Search results for: drug release metronidazole

Authors: Muhammad Imran Din

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The aim of this study was to understand the interaction between multi-walled carbon nano tubes (MCNTs) and anticancer agents and evaluate the drug-loading ability of MCNTs. Batch adsorption experiments were carried out for adsorption of 5-Fluorouracil (5-FL) using MCNTs. The effect of various operating variables, viz., adsorbent dosage, pH, contact time and temperature for adsorption of 5-Fluorouracil (5-FL) has been studied. The Freundlich adsorption model was successfully employed to describe the adsorption process. It was found that the pseudo-second-order mechanism is predominant and the overall rate of the 5-Fluorouracil (5-FL) adsorption process appears to be controlled by the more than one-step. Thermodynamic parameters such as free energy change (ΔG°), enthalpy change (ΔH°) and entropy change (ΔS°) have been calculated respectively, revealed the spontaneous, endothermic and feasible nature of adsorption process. The results showed that carbon nano tubes were able to form supra molecular complexes with 5-Fluorouracil (5-FL) by π-π stacking and possessed favorable loading properties as drug carriers.

Keywords: drug, adsorption, anticancer, 5-Fluorouracil (5-FL)

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Authors: Muhammad Yasir, Debarun Dutta, Mark Willcox

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Biomaterial-associated infections are a multi-billion dollar burden globally. Antimicrobial peptide-based coatings may be able to prevent such infections. The aim of this study was to investigate the mechanism of action surface bound peptides (AMPs) against Pseudomonas aeruginosa 6294. Melimine and Mel4 were covalently attached to glass coverslips using azido-benzoic acid. Attachment was confirmed using X-ray photoelectron spectroscopy. P. aeruginosa was allowed to attach to AMP-coated glass for up to 6 hours. The effect of the surface-bound AMPs on bacterial cell membranes was evaluated using the dyes DiSC3-(5), Sytox green, SYTO 9 and propidium iodide with fluorescence microscopy. Release of cytoplasmic materials ATP and DNA/RNA were determined in the surrounding fluid. The amount of cell death was estimated by agar plate counts. The AMPs were successfully covalently bound to the glass as demonstrated by increases in %nitrogen of 3.6% (melimine) and 2.3% (Mel4) compared to controls. Immobilized peptides disrupted the cytoplasmic membrane potential of P. aeruginosa within 10 min. This was followed by the release of ATP after 2 h. Membrane permeabilization started at 3 h of contact with glass coated AMPs. There was a significant number of bacteria (59% for melimine; 36% for Mel-4) with damaged membranes after 4 h of contact. At the 6 h time point, release of DNA occurred with melimine releasing 2 times the amount of DNA/RNA than Mel4 surfaces (p < 0.05). Surface bound AMPs were able to disrupt cell membranes with subsequent release of cytoplasmic materials, and ultimately resulting in bacterial death.

Keywords: biomaterials, immobilized antimicrobial peptides, P. aeruginosa, mode of action

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Authors: Zhaoguo Liu, Cunsi Shen, Yin Lu

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Growing evidence has shown that menthol has potent anticancer activity in various human cancers. However, its effect on skin cancer remains largely unknown. In the present study, we investigated the chemopreventive potential of menthol against 7, 12-dimethylbenz[a] anthracene(DMBA)/12-O-tetradecanoylphorbol 13-acetate (TPA)-induced skin tumorigenesis in ICR mice. Our results showed that menthol significantly inhibited TPA-induced inflammatory responses and pro-inflammatory cytokine release. We also found that menthol treatment significantly inhibited TPA-induced lipid peroxidation (LPO), mouse UDP-glucumno-syltransferase (UGT), mouse NADH Dehydrogenase, Quinone 1 (NQO1) release. Furthermore, we found menthol treatment significantly inhibited the tumor incidence and number of tumors (P < 0.001). Interestingly, we observed that menthol treatment significantly inhibited TPA-induced altered activity of NF-κB in skin tumor. Consistently, menthol-treated tumors also showed significantly suppressed the Ras-Raf-ERK signaling pathway. Thus, our results suggest that menthol inhibits DMBA/TPA-induced skin tumorigenesis by attenuating the Ras and inhibiting NF-κB activity via inhibition of inflammation responses and pro-inflammatory cytokine release.

Keywords: DMBA/TPA, NF-κB, Ras-Raf-ERK, skin tumorigenesis

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Authors: Shraddha Acharya, Sharad Kumar Sharma, Ratna Bhattarai, Bhagwan Maharjan, Deepak Dahal, Serpahine Kaminsa

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Background: Drug-resistant (DR) tuberculosis (TB) continues to be a threat in Nepal, with an estimated 2800 new cases every year. The treatment of DR-TB with second line TB drugs is complex and takes longer time with comparatively lower treatment success rate than drug-susceptible TB. Delay in treatment initiation for DR-TB patients might further result in unfavorable treatment outcomes and increased transmission. This study thus aims to determine median time taken to initiate second-line treatment among Rifampicin Resistant (RR) diagnosed TB patients and to assess the proportion of treatment delays among various type of DR-TB cases. Method: A retrospective cohort study was done using national routine electronic data (DRTB and TB Laboratory Patient Tracking System-DHIS2) on drug resistant tuberculosis patients between January 2020 and December 2022. The time taken for treatment initiation was computed as– days from first diagnosis as RR TB through Xpert MTB/Rif test to enrollment on second-line treatment. The treatment delay (>7 days after diagnosis) was calculated. Results: Among total RR TB cases (N=954) diagnosed via Xpert nationwide, 61.4% were enrolled under shorter-treatment regimen (STR), 33.0% under longer treatment regimen (LTR), 5.1% for Pre-extensively drug resistant TB (Pre-XDR) and 0.4% for Extensively drug resistant TB (XDR) treatment. Among these cases, it was found that the median time from diagnosis to treatment initiation was 6 days (IQR:2-15.8). The median time was 5 days (IQR:2.0-13.3) among STR, 6 days (IQR:3.0-15.0) among LTR, 30 days (IQR:5.5-66.8) among Pre-XDR and 4 days (IQR:2.5-9.0) among XDR TB cases. The overall treatment delay (>7 days after diagnosis) was observed in 42.4% of the patients, among which, cases enrolled under Pre-XDR contributed substantially to treatment delay (72.0%), followed by LTR (43.6%), STR (39.1%) and XDR (33.3%). Conclusion: Timely diagnosis and prompt treatment initiation remain fundamental focus of the National TB program. The findings of the study, however suggest gaps in timeliness of treatment initiation for the drug-resistant TB patients, which could bring adverse treatment outcomes. Moreover, there is an alarming delay in second line treatment initiation for the Pre-XDR TB patients. Therefore, this study generates evidence to identify existing gaps in treatment initiation and highlights need for formulating specific policies and intervention in creating effective linkage between the RR TB diagnosis and enrollment on second line TB treatment with intensified efforts from health providers for follow-ups and expansion of more decentralized, adequate, and accessible diagnostic and treatment services for DR-TB, especially Pre-XDR TB cases, due to the observed long treatment delays.

Keywords: drug-resistant, tuberculosis, treatment initiation, Nepal, treatment delay

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Authors: Nety Trisnawaty, Mirna Febriani

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The use of stainless steel wires in the field of dentistry is widely used, especially for orthodontic and prosthodontic treatment using stainless steel wire. The oral cavity is the ideal environment for corrosion, which can be caused by saliva. Prevention of corrosion on stainless steel wires can be done by using an organic or non-organic corrosion inhibitor. One of the organic inhibitors that can be used to prevent corrosion is black tea leaves extracts. To explain the comparison of chromium ions release for stainlees steel between artificial saliva and black tea leaves extracts. In this research we used artificial saliva, black tea leaves extracts, stainless steel wire and using Atomic Absorption Spectrophometric testing machine. The samples were soaked for 1, 3, 7 and 14 days in the artificial saliva and black tea leaves extracts. The results showed the difference of chromium ion release soaked in artificial saliva and black tea leaves extracts on days 1, 3, 7 and 14. Statistically, calculation with independent T-test with p < 0,05 showed a significant difference. The longer the duration of days, the more ion chromium were released. The conclusion of this study shows that black tea leaves extracts can inhibit the corrosion rate of stainless steel wires.

Keywords: chromium ion, stainless steel, artificial saliva, black tea leaves extracts

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Authors: Sperisa Distantina, Rieke Ulfha Noviyanti, Sri Sutriyani, Fadilah Fadilah, Mujtahid Kaavessina

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In this research, carrageenan extracted from seaweed Eucheuma cottonii was mixed with polyvinyl alcohol (PVA) and then crosslinked using glutaraldehyde (GA). The obtained hydrogel films were applied to control the drug release rate of paracetamol. The aim of this research was to develop a mathematical model that can be used to describe the mass transfer rate of paracetamol from the hydrogel film into buffer solution. The effect of weight ratio carrageenan-PVA (5: 0, 1: 0.5, 1: 1, 1: 2, 0: 5) on the parameters of the mathematical model was investigated also. Based on the experimental data, the proposed mathematical model could describe the mass transfer rate of paracetamol. The weight ratio of carrageenan-PVA greatly affected the amount of paracetamol absorbed in the hydrogel film and the mass transfer rate of paracetamol.

Keywords: carrageenan-PVA, crosslinking, glutaraldehyde, hydrogel, paracetamol, mass transfer

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Authors: Behcet Al, Şener Cindoruk, Suat Zengin, Mehmet Murat Oktay, Mehmet Mustafa Sunar, Hatice Eroglu, Cuma Yildirim

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Objective: In present study we aimed to investigate the chronic drug use due to chronic diseases in patients admitted to emergency department. Materials-Methods: 144 patients who applied to emergency department (ED) of medicine school of Gaziantep University between June 2013 and September 2013 with chronic diseases and use chronic drugs were included. Information about drugs used by patients were recorded. Results: Of patients, half were male, half were female, and the mean age was 58 years. The first three common diseases were diabetes mellitus, hypertension and coronary artery diseases. Of patients, %79.2 knew their illness. Fifty patients began to use drug within three months, 36 patient began to use within the last one year. While 42 patients brought all of their drugs with themselves, 17 patients brought along a portion of drugs. While three patients stopped their medication completely, 125 patients received medication on a regular basis. Fifty-two patient described the drugs with names, 13 patients described with their colors, 3 patients described by grammes, 45 patients described with the size of the tablet and 13 patients could not describe the drugs. Ninety-two patients explained which kind of drugs were used for each diseases, 17 patient explained partly, and 35 patients had no idea. Hundred patients received medication by themselves, 44 patients medications were giving by their relatives and med carers. Of medications, 140 were written by doctors directly, three medication were given by pharmacist; and one patient bought the drug by himself. For 11 patients the drugs were not harmonious to their diseases. Fifty-one patients admitted to the ED two times within last week, and 73 admitted two times within last month. Conclusion: The majority of patients with chronic diseases and use chronic drugs know their diseases and use the drugs in order, but do not have enough information about their medication.

Keywords: chronic disease, drug use, emergency department, medication

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Authors: Ibrahim M. Labouta, Marwa H. El-Wakil, Hayam M. Ashour, Ahmed M. Hassan, Manal N. Saudi

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The receptor tyrosine kinase c-Met is an attractive target for therapeutic treatment of cancers nowadays. Among the wide variety of heterocycles that have been explored for developing c-Met kinase inhibitors, the 1,2,4-triazines have been rarely investigated, although they are well known in the literature to possess antitumor activities. Herein we describe the design and synthesis of a novel series of 1,2,4-triazine derivatives possessing N-acylarylhydrazone moiety and another series combining the 1,2,4-triazine scaffold to the well-known anticancer drug 6-MP in order to explore their “double-drug” effect. The synthesized compounds were evaluated for their in vitro antitumor activity against three c-Met addicted cancer cell lines (A549, HT-29 and MKN-45). Most compounds showed moderate to excellent antiproliferative activity and four compounds showed potent inhibitory activity more than the reference drug Foretinib against one or more cancer cell lines. The obtained results revealed that the potent compounds are highly selective to A549 (lung adenocarcinoma) cancer cell line. The c-Met kinase inhibitory activity of the potent derivatives is still under investigation. The present study clearly demonstrates that the 1,2,4-triazine core ring exhibits promising antitumor activity with potential c-Met kinase inhibitory activity.

Keywords: 1, 2, 4-triazine, antitumor, c-Met inhibitor, double-drug

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Authors: Moustafa Ali Elwan, Ibrahim Salem Abdelrafa, Ashraf Moharm

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed oral and topical drugs worldwide. Moreover, NSAIDs are responsible for most of all adverse drug reactions. For several decades, there are numerous attempts to use the cutaneous layers as a gate into the body for the local delivery of the therapeutic agent. Transdermal drug delivery is a validated technology contributing significantly to global pharmaceutical care. Transdermal Drug Delivery systems can be improved by using therapeutic agents. Moreover, Transdermal Drug Delivery systems can be improved by using chemical enhancers like ultrasound or iontophoresis. Iontophoresis provides a mechanism to enhance the penetration of hydrophilic and charged molecules across the skin. Objective: to compare the drug administration by ‘iontophoresis’ versus the oral rule. Methods: This study was conducted at the Faculty of Physical Therapy, Modern University for technology and information, Cairo, Egypt, on 20 participants (8 female & 12 male) who complained of tennis elbow. Their mean age was (25.45 ± 3.98) years, and all participants were assessed in many aspects: Pain threshold was assessed by algometer. Range of motion was assessed by electro goniometer, and isometric strength was assessed by a portable hand-held dynamometer. Then Participants were randomly assigned into two groups: group A was treated with oral NSAID (diclofenac) while group B was treated via administration of NSAIDs (diclofenac) via an iontophoresis device. All the participants were subjected to blood samples analysis in both pre-administration of the drug and post-administration of the drug for 24 hours (sample/every 6 hours). Results: The results demonstrated that there was a significant improvement in group b, “iontophoresis NSAIDs group,” more than in group B,” oral NSAIDs group,” in all measurements ‘ pain threshold, strength, and range of motion. Also, the iontophoresis method shows higher maximum plasma concentrations (Cmax) and concentration-time curves than the oral method.

Keywords: diclofenac, iontophoresis, NSAIDs, oral, tennis elbow

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Authors: Siphesihle Hlongwane

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Background: Globally, alcohol consumption, smoking, and the use of illicit drugs kill more than 11.8 million people each year. In sub-Saharan Africa, substance abuse is responsible for more than 6.4% of all deaths recorded and about 4.7% of all Disability Adjusted Life Years (DALYs), with numbers still expected to grow if no drastic measures are taken to curb and address drug use. In a setting where substance use is rife, understanding contextual factors that influence an individual’s perceived eligibility to seek rehabilitation is paramount. Using the candidacy framework, we unpack how situational factors influence an individual’s perceived eligibility for healthcare uptake in adolescents and youth with substance use disorder (SUD). Methods: The candidacy framework is concerned with how people consider their eligibility for accessing a health service. The study collected and analyzed primary qualitative data to answer the research question. Data were collected between January and July 2022 on participants aged between 18 and 35 for drug users and 18 to 60 for family members. Participants include 20 previous and current drug users and 20 family members that experience the effects of addiction. A pre-drafted semi-structured interview guide was administered to a conveniently sampled population supplemented with a referral sampling method. Data were thematically analyzed using the NVivo 12pro software to manage the data. Findings: Our findings show that people with substance use disorders are aware of their drug use habits and acknowledge their candidacy for health services. Candidacy for health services is also acknowledged by those around them, such as family members and peers, and as such, information on the navigation of health services for drug users is shared by those who have attended health services, those affected by drug use, and this includes health service research by family members to identify accessible health services. While participants reported willingness to quit drug use if assistance is provided, the permeability of health care services is hindered by both individual determinations to quit drug use from long-time use and the availability of health services for drug users, such as rehabilitation centers. Our findings also show that drug users are conscious and can articulate their ailments; however, the hunt for the next dose of drugs and long waiting cues for health service acquisition overshadows their claim to health services. Participants reported a mixture of treatments prescribed, with some more gruesome than others prescribed, thus serving as both a facilitator and barrier for health service uptake. Despite some unorthodox forms of treatments prescribed in health care, the majority of those who enter treatment complete the process of treatment, although some are met with setbacks and sometimes relapse after treatment has finished. Conclusion: Drug users are able to ascertain their candidacy for health services; however, individual and environmental characteristics relating to drug use hinder the use of health services. Drug use interventions need to entice health service uptake as a way to improve candidacy for health use.

Keywords: substance use disorder, rehabilitation, drug use, relapse, South Africa, candidacy framework

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Authors: Wanwimon Mekwimon

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Drug addiction is a serious problem in Thailand which has occurred continuously and repeatedly and enormously impacting health and economy of drug users. The indigenous wisdom and folk medicine is an attractive alternative choice, especially in detoxification and rehabilitation period. There are two objectives: First is to study about rehabilitation process and the curing for drug eaters and 2nd is to investigate the effectiveness of the curing and rehabilitation process by indigenous wisdom at Tamkrabok monastery, Pra-Puttabat district, Saraburi province. The main informants are 10 curers, 15 patients and 17 after-1-year rehabilitators. In the process, the semi-structured questionnaire is administered, the data are analyzed and proved by triangulation. The curing and rehabilitation process which use herbal remedies has a period of 15 days (5 days for detoxification and 10 days for recovery period) and the occupational training and self-consciousness awakening were delivered. The follow-up process includes twice-a-month recall for 6 months, follow-up letters and in depth interview with their families. The outcome of 1 year post-treatment was 94% (16 from 17). There are many reasons for not relapsing: the recovering patients have drawn on their inner strength, self-awareness and coping skill as well as their family and social support while rehabilitation process which includes difficulties in contacting with family members. They can void themselves from high risk situations to relapse. Recommendations: The follow-up system should be improved for continuous quality improvement, there should be the qualification standard for herbal remedies and the comparison among rehabilitation process of Tamkrabok and another methods are to be guideline for the further development.

Keywords: rehabilitation, drug addiction, Thai indigenous knowledge, herbal remedies

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Authors: Lili Yang, Jirui Gong, Qinpu Luo, Min Liu, Bo Yang, Zihe Zhang

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Anthropogenic activities have increased nitrogen (N) inputs to grassland ecosystems. Knowledge of the impact of N addition on litter decomposition is critical to understand ecosystem carbon cycling and their responses to global climate change. The aim of this study was to investigate the effects of N addition and litter types on litter decomposition of a semi-arid temperate grassland during growing and non-growing seasons in Inner Mongolia, northern China, and to identify the relation between litter decomposition and C: N: P stoichiometry in the litter-soil continuum. Six levels of N addition were conducted: CK, N1 (0 g Nm−2 yr−1), N2 (2 g Nm−2 yr−1), N3 (5 g Nm−2 yr−1), N4 (10 g Nm−2 yr−1) and N5 (25 g Nm−2 yr−1). Litter decomposition rates and nutrient release differed greatly among N addition gradients and litter types. N addition promoted litter decomposition of S. grandis, but exhibited no significant influence on L. chinensis litter, indicating that the S. grandis litter decomposition was more sensitive to N addition than L. chinensis. The critical threshold for N addition to promote mixed litter decomposition was 10 -25g Nm−2 yr−1. N addition altered the balance of C: N: P stoichiometry between litter, soil and microbial biomass. During decomposition progress, the L. chinensis litter N: P was higher in N2-N4 plots compared to CK, while the S. grandis litter C: N was lower in N3 and N4 plots, indicating that litter N or P content doesn’t satisfy microbial decomposers with the increasing of N addition. As a result, S. grandis litter exhibited net N immobilization, while L. chinensis litter net P immobilization. Mixed litter C: N: P stoichiometry satisfied the demand of microbial decomposers, showed net mineralization during the decomposition process. With the increasing N deposition in the future, mixed litter would potentially promote C and nutrient cycling in grassland ecosystem by increasing litter decomposition and nutrient release.

Keywords: C: N: P stoichiometry, litter decomposition, nitrogen addition, nutrient release

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Authors: Tanvir Ahmed, Thanh N. Long, Phan T. Huong, Donald E. Stewart

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This paper presents views on condom use and the contexts of safe and unsafe sexual practices with different sexual partners and their relationships among Injecting Drug Users (IDUs) in Hai Phong, Vietnam. Fifteen IDUs participated and two local interviewers conducted qualitative semi-structured face-to-face interviews in September-October, 2012 in Vietnamese language. Data were analyzed thematically. Non-protective condom attitudes include negotiate or convince Female Sex Workers (FSW); not realizing risk, importance or necessity; partner doesn’t like, and having extra money/drug from clients. On the other hand, self-awareness, family-consciousness, suspicion of STI presence, fear of getting HIV, and client negotiation sometimes resulted in a safe-sex practice. A thematic diagram was developed to present the relationship (strong/weak) between condom attitude and sexual practice (safe/unsafe) by partner types. The experiences and views reflected in the qualitative information emphasize the heightened need for safe-sex education especially among young IDUs (male/female) highlighting sexual transmission risk.

Keywords: AIDS, HIV, injecting drug user, risk behaviors, Vietnam

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Authors: Peramachi Sathiyamoorthy, Jacop Gopas, Avi Golan Goldhirsh

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Corchorus olitorius is a leafy vegetable and an industrial crop. The herb has antioxidant, anti inflammatory, and anti-cancer properties. To assay the pharmaceutical properties, aqueous extracts of leaves and seeds from C. olitorius were tested against drug resistant melanoma cell line. The test showed LC50 of the extract was 0.08µg/ml. Aqueous seed extract exhibited higher melanoma inhibiting activity than leaf extract. Dialysis of seed extract showed that the active compound is less than 12 KDa. The compound with <3 KDa MW separated by microconcentration of seed extract showed 70.5 % inhibition of melanoma cell growth. Among the two fractions obtained by Gel filtration with G10 column, the first fraction at 1:2000 dilutions exhibited 100% inhibition of melanoma growth. The compound with Rf value 0.86 (MA4) isolated by TLC separation showed about 98% cytotoxicity against melanoma at 1: 1000 dilutions. Furthermore, HPLC separation of MA4 compound with Superdex 75 column resulted in 4 compounds. Out of 4, one compound showed melanoma inhibition. The active compound is identified by reagent methods as Strophanthidin. Further toxicological and clinical studies will lead to the development of a potential drug to treat drug resistant melanoma.

Keywords: corchorus olitorius, melanoma, drug development, strophanthidin

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Authors: Asiya Mahtab, Sushama Talegaonkar

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The research is aimed at developing targeted lipid-based nanocarrier systems of chondroitin sulfate (CS) to deliver an antirheumatic drug to the inflammatory site in arthritic paw. Lipid-based nanoparticle (TEF-lipo) was prepared by using a thin-film hydration method. The coating of prepared drug-loaded nanoparticles was done by the ionic interaction mechanism. TEF-lipo and CS-coated lipid nanoparticle (CS-lipo) were characterized for mean droplet size, zeta potential, and surface morphology. TEF-lipo and CS-lipo were further subjected to in vitro cell line studies on RAW 264.7 murine macrophage, U937, and MG 63 cell lines. The pharmacodynamic study was performed to establish the effectiveness of the prepared lipid-based conventional and targeted nanoparticles in comparison to pure drugs. Droplet size and zeta potential of TEF-lipo were found to be 128. 92 ± 5.42 nm and +12.6 ± 1.2 mV. It was observed that after the coating of TEF-lipo with CS, particle size increased to 155.6± 2.12 nm and zeta potential changed to -10.2± 1.4mV. Transmission electron microscopic analysis revealed that the nanovesicles were uniformly dispersed and detached from each other. Formulations followed sustained release pattern up to 24 h. Results of cell line studies ind icated that CS-lipo formulation showed the highest cytotoxic potential, thereby proving its enhanced ability to kill the RAW 264.7 murine macrophage and U937 cells when compared with other formulations. It is clear from our in vivo pharmacodynamic results that targeted nanocarriers had a higher inhibitory effect on arthritis progression than nontargeted nanocarriers or free drugs. Results demonstrate that this approach will provide effective treatment for rheumatoid arthritis, and CS served as a potential prophylactic against the advancement of cartilage degeneration.

Keywords: adjuvant induced arthritis, chondroitin sulfate, rheumatoid arthritis, teriflunomide

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Authors: Chabungbam Niranjit Khuman, Makarand Madhao Ghangrekar, Arunabha Mitra

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The cost of aeration is one of the limiting factors in the upscaling of microbial fuel cells (MFC) for field-scale applications. Wetland macrophytes have the ability to release oxygen into the water to maintain aerobic conditions in their root zone. In this experiment, the efficacy of rhizospheric oxygen release of wetland macrophytes as a source of oxygen in the cathodic chamber of MFC was conducted. The experiment was conducted in an MFC consisting of a three-liter anodic chamber made of ceramic cylinder and a 27 L cathodic chamber. Untreated carbon felts were used as electrodes (i.e., anode and cathode) and connected to an external load of 100 Ω using stainless steel wire. Wetland macrophytes (Canna indica) were grown in the cathodic chamber of the MFC in a hydroponic fashion using a styrofoam sheet (termed as macrophytes assisted-microbial fuel cell, M-MFC). The catholyte (i.e., water) in the M-MFC had negligible contact with atmospheric air due to the styrofoam sheet used for maintaining the hydroponic condition. There was no mixing of the catholyte in the M-MFC. Sucrose based synthetic wastewater having chemical oxygen demand (COD) of 3000 mg/L was fed into the anodic chamber of the MFC in fed-batch mode with a liquid retention time of four days. The C. indica thrived well throughout the duration of the experiment without much care. The average dissolved oxygen (DO) concentration and pH value in the M-MFC were 3.25 mg/L and 7.07, respectively, in the catholyte. Since the catholyte was not in contact with air, the DO in the catholyte might be considered as solely liberated from the rhizospheric oxygen release of C. indica. The maximum COD removal efficiency of M-MFC observed during the experiment was 76.9%. The inadequacy of terminal electron acceptor in the cathodic chamber in M-MFC might have hampered the electron transfer, which in turn, led to slower specific microbial activity, thereby resulting in lower COD removal efficiency than the traditional MFC with aerated catholyte. The average operating voltage (OV) and open-circuit voltage (OCV) of 294 mV and 594 mV, respectively, were observed in M-MFC. The maximum power density observed during polarization was 381 mW/m³, and the maximum sustainable power density observed during the experiment was 397 mW/m³ in M-MFC. The maximum normalized energy recovery and coulombic efficiency of 38.09 Wh/m³ and 1.27%, respectively, were observed. Therefore, it was evidenced that rhizospheric oxygen release of wetland macrophytes (C. indica) was capable of sustaining the cathodic reaction in MFC for field-scale applications.

Keywords: hydroponic, microbial fuel cell, rhizospheric oxygen release, wetland macrophytes

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Authors: Mohit Wadhawan, Sushma Rathaur

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Lymphatic filariasis, also called elephantiasis is a tropical disease afflicting over 120 million people in 81 countries worldwide. Existing anti filarial drugs are effective against the larval stages of filarial parasites which call for an urgent need of drugs which are macrofilaricidal. Identification of molecular targets crucial for survival of filarial parasites is a prerequisite for drug designing. Prolyl oligopeptidase (POP) is one such crucial enzyme involved in the maturation and degradation of neuropeptides and peptide hormones. We have identified this peptidase in the bovine filarial parasite, Setaria cervi. Effect of inhibition of POP on the proteome profile of filarial parasite has been discussed in this study. Filarial parasites were exposed to Z-pro-prolinal (ZPP), a specific POP inhibitor for 8 h and the motility and viability of the parasites was observed. It significantly reduced the motility and viability of the parasites. To study the proteome profile, the cytosolic, endoplasmic reticulum (ER) and mitochondrial extracts of the adult female parasites were subjected to 2-dimensional electrophoresis. As analyzed by the PD-Quest software, the ZPP caused the alteration in the different subcellular proteins, and the significantly altered proteins were identified using MALDI-MS/MS spectrometry. The major proteins identified were found to play important role in diverse biological functions like signaling, redox regulation, energy metabolism, stress response, and cytoskeleton formation. Moreover, we found upregulation in the calcium binding proteins such as calreticulin, calponin, and calpain-6 suggesting that POP inhibition regulates calcium release. This relates to earlier reports that POP plays non-catalytic role in inositol 1,4,5-trisphosphate (IP3) signaling inducing release of calcium from ER. Taken together, the data demonstrated that inhibition of prolyl oligopeptidase alter the overall proteome signifying its role in survival of the filarial parasites. Thus this study provides a basis for the use of POP as a chemotherapeutic target for the treatment of lymphatic filariasis.

Keywords: lymphatic filariasis, setaria cervi, prolyl oligopeptidase, proteomics

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Authors: Shishen Xie, Yingda L. Xie

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Tuberculosis (TB) is a potentially serious infectious disease that remains a health concern. The Interferon Gamma Release Assay (IGRA) is a blood test to find out if an individual is tuberculous positive or negative. This study applies statistical analysis to the clinical data of interferon-gamma levels of seventy-three subjects who diagnosed pulmonary TB in an anti-tuberculous treatment. Data analysis is performed to determine if there is a significant decline in interferon-gamma levels for the subjects during a period of six months, and to infer if the anti-tuberculous treatment is effective.

Keywords: data analysis, interferon gamma release assay, statistical methods, tuberculosis infection

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Authors: Wajid Rehman, Sirajul Haq, Bakhtiar Muhammad, Syed Fahad Hassan, Amin Badshah, Muhammad Waseem, Fazal Rahim, Obaid-Ur-Rahman Abid, Farzana Latif Ansari, Umer Rashid

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Five novel triorganotin (IV) compounds have been synthesized and characterized. The tin atom is penta-coordinated to assume trigonal-bipyramidal geometry. Using in silico derived parameters; the objective of our study is to design and synthesize promiscuous antibacterials potent enough to combat resistance. Among various synthesized organotin (IV) complexes, compound 5 was found as potent antibacterial agent against various bacterial strains. Further lead optimization of drug-like properties was evaluated through in silico predictions. Data mining and computational analysis were utilized to derive compound promiscuity phenomenon to avoid drug attrition rate in designing antibacterials. Xanthine oxidase and human glucose- 6-phosphatase were found as only true positive off-target hits by ChEMBL database and others utilizing similarity ensemble approach. Propensity towards a-3 receptor, human macrophage migration factor and thiazolidinedione were found as false positive off targets with E-value 1/4> 10^-4 for compound 1, 3, and 4. Further, displaying positive drug-drug interaction of compound 1 as uricosuric was validated by all databases and docked protein targets with sequence similarity and compositional matrix alignment via BLAST software. Promiscuity of the compound 5 was further confirmed by in silico binding to different antibacterial targets.

Keywords: antibacterial activity, drug promiscuity, ADMET prediction, metallo-pharmaceutical, antimicrobial resistance

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Authors: H. Achache, Y. Madani, A. Benzerdjeb

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The present study is based on the three-dimensional digital analysis by the finite elements method of the mechanical loading effect on the delamination of unidirectional and multidirectional stratified composites. The aim of this work is the determination of the release energy rate G in mode I and the Von Mises equivalent constraint distribution along the damaged area under the influence of several parameters such as the applied load and the delamination size. The results obtained in this study show that the unidirectional composite laminates have better mechanical resistance one the loading line than the multidirectional composite laminates.

Keywords: delamination, release energy rate, stratified composite, finite element method, ply

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Authors: Lacramioara Ochiuz, Manuela Hortolomei, Aurelia Vasile, Iulian Stoleriu, Marcel Popa, Cristian Peptu

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Local antibiotherapy is one of the most effective acne therapies. Erythromycin (ER) is a macrolide antibiotic topically administered for over 30 years in the form of gel, ointment or hydroalcoholic solution for the acne therapy. The use of ER as a base for topical dosage forms raises some technological challenges due to the physicochemical properties of this substance. The main disadvantage of ER is the poor water solubility (2 mg/mL) that limits both formulation using hydrophilic bases and skin permeability. Cyclodextrins (CDs) are biocompatible cyclic oligomers of glucose, with hydrophobic core and hydrophilic exterior. CDs are used to improve the bioavailability of drugs by increasing their solubility and/or their rate of dissolution after including the poorly water soluble substances (such as ER) in the hydrophobic cavity of CDs. Adding CDs leads to the increase of solubility and improved stability of the drug substance, increased permeability of substances of low water solubility, decreased toxicity and even to active dose reduction as a result of increased bioavailability. CDs increase skin tolerability by reducing the irritant effect of certain substances. We have included ER to lactide modified β-cyclodextrin, in order to improve the therapeutic effect of topically administered ER. The aims of the present study were to synthesise and describe a new complex with prolonged release of ER with lactide modified β-cyclodextrin (CD-LA_E), to investigate the CD-LA_E complex by scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR), to analyse the effect of semisolid base on the in vitro and ex vivo release characteristics of ER in the CD-LA_E complex by assessing the permeability coefficient and the release kinetics by fitting on mathematical models. SEM showed that, by complexation, ER changes its crystal structure and enters the amorphous phase. FTIR analysis has shown that certain specific bands of some groups in the ER structure move during the incapsulation process. The structure of the CD-LA_E complex has a molar ratio of 2.12 to 1 between lactide modified β-cyclodextrin and ER. The three semisolid bases (2% Carbopol, 13% Lutrol 127 and organogel based on Lutrol and isopropyl myristate) show a good capacity for incorporating the CD-LA_E complex, having a content of active ingredient ranging from 98.3% to 101.5% as compared to the declared value of 2% ER. The results of the in vitro dissolution test showed that the ER solubility was significantly increased by CDs incapsulation. The amount of ER released from the CD-LA_E gels was in the range of 76.23% to 89.01%, whereas gels based on ER released a maximum percentage of 26.01% ER. The ex vivo dissolution test confirms the increased ER solubility achieved by complexation, and supports the assumption that the use of this process might increase ER permeability. The highest permeability coefficient was obtained in ER released from gel based on 2% Carbopol: in vitro 33.33 μg/cm2/h, and ex vivo 26.82 μg/cm2/h, respectively. The release kinetics of complexed ER is performed by Fickian diffusion, according to the results obtained by fitting the data in the Korsmeyer-Peppas model.

Keywords: erythromycin, acne, lactide, cyclodextrin

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Authors: Yu-Hong Lin

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Background: An adverse drug reaction (ADR) reported is an injury which caused by taking medicines. Sometimes the severity of ADR reported may be minor, but sometimes it could be a life-threatening situation. In order to provide healthcare professionals as a better reference in clinical practice, we do data collection and analysis from our hospital. Methods: This was a retrospective study of ADRs reported performed from 2014 to 2015 in our hospital in Taiwan. We collected assessment items of ADRs reported, which contain gender and age, occurring sources, Anatomical Therapeutic Chemical (ATC) classification of suspected drugs, types of adverse reactions, Naranjo score calculating by Naranjo Adverse Drug Reaction Probability Scale and so on. Results: The investigation included two hundred and seven ADRs reported. Most of ADRs reported were occurring in outpatient department (92%). The average age of ADRs reported was 65.3 years. Less than 65 years of age were in the majority in this study (54%). Majority of all ADRs reported were males (51%). According to ATC classification system, the major classification of suspected drugs was cardiovascular system (19%) and antiinfectives for systemic use (18%) respectively. Among the adverse reactions, Dermatologic Effects (35%) were the major type of ADRs. Also, the major Naranjo scores of all ADRs reported ranged from 1 to 4 points (91%), which represents a possible correlation between ADRs reported and suspected drugs. Conclusions: Definitely, ADRs reported is still an extremely important information for healthcare professionals. For that reason, we put all information of ADRs reported into our hospital's computer system, and it will improve the safety of medication use. By hospital's computer system, it can remind prescribers to think of information about patient's ADRs reported. No drugs are administered without risk. Therefore, all healthcare professionals should have a responsibility to their patients, who themselves are becoming more aware of problems associated with drug therapy.

Keywords: adverse drug reaction, Taiwan, healthcare professionals, safe use of medicines

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Authors: Agnieszka Markowska-Radomska, Ewa Dluska

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Maintaining a bioactive substances dense diet is important for the elderly, especially to prevent diseases and to support healthy ageing. Adequate bioactive substances intake can reduce the risk of developing chronic diseases (e.g. cardiovascular, osteoporosis, neurodegenerative syndromes, diseases of the oral cavity, gastrointestinal (GI) disorders, diabetes, and cancer). This can be achieved by introducing a comprehensive supplementation of components necessary for the proper functioning of the ageing body. The paper proposes the multiple emulsions of the W1/O/W2 (water-in-oil-in-water) type as carriers for effective co-encapsulation and co-delivery of bioactive substances in supplementation of the elderly. Multiple emulsions are complex structured systems ("drops in drops"). The functional structure of the W1/O/W2 emulsion enables (i) incorporation of one or more bioactive components (lipophilic and hydrophilic); (ii) enhancement of stability and bioavailability of encapsulated substances; (iii) prevention of interactions between substances, as well as with the external environment, delivery to a specific location; and (iv) release in a controlled manner. The multiple emulsions were prepared by a one-step method in the Couette-Taylor flow (CTF) contactor in a continuous manner. In general, a two-step emulsification process is used to obtain multiple emulsions. The paper contains a proposal of emulsion functionalization by introducing pH-responsive biopolymer—carboxymethylcellulose sodium salt (CMC-Na) to the external phase, which made it possible to achieve a release of components controlled by the pH of the gastrointestinal environment. The membrane phase of emulsions was soybean oil. The W1/O/W2 emulsions were evaluated for their characteristics (drops size/drop size distribution, volume packing fraction), encapsulation efficiency and stability during storage (to 30 days) at 4ºC and 25ºC. Also, the in vitro multi-substance co-release process were investigated in a simulated gastrointestinal environment (different pH and composition of release medium). Three groups of stable multiple emulsions were obtained: emulsions I with co-encapsulated vitamins B12, B6 and resveratrol; emulsions II with vitamin A and β-carotene; and emulsions III with vitamins C, E and D3. The substances were encapsulated in the appropriate emulsion phases depending on the solubility. For all emulsions, high encapsulation efficience (over 95%) and high volume packing fraction of internal droplets (0.54-0.76) were reached. In addition, due to the presence of a polymer (CMC-Na) with adhesive properties, high encapsulation stability during emulsions storage were achieved. The co-release study of encapsulated bioactive substances confirmed the possibility to modify the release profiles. It was found that the releasing process can be controlled through the composition, structure, physicochemical parameters of emulsions and pH of the release medium. The results showed that the obtained multiple emulsions might be used as potential liquid complex carriers for controlled/modified/site-specific co-delivery of bioactive substances in dietary supplementation in the elderly.

Keywords: bioactive substance co-release, co-encapsulation, elderly supplementation, multiple emulsion

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Authors: D. Velayadum, P. Sthandiwe , N. Maharaj, T. Munien, S. Ndamase, G. Zulu, S. Xulu, F. Oosthuizen

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Introduction and aims of the study: It is the responsibility of the pharmacist to manage drug-related problems in order to ensure the greatest benefit to the patient. In order to prevent drug-related morbidity, pharmacists should be aware of medicines that may contribute to certain drug-related problems due to their pharmacological action. In an attempt to assist healthcare practitioners to prevent drug-related morbidity (PDRM), indicators for prevention have been designed. There are currently no indicators available for primary health care in developing countries like South Africa, where the majority of the population access primary health care. There is, therefore, a need to develop such indicators, specifically with the aim of assisting healthcare practitioners in primary health care. Methods: A literature study was conducted to compile a comprehensive list of PDRM indicators as developed internationally using the search engines Google Scholar and PubMed. MESH term used to retrieve suitable articles was 'preventable drug-related morbidity indicators'. The comprehensive list of PDRM indicators obtained from the literature study was further evaluated for face validity. Face validity was done in duplicate by 2 sets of independent researchers to ensure 1) no duplication of indicators when compiling a single list, 2) inclusion of only medication available in primary healthcare, and 3) inclusion of medication currently available in South Africa. Results: The list of indicators, compiled from PDRM indicators in the USA, UK, Portugal, Australia, India, and Canada contained 324 PDRM. 184 of these indicators were found to be duplicates, and the duplications were omitted, leaving a final list of 140. The 140 PDRM indicators were evaluated for face-validity, and 97 were accepted as relevant to primary health care in South Africa. 43 indicators did not comply with the criteria and were omitted from the final list. Conclusion: This study is a first step in compiling a list of PDRM indicators for South Africa. It is important to take cognizance to the fact the health systems differ vastly internationally, and it is, therefore, important to develop country-specific indicators.

Keywords: drug-related morbidity, primary healthcare, South Africa, developing countries

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Authors: Antonio Montes, Antonio Cozar, Clara Pereyra, Diego Valor, Enrique Martinez de la Ossa

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Tissues and organs can be damaged because of traumatism, congenital illnesses, or cancer and the traditional therapeutic alternatives, such as surgery, cannot usually completely repair the damaged tissues. Tissue engineering allows regeneration of the patient's tissues, reducing the problems caused by the traditional methods. Scaffolds, polymeric structures with interconnected porosity, can be promoted the proliferation and adhesion of the patient’s cells in the damaged area. Furthermore, by means of impregnation of the scaffold with beneficial active substances, tissue regeneration can be induced through a drug delivery process. The objective of the work is the fabrication of a PVA scaffold coated with Gallic Acid and polypyrrole through a one-step foaming and impregnation process using the SSI technique (Supercritical Solvent Impregnation). In this technique, supercritical CO₂ penetrates into the polymer chains producing the plasticization of the polymer. In the depressurization step a CO₂ cellular nucleation and growing to take place to an interconnected porous structure of the polymer. The foaming process using supercritical CO₂ as solvent and expansion agent presents advantages compared to the traditional scaffolds’ fabrication methods, such as the polymer’s high solubility in the solvent or the possibility of carrying out the process at a low temperature, avoiding the inactivation of the active substance. In this sense, the supercritical CO₂ avoids the use of organic solvents and reduces the solvent residues in the final product. Moreover, this process does not require long processing time that could cause the stratification of substance inside the scaffold reducing the therapeutic efficiency of the formulation. An experimental design has been carried out to optimize the SSI technique operating conditions, as well as a study of the morphological characteristics of the scaffold for its use in tissue engineerings, such as porosity, conductivity or the release profiles of the active substance. It has been proved that the obtained scaffolds are partially porous, conductors of electricity and are able to release Gallic Acid in the long term.

Keywords: scaffold, foaming, supercritical, PVA, polypyrrole, gallic acid

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Authors: Sarah K. Amer, Walaa Alaa

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Epilepsy is an important cause of mortality and morbidity, according to WHO statistics. It is characterized by the presence of frequent seizures occurring more than 24 hours apart. Carbamazepine (CBZ) is considered first-line treatment for epilepsy. However, reports have shown that CBZ oral formulations failed to achieve optimum systemic delivery, minimize side effects, and enhance patient compliance. Besides, the literature has signified the lack of therapeutically efficient CBZ transdermal formulation and the urge for its existence owing to its ease and convenient method of application and highlighted capability to attain higher bioavailability and more extended-release profiles compared to conventional oral CBZ tablets. This work aims to prepare CBZ microspheres (MS) that are embedded in a transdermal gel containing Vitamin B to be co-delivered. MS were prepared by emulsion-solvent diffusion method using Eudragit S as core forming polymer and hydroxypropyl methylcellulose (HPMC) polymer. The MS appeared to be spherical and porous in nature, offering a large surface area and high entrapment efficiency of CBZ. The transdermal gel was prepared by solvent-evaporation technique using HPMC that, offered high entrapment efficiency and Eudragit S that provided an extended-release profile. Polyethylene glycol, Span 80 and Pyridoxine were also added. Data indicated that combinations of CBZ with pyridoxine can reduce epileptic seizures without affecting motor coordination. Extended-release profiles were evident for this system. The patches were furthermore tested for thickness, moisture content, folding endurance, spreadability and viscosity measurements. This novel pharmaceutical formulation would be of great influence on seizure control, offering better therapeutic effects.

Keywords: epilepsy, carbamazepine, pyridoxine, transdermal

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Authors: Firman Riyudha, Endrik Mifta Shaiful

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The spread of drug users is one kind of behavioral epidemiology that becomes a threat to every country in the world. This problem caused various crisis simultaneously, including financial or economic crisis, social, health, until human crisis. Most drug users are teenagers at school age. A new deterministic model would be constructed to determine the dynamics of the spread of drug users by considering level of education in a susceptible population. Based on the analytical model, two equilibria points were obtained; there were E₀ (zero user) and E₁ (endemic equilibrium). Existence of equilibrium and local stability of equilibria depended on the Basic Reproduction Ratio (R₀). This parameter was defined as the expected rate of secondary prevalence and primary prevalence in virgin population along spreading primary prevalence. The zero-victim equilibrium would be locally asymptotically stable if R₀ < 1 while if R₀ > 1 the endemic equilibrium would be locally asymptotically stable. The result showed that R₀ was proportional to the rate of interaction of each susceptible population based on educational level with the users' population. It is concluded that there was a need to be given a control in interaction, so that drug users population could be minimized. Numerical simulations were also provided to support analytical results.

Keywords: drugs users, level education, mathematical model, stability

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Authors: Prakash Singh

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Many schools throughout the world are facing constant pressure to cope with the violence and drug abuse of learners who show little or no respect for acceptable and desirable social norms. These delinquent learners tend to harbour feelings of being beyond reproach because they strongly believe that it is well within their rights to engage in violent and destructive behaviour. Knives, guns, and other weapons appear to be more readily used by them on the school premises than before. It is known that learners smoke, drink alcohol, and use drugs during school hours, hence, their ability to concentrate, work, and learn, is affected. They become violent and display disruptive behaviour in their classrooms as well as on the school premises, and this atrocious behaviour makes it possible for drug dealers and gangsters to gain access onto the school premises. The primary purpose of this exploratory quantitative study was therefore to establish how tobephobia (TBP), caused by school violence and drug abuse, affects teaching and learning in schools. The findings of this study affirmed that poor discipline resulted in producing poor quality education. Most of the teachers in this study agreed that educating learners who consumed alcohol and other drugs on the school premises resulted in them suffering from TBP. These learners are frequently abusive and disrespectful, and resort to violence to seek attention. As a result, teachers feel extremely demotivated and suffer from high levels of anxiety and stress. The word TBP will surely be regarded as a blessing by many teachers throughout the world because finally, there is a word that will make people sit up and listen to their problems that cause real fear and anxiety in schools.

Keywords: aims and objectives of quality education, debilitating effects of tobephobia, fear of failure associated with education, learners' violent behaviour and drug abuse

Procedia PDF Downloads 276

Authors: Lin Tang, Xiaoxia Guo, Lingling Zhang

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Recent vaccine scandals overshadowed China’s accomplishment of public health, triggering discussions on the causes of vaccine incidents. Through legal interpretation of selected vaccine incidents and analysis of systemic vulnerabilities in vaccine circulation and lot release, a panoramic review of legislative progresses in the vaccine administration sheds the light on this debate. In essence, it is the combination of the lagging legal system and the absence of information technology infrastructure in the process of vaccine administration reform that has led to the recurrence of vaccine incidents. These findings have significant implications for further improvement of vaccine administration and China’s participation in global healthcare.

Keywords: legislation, lot release, public health, reform, vaccine administration, vaccine circulation

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Authors: Owonikoko Abayomi Dele

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Epilepsy is an unresolved disease that needs urgent attention. It is a brain disorder that affects over sixty-five (65) million people around the globe. Despite the availability of commercial anti-epileptic drugs, the war against this unmet condition is yet to be resolved. Most epilepsy patients are resistant to available anti-epileptic medications thus the need for affordable novel therapy against epilepsy is a necessity. Numerous phytochemicals have been reported for their potency, efficacy and safety as therapeutic agents against many diseases. This study investigated 99 isolated phytochemicals from Chasmanthera dependens and Carissa edulis against carbonic anhydrase (ii) drug target. The absorption, distribution, metabolism, excretion and toxicity (ADMET) of the isolated compounds were examined using admet SAR-2 web server while Swiss ADME was used to analyze the oral bioavailability, drug-likeness and lead-likeness properties of the selected leads. PASS web server was used to predict the biological activities of selected leads while other important physicochemical properties and interactions of the selected leads with the active site of the target after successful molecular docking simulation with the pyrx virtual screening tool were also examined. The results of these study identified seven lead compounds; C49- alpha-carissanol (-7.6 kcal/mol), C13- Catechin (-7.4 kcal/mol), C45- Salicin (-7.4 kcal/mol), C6- Bisnorargemonine (-7.3 kcal/mol), C36- Pallidine (-7.1 kcal/mol), S4- Lacosamide (-7.1 kcal/mol), and S7- Acetazolamide (-6.4 kcal/mol) for CA II (3HS4 receptor). These leads compounds are probable inhibitors of this drug target due to the observed good binding affinities and favourable interactions with the active site of the drug target, excellent ADMET profiles, PASS Properties, drug-likeness, lead-likeness and oral bioavailability properties. The identified leads have better binding energies as compared to the binding energies of the two standards. Thus, seven identified lead compounds can be developed further towards the development of new anti-epileptic medications.

Keywords: drug-likeness, phytochemicals, carbonic anhydrases, metalloeazymes, active site, ADMET

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