dissolution studies. Conclusion: The generated ILs exhibited promising disintegration and dissolution profiles which can be used to formulate conventional oral tablets.Keywords: ibuprofen, Ils ionic liquids, ILs polymeric mixture, solubility, bioavailability
Procedia PDF Downloads 221246 Pharmaceutical Technology Formulation and Designing of Amlodipine Besylate Transdermal Patches (AMLOBES) by Solvent Evaporation Method
Authors: Tayba Akram
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The transdermal drug delivery is now a promising route for drug delivery systems. This route has the potential advantage of avoiding hepatic first-pass metabolism, decreasing side effects gastrointestinal effects, improving patient compliance and increasing bioavailability. The major limitation of this route is the difficulty of permeating the drug through the skin. The formulation is carried out to develop matrix-type transdermal patches containing Amlodepine besylate and polymer Eudragit by solvent casting method. Different ratios of Propylene glycol are used as plasticizers & Tween 80 is used as a permeation enhancer appropriate ratio of two solvents, ethanol and methanol, is used for effective mixing. The possible drug-polymer interactions were studied. Formulated transdermal patches were evaluated with regard to physicochemical characteristics, in-vitro permeation studies and stability studies. All the prepared formulations showed good physical stability. The in-vitro permeation studies were performed using the Franz diffusion cell. Out of all the formulated patches, F 8 showed good permeation in 24 hrs. So, these two formulations were selected as the best formulations.Keywords: drug delivery, gastrointestinal effect, Amlodepine besylate, Eudragit
Procedia PDF Downloads 261245 Resveratrol and Clobetasol-17-Propionate Co-administration to Manage Oral Lichen Planus: Embedding Actives-Loaded Lipid Microspheres Into a Patient-Friendly Buccal Patch
Authors: Giulia Di Prima, Maria Elena Mauceri, Giovanna Giuliana, Viviana De Caro
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Oral Lichen Planus (OLP) is a chronic, non-infectious inflammatory disease of the oral cavity characterized by symmetrical and bilateral lesions or multiple lesions affecting the buccal mucosa, the tongue, and the gingiva, causing severe pain and impairing patients’ quality of life. The conventional OLP treatment involves the topical administration of corticosteroids and clobetasol-17-propionate (CLB) remain the primary therapeutic option, even if there are no commercially available pharmaceutical forms intended for oromucosal application. An underestimated aspect of OLP pathogenesis is the role of oxidative stress. During inflammation, the generation of ROS is significantly enhanced. The latter can cause damage to several cellular components as protein, membrane lipids, nucleic acids, etc., inducing genetic mutations and playing a critical role in the potential malignant degeneration. A recent systematic review of over 1154 studies has demonstrated that antioxidants might not only effectively reduce pain but also increase the disease resolution rate and prevent potentially malignant outcomes. Among natural antioxidants resveratrol (RSV) is a polyphenol that was recently focused by researchers due to its biological actions by which it could be useful in the management of OLP in co-administration with conventional corticosteroids. However, both RSV and CLB suffer from several drawback related to their formulation and administration. Based on these considerations, the aim of this work was to develop novel, personalizable and patient-friendly drug delivery systems for the loco-regional clinical administration of CLB or co-administration of CLB+RSV to treat OLP lesions in order to evaluate both i) the clinical efficacy of stand-alone CLB when administered through a standardizable and innovative formulation instead of the conventionally used ones and ii) the clinical efficacy of the co-administration of the two selected active molecules, in terms of healing rate respect the control group (administration of a conventional CLB-loaded semisolid formulation). To address this issue while also overcoming the limitations of the chosen drugs a microcomposite patch was designed and characterized. Lipid-based microparticles (LMPs) as solid lipid microparticles (SLM) and microstructured lipid carriers (MLC) were then optimized to encapsulate CLB and RSV, respectively. The LMPs were prepared according to a patented technique and were accurately designed to be applied into the oral cavity. They thus resulted suitable in terms of melting temperature range (compliant with the oral temperature) and particle size (<450 μm). Moreover, in view of their next use for the preparation of the final dosage forms, they were further investigated as pharmaceutical intermediate in terms of particle shape and flow properties. Subsequently, two different buccal patches were prepared by dispersing the LMPs into a mucoadhesive hydrophilic gel then subjected to solvent casting: the CLB series patches were loaded only with the SLM-CLB, while the CLB+RSV series patches contained both SLM-CLB and MLC-RSV. Both formulations resulted soft, deformable, homogeneous, reproducible, mucoadhesive, low swellable and potentially comfortable for patients. Finally, their ex vivo ability to promote actives entry into the buccal tissue was also demonstrated, making them promising drug delivery systems for a further clinical trial actually in progress (Oral Medicine Unit, Palermo University Hospital Policlinico “P. Giaccone”).Keywords: buccal patch, clobetasol-17-propionate, lipid microparticles, oral lichen planus, resveratrol
Procedia PDF Downloads 361244 B12-Functionalized PEGylated Liposomes for the Oral Delivery of Insulin: In Vitro and in Vivo Studies
Authors: Susan Sarhadi, Seyedeh Alia Moosavian, Mohammad Mashreghi, Niloufar Rahiman, Shiva Golmohamadzadeh, Kayvan Sadri, Jamshidkhan Chamani, Mahmoud Reza Jaafari
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Orally administered Insulin has to survive the harsh gastrointestinal tract condition, penetrate the enteric epithelial barrier, and bypass the first pass effect before reaching the bloodstream. To address this problem, PEGylated liposomal insulin was prepared and modified with B12 to improve the stability and absorption of insulin in the gastrointestinal environment. Liposomes were prepared by film method plus extrusion, linked to B12, and characterized for their particle size, zeta potential, and encapsulation efficiency (EE%). The release profile in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were evaluated. The results indicated that B12-targeted PEGylated liposomes were more stable than non-functionalized Lip-PEG in SGF and SIF. In vitro, results showed significantly enhanced cellular uptake of B12-targeted PEGylated liposomes in Caco-2 cells compared to non-targeted liposomes. In the meantime, they had no toxicity on Caco-2 cells. In BALB/c mice, B12-targeted PEGylated liposomes showed higher insulin accumulation in the intestine and liver. In diabetic rats B12 targeted PEGylated liposomes provided higher insulin bioavailability compared with other formulations. These findings suggest that B12-targeted liposomes could be an effective formulation for oral delivery of insulin and merits further investigations.Keywords: insulin, liposomes, vitamin B12, oral delivery
Procedia PDF Downloads 321243 De-convolution Based IVIVC Correlation for Tacrolimus ER Tablet (Narrow Therapeutic Index Drug) With Widening of Dissolution Prediction for Virtual Bioequivalence
Authors: Sajad Khaliq Dar, Dipanjan Goswami, Arshad H. Khuroo, Mohd. Akhtar, Pulak Kumar Metia, Sudershan Kumar
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Background: Development of modified-release oral dosage formulations (OSD) like tacrolimus in narrow therapeutic categories, together with high levels of intra-individual variability, impose greater challenges. The risk assessment for bioequivalence studies requires developing a suitable design through pilot studies involving the comparison of multiple formulations of the same product with a marketed product to understand the in-vivo behaviour. These formulations could have varying coating levels and other minor quantitative differences to achieve the desired release rate for the final product. Although small-scale studies are critical before the conduct of full-scale Pharmacokinetic (PK) studies, regulatory agencies evaluate critical bioavailability attributes (CBA) before approving the submitted dossiers. Since Tacrolimus is a BCS Class II drug, therefore developing the extended-release formulation, in addition to associated challenges, provides an opportunity to present the In vitro-in vivo correlations (IVIVC) to regulatory agencies, not only to exhibit product quality but also to reduce the burden of additional human trials and cost involved to them for bringing the product to market. Objective: The objective of this study was to develop a Level-A In vitro - In vivo Correlation (IVIVC) model for Sun Pharma’s test formulation Tacrolimus ER tablet 4mg and extend its application to a widened dissolution window of 25% at 2.5 hours (critical release time) sampling time point. Experimental Procedure: Post the conduct of two in-vivo studies, a pilot study evaluating two test prototypes on 24 subjects (under fasting) and a pivotal study having 50 subjects (under fasting), the observed pharmacokinetic profile was used for IVIVC model development. The dissolution media used was 0.005% HPC + 0.25% SLS in Water 900 mL at pH 4.50 using USP II (Paddle) apparatus with alternative sinkers operated at 100 RPM. The sampling time points were chosen to mimic the drug absorption in vivo. The dissolution best fit to data was obtained using Makoid Banakar kinetics. Then deconvolution, anchoring to concepts of the single compartment by Wagner Nelson method was applied for tacrolimus slow-release formulation batch with film coating weight build-up of 5.4% (used in pilot bio study), medium release with Hypromellose (retard-release exhibit batch used in the pivotal study) and fast release formulation batch with film coating weight build-up of 5.05% (used in pilot bio study). Results and Conclusion: The results were deemed acceptable as prediction errors for internal and external validation were < 3% depicting in-vitro drug release mimics in-vivo absorption. Moreover, the prediction result for the Test/Reference ratio was <15% for all test formulations and widening dissolution (i.e., 39%-64% drug release at 2.5hrs) predictions were well within 80-125% when compared against Envarsus XR (reference drug). This IVIVC-validated model can be used in the futuristic exploration of dose titration with 1mg tacrolimus ER OSD as a surrogate for In-vivo bioequivalence trials.Keywords: pharmacokinetics, BCS, oral dosage form, Bioavailability, intra-individual variability
Procedia PDF Downloads 391242 Development of National Guidelines for Conducting Research and Development of Herbal Medicine in Thailand According to International Standards
Authors: Patcharaporn Sudchada, Nuntika Prommee
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Background: Herbal medicines constitute a vital component of Thailand's healthcare system and possess significant potential for international recognition. However, the absence of standardized clinical research guidelines aligned with international standards, coupled with unique local challenges, has hindered the development and registration of Thai herbal medicines in the global market. Objective: To establish comprehensive research and development guidelines for herbal medicine formulations that comply with international standards, with particular emphasis on enhancing research quality, scientific credibility, and facilitating both domestic registration and international market acceptance. Methods: The research methodology comprised eight sequential phases: (1) systematic collection and review of relevant documentation and regulatory frameworks; (2) development of preliminary content structure and template designs; (3) systematic analysis and synthesis of scientific evidence and regulatory data; (4) creation of detailed research guidelines and accompanying templates; (5) execution of domestic and international consultation meetings and study visits involving nine stakeholder groups; (6) systematic expert review of the draft guidelines; (7) incorporation of feedback from relevant regulatory and research agencies; and (8) finalization and validation of the comprehensive guidelines. Results: The study produced comprehensive research and development guidelines for herbal medicines that meet international standards, encompassing the complete development pathway from initial concept through pre-clinical studies, product development, preparation protocols, clinical trial conduct, and product registration procedures. The guidelines include standardized templates and forms specifically designed for clinical research documentation. Conclusion: The established guidelines represent a significant advancement in standardizing clinical research for Thai herbal medicines, enhancing their scientific credibility and potential for international acceptance. Nevertheless, Thailand continues to face specific challenges, including insufficient specialized personnel in herbal research (particularly in clinical trials), challenges in integrating traditional Thai medicine principles with modern scientific methodology, limited research infrastructure, inadequate funding mechanisms, complex registration procedures, and public skepticism toward herbal products. The policy recommendations outlined in this research provide a strategic framework for addressing these challenges and promoting sustainable development of Thai herbal medicines within the national context.Keywords: herbal medicine, clinical research, international standards, research guidelines, drug development, traditional thai medicine, regulatory compliance
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