Search results for: ex vivo bovine bone
1157 Treatment of Premalignant Lesions: Curcumin a Promising Non-Surgical Option
Authors: Heba A. Hazzah, Ragwa M. Farid, Maha M. A. Nasra, Mennatallah Zakria, Magda A. El Massik, Ossama Y. Abdallah
Abstract:
Introduction: Curcumin (Cur) is a polyphenol derived from the herbal remedy and dietary spice turmeric. It possesses diverse anti-inflammatory and anti-cancer properties following oral or topical administration. The buccal delivery of curcumin can be useful for both systemic and local disease treatments such as gingivitis, periodontal diseases, oral carcinomas, and precancerous oral lesions. Despite of its high activity, it suffers a limited application due to its low oral bioavailability, poor aqueous solubility, and instability. Aim: Preparation and characterization of curcumin solid lipid nanoparticles with a high loading capacity into a mucoadhesive gel for buccal application. Methodology: Curcumin was formulated as nanoparticles using different lipids, namely Gelucire 39/01, Gelucire 50/13, Precirol, Compritol, and Polaxomer 407 as a surfactant. The SLN were dispersed in a mucoadhesive gel matrix to be applied to the buccal mucosa. All formulations were evaluated for their content, entrapment efficiency, particle size, in vitro drug dialysis, ex vivo mucoadhesion test, and ex vivo permeation study using chicken buccal mucosa. Clinical evaluation was conducted on 15 cases suffering oral erythroplakia and erosive lichen planus. Results: The results showed high entrapment efficiency reaching almost 90 % using Gelucire 50, the loaded gel with Cur-SLN showed good adhesion property and 25 minutes in vivo residence time. In addition to stability enhancement for the Cur powder. All formulae did not show any drug permeated however, a significant amount of Cur was retained within the mucosal tissue. Pain and lesion sizes were significantly reduced upon topical treatment. Complete healing was observed after 6 weeks of treatment. Conclusion: These results open a room for the pharmaceutical technology to optimize the use of this golden magical powder to get the best out of it. In addition, the lack of local anti-inflammatory compounds with reduced side effects intensifies the importance of studying natural products for this purpose.Keywords: curcumin, erythroplakia, mucoadhesive, pain, solid lipid nanoparticles
Procedia PDF Downloads 4511156 Calcium Biochemical Indicators in a Group of Schoolchildren with Low Socioeconomic Status from Barranquilla, Colombia
Authors: Carmiña L. Vargas-Zapata, María A. Conde-Sarmiento, Maria Consuelo Maestre-Vargas
Abstract:
Calcium is an essential element for good growth and development of the organism, and its requirement is increased at school age. Low socio-economic populations of developing countries such as Colombia may have food deficiency of this mineral in schoolchildren that could be reflected in calcium biochemical indicators, bone alterations and anthropometric indicators. The objective of this investigation was to evaluate some calcium biochemical indicators in a group of schoolchildren of low socioeconomic level from Barranquilla city and to correlate with body mass index. 60 schoolchildren aged 7 to 15 years were selected from Jesus’s Heart Educational Institution in Barranquilla-Atlántico, apparently healthy, without suffering from infectious or gastrointestinal diseases, without habits of drinking alcohol or smoking another hallucinogenic substance and without taking supplementation with calcium in the last six months or another substance that compromises bone metabolism. The research was approved by the ethics committee at Universidad del Atlántico. The selected children were invited to donate a blood and urine sample in a fasting time of 12 hours, the serum was separated by centrifugation and frozen at ˗20 ℃ until analyzed and the same was done with the urine sample. On the day of the biological collections, the weight and height of the students were measured to determine the nutritional status by BMI using the WHO tables. Calcium concentrations in serum and urine (SCa, UCa), alkaline phosphatase activity total and of bone origin (SAPT, SBAP) and urinary creatinine (UCr) were determined by spectrophotometric methods using commercial kits. Osteocalcin and Cross-linked N-telopeptides of type I collagen (NTx-1) in serum were measured with an enzyme-linked inmunosorbent assay. For statistical analysis the Statgraphics software Centurium XVII was used. 63% (n = 38) and 37% (n = 22) of the participants were male and female, respectively. 78% (n = 47), 5% (n = 3) and 17% (n = 10) had a normal, malnutrition and high nutritional status, respectively. The averages of evaluated indicators levels were (mean ± SD): 9.50 ± 1.06 mg/dL for SCa; 181.3 ± 64.3 U/L for SAPT, 143.8 ± 73.9 U/L for SBAP; 9.0 ± 3.48 ng/mL for osteocalcin and 101.3 ± 12.8 ng/mL for NTx-1. UCa level was 12.8 ± 7.7 mg/dL that adjusted with creatinine ranged from 0.005 to 0.395 mg/mg. Considering serum calcium values, approximately 7% of school children were hypocalcemic, 16% hypercalcemic and 77% normocalcemic. The indicators evaluated did not correlate with the BMI. Low values were observed in calcium urinary excretion and high in NTx-1, suggesting that mechanisms such as increase in renal retention of calcium and in bone remodeling may be contributing to calcium homeostasis.Keywords: calcium, calcium biochemical, indicators, school children, low socioeconomic status
Procedia PDF Downloads 1121155 Spinal Hydatidosis: Therapeutic Management of 5 Cases
Authors: Ghoul Rachid Brahim, Trad Khodja Rafik
Abstract:
Vertebral localization of the hydatid cyst is a severe form of bone hydatidosis, is a parasitic infection caused by the larval forms of the tapeworms Echinococcus granulosus, The disease is slowly remaining silent (a long incubation period) which may explain why this pathology is often discovered at the stage of neurological complications. The objective of this study is to recall the clinical and radiological aspects of this condition and the importance of early diagnosis and appropriate management. We report a study of 5 patients with vertebral hydatidosis, four men and one woman, four (04) patients operated in the emergency setting for spinal cord compression (decompression by wide laminectomy with evacuation of intra and extra canal vesicles).Albendazole-based medical treatment is instituted in all patients. Results: The evolution was favorable for three patients, the other two patients reoperated for a local recurrence. Conclusion: Vertebral hydatidosis is a rare condition with a poor prognosis due to the risk of neurological damage, the infiltrating nature of bone lesions, the frequency of relapses and therapeutic difficulties. The only curative method remains surgery, which must aim for complete and large excision of the lesions as if it were a “malignant tumour”.Keywords: hydatidosis, Echinococcosis granulosus, hydatid cyst, spinal cord compression, laminectomy
Procedia PDF Downloads 971154 FracXpert: Ensemble Machine Learning Approach for Localization and Classification of Bone Fractures in Cricket Athletes
Authors: Madushani Rodrigo, Banuka Athuraliya
Abstract:
In today's world of medical diagnosis and prediction, machine learning stands out as a strong tool, transforming old ways of caring for health. This study analyzes the use of machine learning in the specialized domain of sports medicine, with a focus on the timely and accurate detection of bone fractures in cricket athletes. Failure to identify bone fractures in real time can result in malunion or non-union conditions. To ensure proper treatment and enhance the bone healing process, accurately identifying fracture locations and types is necessary. When interpreting X-ray images, it relies on the expertise and experience of medical professionals in the identification process. Sometimes, radiographic images are of low quality, leading to potential issues. Therefore, it is necessary to have a proper approach to accurately localize and classify fractures in real time. The research has revealed that the optimal approach needs to address the stated problem and employ appropriate radiographic image processing techniques and object detection algorithms. These algorithms should effectively localize and accurately classify all types of fractures with high precision and in a timely manner. In order to overcome the challenges of misidentifying fractures, a distinct model for fracture localization and classification has been implemented. The research also incorporates radiographic image enhancement and preprocessing techniques to overcome the limitations posed by low-quality images. A classification ensemble model has been implemented using ResNet18 and VGG16. In parallel, a fracture segmentation model has been implemented using the enhanced U-Net architecture. Combining the results of these two implemented models, the FracXpert system can accurately localize exact fracture locations along with fracture types from the available 12 different types of fracture patterns, which include avulsion, comminuted, compressed, dislocation, greenstick, hairline, impacted, intraarticular, longitudinal, oblique, pathological, and spiral. This system will generate a confidence score level indicating the degree of confidence in the predicted result. Using ResNet18 and VGG16 architectures, the implemented fracture segmentation model, based on the U-Net architecture, achieved a high accuracy level of 99.94%, demonstrating its precision in identifying fracture locations. Simultaneously, the classification ensemble model achieved an accuracy of 81.0%, showcasing its ability to categorize various fracture patterns, which is instrumental in the fracture treatment process. In conclusion, FracXpert has become a promising ML application in sports medicine, demonstrating its potential to revolutionize fracture detection processes. By leveraging the power of ML algorithms, this study contributes to the advancement of diagnostic capabilities in cricket athlete healthcare, ensuring timely and accurate identification of bone fractures for the best treatment outcomes.Keywords: multiclass classification, object detection, ResNet18, U-Net, VGG16
Procedia PDF Downloads 1201153 Development of a Paediatric Head Model for the Computational Analysis of Head Impact Interactions
Authors: G. A. Khalid, M. D. Jones, R. Prabhu, A. Mason-Jones, W. Whittington, H. Bakhtiarydavijani, P. S. Theobald
Abstract:
Head injury in childhood is a common cause of death or permanent disability from injury. However, despite its frequency and significance, there is little understanding of how a child’s head responds during injurious loading. Whilst Infant Post Mortem Human Subject (PMHS) experimentation is a logical approach to understand injury biomechanics, it is the authors’ opinion that a lack of subject availability is hindering potential progress. Computer modelling adds great value when considering adult populations; however, its potential remains largely untapped for infant surrogates. The complexities of child growth and development, which result in age dependent changes in anatomy, geometry and physical response characteristics, present new challenges for computational simulation. Further geometric challenges are presented by the intricate infant cranial bones, which are separated by sutures and fontanelles and demonstrate a visible fibre orientation. This study presents an FE model of a newborn infant’s head, developed from high-resolution computer tomography scans, informed by published tissue material properties. To mimic the fibre orientation of immature cranial bone, anisotropic properties were applied to the FE cranial bone model, with elastic moduli representing the bone response both parallel and perpendicular to the fibre orientation. Biofiedility of the computational model was confirmed by global validation against published PMHS data, by replicating experimental impact tests with a series of computational simulations, in terms of head kinematic responses. Numerical results confirm that the FE head model’s mechanical response is in favourable agreement with the PMHS drop test results.Keywords: finite element analysis, impact simulation, infant head trauma, material properties, post mortem human subjects
Procedia PDF Downloads 3261152 Positive Effects of Aerobic Exercise after Bone Marrow Stem Cell Transplantation on Recovery of Dopaminergic Neurons and Promotion of Angiogenesis Markers in the Striatum of Parkinsonian Rats
Authors: S. A. Hashemvarzi, A. Heidarianpour, Z. Fallahmohammadi, M. Pourghasem, M. Kaviani
Abstract:
Introduction: Parkinson’s disease (PD) is a progressive neurodegenerative in the central nervous system characterized by the loss of dopaminergic neurons in the substantia nigra resulting in loss of dopamine release in the striatum. Non-drug treatment options such as Stem cell transplantation and exercise have been considered for treatment of Parkinson's disease. Purpose: The purpose of this study was to evaluate the effect of aerobic exercise after bone marrow stem cells transplantation on recovery of dopaminergic neurons and promotion of angiogenesis markers in the striatum of parkinsonian rats. Materials and Methods: 42 male Wistar rats were divided randomly into six groups: Normal (N), Sham (S), Parkinson’s (P), Stem cells transplanted Parkinson’s (SP), Exercised Parkinson’s (EP) and Stem cells transplanted + Exercised Parkinson’s (SEP). To create a model of Parkinson's, the striatum was destroyed by injection of 6-hydroxy-dopamine into the striatum through stereotaxic apparatus. Stem cells were derived from the bone marrow of femur and tibia of male rats with 6-8 weeks old. After cultivation, approximately 5×105 cells in 5 microliter of medium were injected into the striatum of rats through the channel. Aerobic exercise was included 8 weeks of running on the treadmill with a speed of 15 meters per minute. At the end, all subjects were decapitated and striatum tissues were separately isolated for measurement of vascular endothelial growth factor (VEGF), dopamine (DA) and tyrosine hydroxylase (TH) levels. Results: VEGF, DA and TH levels in the striatum of parkinsonian rats significantly increased in treatment groups (SP, EP and SEP), especially in SEP group compared to P group after treatment (P<0.05). Conclusion: The findings implicate that the BMSCs transplantation in combination with exercise would have synergistic effects leading to functional recovery, dopaminergic neurons recovery and promotion of angiogenesis marker in the striatum of parkinsonian rats.Keywords: stem cells, treadmill training, neurotrophic factors, Parkinson
Procedia PDF Downloads 3421151 Determination of Skeletal Age in Nigerian Children: Applicability of the Greulich and Pyle Atlas
Authors: Udoaka A. I., Didia B. C.
Abstract:
Background: The maturation of a child’s bones as it grows to adulthood can be viewed radiologically. The skeletal age (bone age) is the average age at which a particular stage of bone maturation is achieved. The Greulich and Pyle standard is the commonest method used to assess the skeletal age using the hand and wrist radiograph throughout the world. This atlas was compiled solely from Caucasian children and made use of the orderly sequence of carpal ossification to determine the skeletal age. Several authors have faulted this atlas for not being suitable for other races. Aim: The aim of this study is to determine if the Greulich and Pyle Atlas is applicable to Nigerian children when compared to their chronological ages. Methods: The total number of 78 normal radiographs of the hand and wrist of Nigerian children obtained from several hospitals were used for this study . These radiographs were compared with the atlas and their skeletal ages noted form the atlas. The child’s chronological age in each case was also recorded. Results: The result shows a mean increase of two months in the skeletal ages of the Nigerian children compared to the atlas. This difference, however, was not significant. The skeletal age (in months) was greater in 77% of the children than the expected age in the atlas. Conclusion: The mean skeletal age of Nigerian children, though more than the standard in the atlas, is not statistically significant; as a result the study finds the radiographic atlas of Greulich and Pyle atlas applicable to Nigerian children.Keywords: Greulich and Pyle Atlas, radiograph, skeletal age
Procedia PDF Downloads 2561150 Immunosupressive Effect of Chloroquine through the Inhibition of Myeloperoxidase
Authors: J. B. Minari, O. B. Oloyede
Abstract:
Polymorphonuclear neutrophils (PMNs) play a crucial role in a variety of infections caused by bacteria, fungi, and parasites. Indeed, the involvement of PMNs in host defence against Plasmodium falciparum is well documented both in vitro and in vivo. Many of the antimalarial drugs such as chloroquine used in the treatment of human malaria significantly reduce the immune response of the host in vitro and in vivo. Myeloperoxidase is the most abundant enzyme found in the polymorphonuclear neutrophil which plays a crucial role in its function. This study was carried out to investigate the effect of chloroquine on the enzyme. In investigating the effects of the drug on myeloperoxidase, the influence of concentration, pH, partition ratio estimation and kinetics of inhibition were studied. This study showed that chloroquine is concentration-dependent inhibitor of myeloperoxidase with an IC50 of 0.03 mM. Partition ratio estimation showed that 40 enzymatic turnover cycles are required for complete inhibition of myeloperoxidase in the presence of chloroquine. The influence of pH on the effect of chloroquine on the enzyme showed significant inhibition of myeloperoxidase at physiological pH. The kinetic inhibition studies showed that chloroquine caused a non-competitive inhibition with an inhibition constant Ki of 0.27mM. The results obtained from this study shows that chloroquine is a potent inhibitor of myeloperoxidase and it is capable of inactivating the enzyme. It is therefore considered that the inhibition of myeloperoxidase in the presence of chloroquine as revealed in this study may partly explain the impairment of polymorphonuclear neutrophil and consequent immunosuppression of the host defence system against secondary infections.Keywords: myeloperoxidase, chloroquine, inhibition, neutrophil, immune
Procedia PDF Downloads 3741149 Nutrient Foramina of the Lunate Bone of the Hand – an Anatomical Study
Authors: P.J. Jiji, B.V. Murlimanju, Latha V. Prabhu, Mangala M. Pai
Abstract:
Background: The lunate bone dislocation can lead to the compression of the median nerve and subsequent carpal tunnel syndrome. The dislocation can interrupt the vasculature and would cause avascular necrosis. The objective of the present study was to study the morphology and number of the nutrient foramina in the cadaveric dried lunate bones of the Indian population. Methods: The present study included 28 lunate bones (13 right sided and 15 left sided) which were obtained from the gross anatomy laboratory of our institution. The bones were macroscopically observed for the nutrient foramina and the data was collected with respect to their number. The tabulation of the data and analysis were done. Results: All of our specimens (100%) exhibited the nutrient foramina over the non-articular surfaces. The foramina were observed only over the palmar and dorsal surfaces of the lunate bones. The foramen ranged between 2 and 10. The foramina were more in number over the dorsal surface (average number 3.3) in comparison to the palmar surface (average number 2.4). Conclusion: We believe that the present study has provided important data about the nutrient foramina of the lunate bones. The data is enlightening to the orthopedic surgeon and would help in the hand surgeries. The morphological knowledge of the vasculature, their foramina of entry and their number is required to understand the concepts in the lunatomalacia and Kienbock’s disease.Keywords: avascular necrosis, foramen, lunate, nutrient
Procedia PDF Downloads 2441148 Impact of 99mTc-MDP Bone SPECT/CT Imaging in Failed Back Surgery Syndrome
Authors: Ching-Yuan Chen, Lung-Kwang Pan
Abstract:
Objective: Back pain is a major health problem costing billions of health budgets annually in Taiwan. Thousands of back pain surgeries are performed annually with up to 40% of patients complaining of back pain at time of post-surgery causing failed back surgery syndrome (FBSS), although diagnosis in these patients may be complex. The aim of study is to assess the feasibility of using bone SPECT-CT imaging to localize the active lesions causing persistent, recurrent or new backache after spine surgery. Materials and Methods: Bone SPECT-CT imaging was performed after the intravenous injection of 20 mCi of 99mTc-MDP for all the patients with diagnosis of FBSS. Patients were evaluated using status of subjectively pain relief, functional improvement and degree of satisfaction by reviewing the medical records and questionnaires in a 2 more years’ follow-up. Results: We enrolled a total of 16 patients were surveyed in our hospital from Jan. 2015 to Dec. 2016. Four people on SPEC/CT imaging ensured significant lesions were undergone a revised surgery (surgical treatment group). The mean visual analogue scale (VAS) decreased 5.3 points and mean Oswestry disability index (ODI) improved 38 points in the surgical group. The remaining 12 on SPECT/CT imaging were diagnosed as no significant lesions then received drug treatment (medical treatment group). The mean VAS only decreased 2 .1 point and mean ODI improved 12.6 points in the medical treatment group. In the posttherapeutic evaluation, the pain of the surgical treatment group showed a satisfactory improvement. In the medical treatment group, 10 of the 12 were also satisfied with the symptom relief while the other 2 did not improve significantly. Conclusions: Findings on SPECT-CT imaging appears to be easily explained the patients' pain. We recommended that SPECT/CT imaging was a feasible and useful clinical tool to improve diagnostic confidence or specificity when evaluating patients with FBSS.Keywords: failed back surgery syndrome, oswestry disability index, SPECT-CT imaging, 99mTc-MDP, visual analogue scale
Procedia PDF Downloads 1731147 Dynamics of Antioxidant and Anti-Radical Activity of the Extracts of Certain Plants of Kazakhstan
Authors: A. Kazbekova, A. Kudaibergenov, G. Atazhanova, S. Adekenov
Abstract:
In recent years, it achieved some progress such a direction as to study the possibility of correlation between different types of biological activity. In particular, in our work, we consider questions such as: the impact of the qualitative composition of total substances in the example of plant extracts on antioxidant and antiradical activity, the presents of correlation between these types of activity, etc. It is known that there is a relationship between the values of optical density of working solutions of extracts and corresponding bioactivity in vitro, in particular, the antioxidant and hepatoprotective effects. In this study, we have identified that among some studied species of wormwood (Artemisia viridis Wild, Artemisia jacutica Drob, Artemisia annua L, Artemisia siversiana Wild, Artemisia adamsii Bess, Artemisia tianschanica, Artemisia obtusiloba Ledeb., Artemisia heptopotamica), as well as extracts of Inula caspica, Аjania tenuifolia, Abies sibirica, Galatella songorica, Mentha asiatica and Thymus mugodzharicus it was identified that the highest content of polyphenol compounds is in Thymus mugodzharicus. At the same time, we determined the antioxidant and antiradical activity, which was the highest for the Thymus mugodzharicus. Butylhydroxyanisole and ascorbic acid were used as comparison substances. Also, it was established that antioxidant and anti-radical activities depend on the concentration of the of all investigated samples. Based on obtained data, we believe that the extract of Thymus mugodzharicus can be recommended for further study on the antioxidant and antiradical activity in vivo, as well as the opportunity of this sample to demonstrate hepatoprotective effect. The study was sponsored by SANTO academic program.Keywords: in vitro, in vivo, antioxidant, hepatoprotective effect
Procedia PDF Downloads 3171146 Prevalence Of Periodontal Disease In Felines In The Outskirts Of The City Of Manaus, Brazil: An Epidemiological Study
Authors: Pármenas Costa Macedo do Nascimento
Abstract:
Periodontal disease is the most common disease in the oral cavity of felines. It starts with the accumulation of bacteria on the tooth surface supporting the tissues of the periodontal tissue, namely gums, alveolar bone, cementum, and periodontal ligament. The main clinical symptom observed by the owner is bad breath, which may lead to local and systemic consequences depending on the stage of periodontal disease, such as bleeding and bone loss. Therefore, the study is important to educate tutors to take better care of the felines oral health in order to try to prevent the disease. For this epidemiological study, the target population has been felines, located on the outskirts of Manaus, in the state of Amazonas, with a geographic area of 155.68 km², with no defined breed, from October 1st to 10th, 2021, whose samples has been randomly selected, with a detailed profile. The variables of interest for this study have been: absence or presence of periodontal disease, gender, age (delimited by age group), and condition (domiciled or homeless). Using a sample of 40 felines from 4 districts of the east side of Manaus chosen at random, an oral exam has been made to identify the studied disease. The animal's apparent age, condition, sex, and presence or absence of periodontal disease has been noted. It has been observed that 70% (28/40) of them had periodontal disease, mostly females, aged between 0 and 5 years and domiciled, totaling 30% (12/40).Keywords: felines, oral cavity, oral exam, periodontal disease
Procedia PDF Downloads 2131145 Anti-Angiogenic Effects of the Macrovipera lebetina obtusa Snake Crude Venom and Obtustatin
Authors: Narine Ghazaryan, Joana Catarina Macedo, Sara Vaz, Naira Ayvazyan, Elsa Logarinho
Abstract:
Macrovipera lebetina obtusa (MLO) is a poisonous snake in Armenia. Obtustatin represents the shortest known monomeric disintegrin, isolated from the snake venom of MLO, and is known to specifically inhibit α1β1 integrin. Its oncostatic effect is due to the inhibition of angiogenesis, which likely arises from α1β1 integrin inhibition in the endothelial cells. To explore the therapeutic potential of the MLO snake venom and obtustatin, we studied activity of obtustatin and MLO venom in vitro, by testing their efficacy in human dermal microvascular endothelial cells (HMVEC-D) and in vivo, using chick embryo chorioallantoic membrane assay (CAM assay). Our in vitro results showed that obtustatin in comparison with MLO venom did not exhibit cytotoxic activity in HMVEC-D cells in comparison to MLO venom. But in vivo results have shown that 4µg /embryo (90 µM) of obtustatin inhibited angiogenesis induced by FGF2 by 17% while MLO snake venom induced 22% reduction of the angiogenic index. The concentration of obtustatin in the crude MLO venom was 0.3 nM, which is 300.000 times less than the concentration of the obtustatin itself. Given this enormous difference in concentration, it is likely that some components of the crude venom contribute to the observed anti-angiogenic effect. Hypotheses will be ascertained to justify this action: components in the MLO venom may increase obtustatin efficacy or have independent but synergic anti-angiogenic activities.Keywords: angiogenesis, alpa1 beta 1 integrin, Macrovipera lebetina obtusa, obtustatin
Procedia PDF Downloads 1961144 Biodegradable Magnesium Alloys with Addition of Rare Earth Elements for Biomedical Applications
Authors: Yuncang Li, Cuie Wen
Abstract:
Biodegradable metallic materials such as magnesium (Mg)-based alloys have attracted extensive interest for use as bone implant materials. However, the high biodegradation rate of existing Mg alloys in the physiological environment of human body leads to losing mechanical integrity before adequate bone healing and producing a large volume of hydrogen gas. Therefore, slowing down the biodegradation rate of Mg alloys is a critical task in developing new biodegradable Mg alloy implant materials. One of the most effective approaches to achieve this is to strategically design new Mg alloys with low biodegradation rate, excellent biocompatibility, and enhanced mechanical properties. Our research selected biocompatible and biofunctional alloying elements such as zirconium (Zr), strontium (Sr), and rare earth elements (REEs) to alloy Mg and has developed a new series of Mg-Zr-Sr-REEs alloys for biodegradable implant applications. Research results indicated that Sr and Zr additions could refine the grain size, decrease the biodegradation rate, and enhance the biological behaviors of the Mg alloys. The REE addition, such as holmium (Ho) and dysprosium (Dy) to Mg-Zr-Sr alloys resulted in enhanced mechanical strength and decreased biodegradation rate. In addition, Ho and Dy additions (≤ 5 wt.%) to Mg-Zr-Sr alloys led to enhancement of cell adhesion and proliferation of osteoblast cells on the Mg-Zr-Sr-Ho/Dy alloys.Keywords: biocompatibility, magnesium, mechanical and biodegrade properties, rare earth elements
Procedia PDF Downloads 1211143 Demonstration of Risk Factors Associated with Male Athlete Triad in Young Elite Athlete from Pakistan
Authors: Muhammad Saleem
Abstract:
Background: Inattentive food choices and engagement in excessive physical activities by male athletes can potentially lead to adverse health consequences. Objective: The aim was to ascertain the occurrence of risk factors associated with the Male Athlete Triad among young elite athletes in Pakistan. Methodology: In 2018, a cross-sectional study based on questionnaires was conducted at the Pakistan Sports Board. The study aimed to explore the risk factors related to the Male Athlete Triad in young elite athletes who were part of national training camps in major metropolitan areas. The study included proficient male elite athletes aged 18 to 25 years, capable of understanding the English questionnaire. The athletes completed a survey encompassing aspects like demographic information, educational background, Body Mass Index (BMI), sports involvement, and hours of participation. Additionally, they filled out the Eating Attitude Test-26 (EAT-26) and questionnaires assessing risks of amenorrhea and low bone mineral density. The prevalence of risk factors for each of the three components was individually evaluated. The collected data underwent analysis using SPSS-20, with descriptive statistics being applied. Results: The study comprised a sample of 90 elite athletes (mean age: 23.57 ± 2.37 years, mean BMI: 21.97 ± 1.90) engaged in various sports. The EAT-26 results indicated that 50% of athletes were at risk of developing an eating disorder. Moreover, 83.3% exhibited disordered eating behaviors that necessitated referral. Risks for amenorrhea were observed in 15% of the participants, and regarding low bone mineral density, notable risks were absent except for the consumption of caffeinated beverages, which was noted in 51.7% of participants. Conclusion: The study identified a significant prevalence of disordered eating risk among male elite athletes in Pakistan. However, the risks associated with amenorrhea and low bone mineral density were not a major concern in this particular group.Keywords: 1. health and physical education risk factors male athlete associated with the male athlete traid in young elite athlete from pakistan., 2. sports sciences pakistan, 3. risk factors sports sciences pakistan, 4. triad and young elite athlete from pakistan
Procedia PDF Downloads 881142 Hybrid Manufacturing System to Produce 3D Structures for Osteochondral Tissue Regeneration
Authors: Pedro G. Morouço
Abstract:
One utmost challenge in Tissue Engineering is the production of 3D constructs capable of mimicking the functional hierarchy of native tissues. This is well stated for osteochondral tissue due to the complex mechanical functional unit based on the junction of articular cartilage and bone. Thus, the aim of the present study was to develop a new additive manufacturing system coupling micro-extrusion with hydrogels printing. An integrated system was developed with 2 main features: (i) the printing of up to three distinct hydrogels; (ii) in coordination with the printing of a thermoplastic structural support. The hydrogel printing module was projected with a ‘revolver-like’ system, where the hydrogel selection was made by a rotating mechanism. The hydrogel deposition was then controlled by pressured air input. The use of specific components approved for medical use was incorporated in the material dispensing system (Nordson EDF Optimum® fluid dispensing system). The thermoplastic extrusion modulus enabled the control of required extrusion temperature through electric resistances in the polymer reservoir and the extrusion system. After testing and upgrades, a hydrogel modulus with 3 syringes (3cm3 capacity each), with a pressure range of 0-2.5bar, a rotational speed of 0-5rpm, and working with needles from 200-800µm was obtained. This modulus was successfully coupled to the extrusion system that presented a temperature up to 300˚C, a pressure range of 0-12bar, and working with nozzles from 200-500µm. The applied motor could provide a velocity range 0-2000mm/min. Although, there are distinct printing requirements for hydrogels and polymers, the novel system could develop hybrid scaffolds, combining the 2 moduli. The morphological analysis showed high reliability (n=5) between the theoretical and obtained filament and pore size (350µm and 300µm vs. 342±4µm and 302±3µm, p>0.05, respectively) of the polymer; and multi-material 3D constructs were successfully obtained. Human tissues present very distinct and complex structures regarding their mechanical properties, organization, composition and dimensions. For osteochondral regenerative medicine, a multiphasic scaffold is required as subchondral bone and overlying cartilage must regenerate at the same time. Thus, a scaffold with 3 layers (bone, intermediate and cartilage parts) can be a promising approach. The developed system may give a suitable solution to construct those hybrid scaffolds with enhanced properties. The present novel system is a step-forward regarding osteochondral tissue engineering due to its ability to generate layered mechanically stable implants through the double-printing of hydrogels with thermoplastics.Keywords: 3D bioprinting, bone regeneration, cartilage regeneration, regenerative medicine, tissue engineering
Procedia PDF Downloads 1651141 Effects of Cymbopogon citratus, Stapf (CS) or Lemon Grass Ethanol Extract on Antioxidant and Vascular Disorders Parameters in Rat
Authors: Suphaket Saenthaweesuk, Nutiya Somparn, Atcharaporn Thewmore
Abstract:
The present study aims to investigate the effects of Cymbopogon citratus, Stapf (CS) or lemon grass ethanol extract on antioxidant and vascular disorders parameters in rat. The CS ethanol extract was screened for its phytochemical contents and antioxidant activity in vitro. Moreover, the extract was studied in rats to evaluate its effects in vivo. Rats were orally administered with CS at 1,000 mg/kg/day for 30 days. Phytochemical screening of CS extract indicated the presence of tannins, flavonoids and phenolic compounds. The extract contained phenolic compounds 1,400.10 ± 0.47 mg of gallic acid equivalents per gram CS extract. The free radical scavenging activity assessed by DPPH assay gave IC50 of 168.77 ± 3.32µg/mL, which is relatively lower than that of BHT with IC50 of 12.34 ± 1.14 µg/mL. In the animals, the protein expression of antioxidant enzymes, γ-glutamylcysteine ligase (γ-GCL) in liver was significantly increased. This was consistent with elevation of serum catalase (CAT) and superoxide dismutase (SOD) activities. However, Protein expression of vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule (ICAM-1) and endothelial nitric oxide synthase (eNOS) in heart and aorta were not differenced from normal control. Taken together, the present study provides evidence that CCS water extract exhibits direct antioxidant properties and can induce cytoprotective enzymes in vivo.Keywords: antioxidant, Cymbopogon citratus Stapf, VCAM-1, γ-glutamylcysteine ligase
Procedia PDF Downloads 3091140 The Osteocutaneous Distal Tibia Turn-over Fillet Flap: A Novel Spare-parts Orthoplastic Surgery Option for Functional Below-knee Amputation
Authors: Harry Burton, Alexios Dimitrios Iliadis, Neil Jones, Aaron Saini, Nicola Bystrzonowski, Alexandros Vris, Georgios Pafitanis
Abstract:
This article portrays the authors’ experience with a complex lower limb bone and soft tissue defect, following chronic osteomyelitis and pathological fracture, which was managed by the multidisciplinary orthoplastic team. The decision for functional amputation versus limb salvage was deemed necessary, enhanced by the principles of “spares parts” in reconstructive microsurgery. This case describes a successful use of the osteocutaneous distal tibia turn-over fillet flap that allowed ‘lowering the level of the amputation’ from a through knee to the conventional level of a below-knee amputation to preserve the knee joint function. This case demonstrates the value of ‘spare-parts’ surgery principles and how these concepts refine complex orthoplastic approaches when limb salvage is not possible to enhance function. The osteocutaneous distal tibia turn-over fillet flap is a robust technique for modified BKA reconstructions that provides sufficient bone length to achieve a tough, sensate stump and functional knee joint.Keywords: osteocutaneous flap, fillet flap, spare-parts surgery, Below knee amputation
Procedia PDF Downloads 1661139 Sphingosomes: Potential Anti-Cancer Vectors for the Delivery of Doxorubicin
Authors: Brajesh Tiwari, Yuvraj Dangi, Abhishek Jain, Ashok Jain
Abstract:
The purpose of the investigation was to evaluate the potential of sphingosomes as nanoscale drug delivery units for site-specific delivery of anti-cancer agents. Doxorubicin Hydrochloride (DOX) was selected as a model anti-cancer agent. Sphingosomes were prepared and loaded with DOX and optimized for size and drug loading. The formulations were characterized by Malvern zeta-seizer and Transmission Electron Microscopy (TEM) studies. Sphingosomal formulations were further evaluated for in-vitro drug release study under various pH profiles. The in-vitro drug release study showed an initial rapid release of the drug followed by a slow controlled release. In vivo studies of optimized formulations and free drug were performed on albino rats for comparison of drug plasma concentration. The in- vivo study revealed that the prepared system enabled DOX to have had enhanced circulation time, longer half-life and lower elimination rate kinetics as compared to free drug. Further, it can be interpreted that the formulation would selectively enter highly porous mass of tumor cells and at the same time spare normal tissues. To summarize, the use of sphingosomes as carriers of anti-cancer drugs may prove to be a fascinating approach that would selectively localize in the tumor mass, increasing the therapeutic margin of safety while reducing the side effects associated with anti-cancer agents.Keywords: sphingosomes, anti-cancer, doxorubicin, formulation
Procedia PDF Downloads 3031138 Arisarum Vulgare: Bridging Tradition and Science through Phytochemical Characterization and Exploring Therapeutic Potential via in vitro and in vivo Biological Activities
Authors: Boudjelal Amel
Abstract:
Arisarum vulgare, a member of the Araceae family, is an herbaceous perennial widely distributed in the Mediterranean region. A. vulgare is recognized for its medicinal properties and holds significant traditional importance in Algeria for the treatment of various human ailments, including pain, infections, inflammation, digestive disorders, skin problems, eczema, cancer, wounds, burns and gynecological diseases. Despite its extensive traditional use, scientific exploration of A. vulgare remains limited. The study aims to investigate for the first time the therapeutic potential of A. vulgare ethanolic extract obtained by ultrasound-assisted extraction. The chemical composition of the extract was determined by LC-MS/MS analysis. For in vitro phytopharmacological evaluation, several assays, including DPPH, ABTS, FRAP and reducing power, were employed to evaluate the antioxidant activity. The antibacterial activity was assessed againt Escherichia coli, Salmonella typhimurium, Staphylococus aureus, Enterococcus feacium by disk diffusion and microdilution methods. The possible inhibitory activity of ethanolic extract was analyzed against the cholinesterases enzymes (AChE and BChE). The DNA protection activity of A. vulgare ethanolic extract was estimated using the agarose gel electrophoresis method. The capacities of the extract to protect plasmid DNA (pBR322) from the oxidizing effects of H2O2 and UV treatment were evaluated by their DNA-breaking forms. The in vivo wound healing potential of a traditional ointment containing 5% of A. vulgare ethanolic extract was also investigated. The LC-MS/MS profiling of the extract revealed the presence of various bioactive compounds, including naringenin, chlorogenic, vanillic, cafeic, coumaric acids, trans-cinnamic and trans ferrulic acids. The plant extract presented considerable antioxidant potential, being the most active for Reducing power (0,07326±0.001 mg/ml) and DPPH (0.14±0.004 mg/ml). The extract showed the highest inhibition zone diameter against Enterococcus feacium (36±0.1 mm). The ethanolic extract of A. vulgare suppressed the growth of Staphylococus aureus, Escherichia coli and Salmonella typhimurium according to the MIC values. The extract of the plant significantly inhibited both AChE and BChE enzymes. DNA protection activity of the A. vulgare extract was determined as 90.41% for form I and 51.92% for form II. The in vivo experiments showed that 5% ethanolic extract ointment accelerated the wound healing process. The topical application of the traditional formulation enhanced wound closure (95,36±0,6 %) and improved histological parameters in the treated group compared to the control groups. The promising biological properties of Arisarum vulgare revealed that the plant could be appraised as a potential origin of bioactive molecules having multifunctional medicinal uses.Keywords: arisarum vulgare, LC-MS/MS, antioxidant activity, antimicrobial activity, cholinesterases enzymes inhibition, dna-damage activity, in vivo wound healing
Procedia PDF Downloads 691137 Parathyroid Hormone Receptor 1 as a Prognostic Indicator in Canine Osteosarcoma
Authors: Awf A. Al-Khan, Michael J. Day, Judith Nimmo, Mourad Tayebi, Stewart D. Ryan, Samantha J. Richardson, Janine A. Danks
Abstract:
Osteosarcoma (OS) is the most common type of malignant primary bone tumour in dogs. In addition to their critical roles in bone formation and remodeling, parathyroid hormone-related protein (PTHrP) and its receptor (PTHR1) are involved in progression and metastasis of many types of tumours in humans. The aims of this study were to determine the localisation and expression levels of PTHrP and PTHR1 in canine OS tissues using immunohistochemistry and to investigate if this expression is correlated with survival time. Formalin-fixed, paraffin-embedded tissue samples from 44 dogs with known survival time that had been diagnosed with primary osteosarcoma were analysed for localisation of PTHrP and PTHR1. Findings showed that both PTHrP and PTHR1 were present in all OS samples. The dogs with high level of PTHR1 protein (16%) had decreased survival time (P<0.05) compared to dogs with less PTHR1 protein. PTHrP levels did not correlate with survival time (P>0.05). The results of this study indicate that the PTHR1 is expressed differently in canine OS tissues and this may be correlated with poor prognosis. This may mean that PTHR1 may be useful as a prognostic indicator in canine OS and could represent a good therapeutic target in OS.Keywords: dog, expression, osteosarcoma, parathyroid hormone receptor 1 (PTHR1), parathyroid hormone-related protein (PTHrP), survival
Procedia PDF Downloads 2761136 The Efficacy of Andrographis paniculata and Chromolaena odorata Plant Extract against Malaria Parasite
Authors: Funmilola O. Omoya, Abdul O. Momoh
Abstract:
Malaria constitutes one of the major health problems in Nigeria. One of the reasons attributed for the upsurge was the development of resistance of Plasmodium falciparum and the emergence of multi-resistant strains of the parasite to anti-malaria drugs. A continued search for other effective, safe and cheap plant-based anti-malaria agents thus becomes imperative in the face of these difficulties. The objective of this study is therefore to evaluate the in vivo anti-malarial efficacy of ethanolic extracts of Chromolaena odorata and Androgaphis paniculata leaves. The two plants were evaluated for their anti-malaria efficacy in vivo in a 4-day curative test assay against Plasmodium berghei strain in mice. The group treated with 500mg/ml dose of ethanolic extract of A. paniculata plant showed parasite suppression with increase in Packed Cell Volume (PCV) value except day 3 which showed a slight decrease in PCV value. During the 4-day curative test, an increase in the PCV values, weight measurement and zero count of Plasmodium berghei parasite values was recorded after day 3 of drug administration. These results obtained in group treated with A. paniculata extract showed anti-malarial efficacy with higher mortality rate in parasitaemia count when compared with Chromolaena odorata group. These results justify the use of ethanolic extracts of A. paniculata plant as medicinal herb used in folklore medicine in the treatment of malaria.Keywords: anti-malaria, curative, plant-based anti-malaria agents, biology
Procedia PDF Downloads 2991135 Human Absorbed Dose Estimation of a New In-111 Imaging Agent Based on Rat Data
Authors: H. Yousefnia, S. Zolghadri
Abstract:
The measurement of organ radiation exposure dose is one of the most important steps to be taken initially, for developing a new radiopharmaceutical. In this study, the dosimetric studies of a novel agent for SPECT-imaging of the bone metastasis, 111In-1,4,7,10-tetraazacyclododecane-1,4,7,10 tetraethylene phosphonic acid (111In-DOTMP) complex, have been carried out to estimate the dose in human organs based on the data derived from rats. The radiolabeled complex was prepared with high radiochemical purity in the optimal conditions. Biodistribution studies of the complex was investigated in the male Syrian rats at selected times after injection (2, 4, 24 and 48 h). The human absorbed dose estimation of the complex was made based on data derived from the rats by the radiation absorbed dose assessment resource (RADAR) method. 111In-DOTMP complex was prepared with high radiochemical purity of >99% (ITLC). Total body effective absorbed dose for 111In-DOTMP was 0.061 mSv/MBq. This value is comparable to the other 111In clinically used complexes. The results show that the dose with respect to the critical organs is satisfactory within the acceptable range for diagnostic nuclear medicine procedures. Generally, 111In-DOTMP has interesting characteristics and can be considered as a viable agent for SPECT-imaging of the bone metastasis in the near future.Keywords: In-111, DOTMP, Internal Dosimetry, RADAR
Procedia PDF Downloads 4071134 Lung Tissue Damage under Diesel Exhaust Exposure: Modification of Proteins, Cells and Functions in Just 14 Days
Authors: Ieva Bruzauskaite, Jovile Raudoniute, Karina Poliakovaite, Danguole Zabulyte, Daiva Bironaite, Ruta Aldonyte
Abstract:
Introduction: Air pollution is a growing global problem which has been shown to be responsible for various adverse health outcomes. Immunotoxicity, such as dysregulated inflammation, has been proposed as one of the main mechanisms in air pollution-associated diseases. Chronic obstructive pulmonary disease (COPD) is among major morbidity and mortality causes worldwide and is characterized by persistent airflow limitation caused by the small airways disease (obstructive bronchiolitis) and irreversible parenchymal destruction (emphysema). Exact pathways explaining the air pollution induced and mediated disease states are still not clear. However, modern societies understand dangers of polluted air, seek to mitigate such effects and are in need for reliable biomarkers of air pollution. We hypothesise that post-translational modifications of structural proteins, e.g. citrullination, might be a good candidate biomarker. Thus, we have designed this study, where mice were exposed to diesel exhaust and the ongoing protein modifications and inflammation in lungs and other tissues were assessed. Materials And Methods: To assess the effects of diesel exhaust a in vivo study was designed. Mice (n=10) were subjected to everyday 2-hour exposure to diesel exhaust for 14 days. Control mice were treated the same way without diesel exhaust. The effects within lung and other tissues were assessed by immunohistochemistry of formalin-fixed and paraffin-embedded tissues. Levels of inflammation and citrullination related markers were investigated. Levels of parenchymal damage were also measured. Results: In vivo study corroborates our own data from in vitro and reveals diesel exhaust initiated inflammatory shift and modulation of lung peptidyl arginine deiminase 4 (PAD4), citrullination associated enzyme, levels. In addition, high levels of citrulline were observed in exposed lung tissue sections co-localising with increased parenchymal destruction. Conclusions: Subacute exposure to diesel exhaust renders mice lungs inflammatory and modifies certain structural proteins. Such structural changes of proteins may pave a pathways to lost/gain function of affected molecules and also propagate autoimmune processes within the lung and systemically.Keywords: air pollution, citrullination, in vivo, lungs
Procedia PDF Downloads 1561133 Ex Vivo Permeation Comparison Study of Flurbiprofen from Nanoparticles through Human Skin
Authors: Sheimah El Bejjaji, Lara Gorsek, Chandler Quilchez, Joaquim Suñer, Mireia Mallandrich
Abstract:
Flurbiprofen is an anti-inflammatory drug used in several treatments. The purpose of this study was to compare the permeation of two different formulations of flurbiprofen through the human skin. The first formulation was a solution of flurbiprofen dissolved with polyethylene glycol 3350 (PEG 3350). The second formulation was flurbiprofen encapsulated in poly-ɛ-caprolactone (PɛCL) nanoparticles (NPs), stabilized with poloxamer 188, submitted individually for freeze-drying with PEG 3350 as a cryoprotectant and sterilized by gamma-irradiation. Human skin was obtained from the abdominal region of a healthy patient. The experimental protocol was approved by the Bioethics Committee of Barcelona SCIAS Hospital (Spain), and they obtained the written informed consent forms. After being frozen to -20ºC, the skin samples were cut with a dermatome at 400 µm. The ex vivo permeation study was performed in Franz diffusion cells with a diffusion area of 2.54 cm². Skin samples were placed between two compartment sites, the dermal side in contact with the receptor medium and the epidermis side in contact with the donor chamber to which the formulation was applied. The permeation study was conducted for 24 hours at 32 ± 0.5 °C in accordance with sink conditions. The results were analyzed with an unpaired t-test, and the p-values indicate the formulation with nanoparticles had a higher permeability coefficient, flux, partition parameter, diffusion parameter, and lag time. The applicability of this formulation topically can benefit articulations and ligament inflammation as an alternative to oral drugs.Keywords: anti-inflammatory drug, flurbiprofen, human skin, nanoparticles, skin permeation
Procedia PDF Downloads 901132 Impact of Diet and COVID-19 Policies on Osteopenia in a Hispanic White Adolescent Girl
Authors: Maria Angelica Trak-Fellermeier, Alison K. Macchi, Rodolfo Galvan, Yolangel Hernandez, Thresia Gambon, Rebeca Martinez, Cristina Palacios
Abstract:
Poor lifestyle habits, vitamin D deficiency, and inadequate calcium intake, particularly during the COVID-19 pandemic, may contribute to severe osteopenia in childhood, increasing future fractures and osteoporosis risk. We here present a case of osteopenia in a 13-year-old white, Hispanic, premenarchal girl who completed the baseline visit of the MetA-Bone Trial during the COVID-19 pandemic. The premenarchal girl has a family history of osteoporosis (maternal grandfather) but no previous fractures; moderate outdoor activity was <1 hour/day 3 times/week with 8 hours/day of sleep. Consumption of dairy products and vegetables was <1 serving/day. Lab blood tests confirmed vitamin D deficiency (serum 25(OH)D: 9 ng/L) and hyperphosphatemia (5.2 mg/dL); other tests were normal. DXA scan Z‐score was ‐2.2 SD (indicative of osteopenia by age and sex). The premenarchal girl was referred to a pediatrician, who confirmed the results, and prescribed a daily supplement with 2000 IU of vitamin D and 1000 mg of calcium. Seclusion during the COVID-19 pandemic may have contributed to the severity of the findings. Therefore, we recommend screening children undergoing growth spurts for vitamin D, calcium, and poor lifestyle habits during and after the pandemic.Keywords: bone mass, vitamin D, puberty, Hispanic
Procedia PDF Downloads 1331131 Development and Characterization of a Film Based on Hydroxypropyl Methyl Cellulose Incorporated by a Phenolic Extract of Fennel and Reinforced by Magnesium Oxide: In Vivo - in Vitro
Authors: Mazouzi Nourdjihane, K. Boutemak, A. Haddad, Y. Chegreouche
Abstract:
In the last decades, biodegradable polymers have been considered as one of the most popular options for the delivery of drugs and various conventional doses. The film forming system (FFS) can be used in topical, transdermal, ophthalmic, oral and gastric applications. Recently this system has focused on improving drug delivery, which can promote drug release. In this context, the aim of this study is to create polymeric film-forming systems for the stomach and to evaluate and test their gastroprotective effects, comparing the effects of changes in composition on film characteristics. It uses a plant-derived polyphenol extract extracted from fennel to demonstrate anti-inflammatory activity in the film. The films are made from hydroxypropyl methylcellulose polymer and different types of plastic, glycerol and polyethylene glycol. The ffs properties show that MgO-glycerol-reinforced hydroxypropylmethylcellulose (HPMC-MgO-Gly) is better than that based on MgO-PEG-reinforced hydroxypropylmethylcellulose (HPMC-MgO-PEG). It is durable, has a faster drying time and allows for maximum recovery. Water vapor strength and blowing speed and other additions show another advantage of HPMC-MgO-Gly compared to HPMC-MgO-PEG, indicating good adhesion between the support (top) and film production. In this study, the gastroprotective effect of fennel phenol extract was found, showing that this plant material has a gastroprotective effect on ulcers and that the film can absorb the active substance.Keywords: film formin system, hydroxypropyl methylcellulose, magnesium oxide, in vivo
Procedia PDF Downloads 661130 In silico Designing and Insight into Antimalarial Potential of Chalcone-Quinolinylpyrazole Hybrids by Preclinical Study in Mice
Authors: Deepika Saini, Sandeep Jain, Ajay Kumar
Abstract:
The quinoline scaffold is one of the most widely studied in the discovery of derivatives with various heterocyclic moieties due to its potential antimalarial activities. In the present study, a chalcone series of quinoline derivatives clubbed with pyrazole were synthesized to evaluate their antimalarial property by in vitro schizont maturation inhibition assay against both chloroquine sensitive, 3D7 and chloroquine resistant, RKL9 strain of Plasmodium falciparum. Further, top five compounds were studied for in vivo preclinical study for antimalarial potential against P. berghei in Swiss albino mice. To understand the mechanism of synthesized analogues, they were screened computationally by molecular docking techniques. Compounds were docked into the active site of a protein receptor, Plasmodium falciparum Cysteine Protease Falcipain-2. The compounds were successfully synthesized, and structural confirmation was performed by FTIR, 1H-NMR, mass spectrometry and elemental analysis. In vitro study suggested that the compounds 5b, 5g, 5l, 5s and 5u possessed best antimalarial activity and further tested for in vivo screening. Compound 5u (CH₃ on both rings) with EC₅₀ 0.313 & 0.801 µg/ml against CQ-S & CQ-R strains of P. falciparum respectively and 78.01% suppression of parasitemia. The molecular docking studies of the compounds helped in understanding the mechanism of action against falcipain-2. The present study reveals the binding signatures of the synthesized ligands within the active site of the protein, and it explains the results from in vitro study in their EC₅₀ values and percentage parasitemia.Keywords: antimalarial activity, chalcone, docking, quinoline
Procedia PDF Downloads 4091129 Transdermal Therapeutic System of Lercanıdipine Hydrochloride: Fabrication and in Vivo Evaluation
Authors: Jiji Jose, R. Narayanacharyulu, Molly Mathew, Jisha Prems
Abstract:
Introduction: Lercanidipine hydrochloride (LD), an effective calcium channel blocker, widely used for the treatment of chronic stable angina and hypertension seems to be potential transdermal therapeutic system candidate, mainly due to its low oral bio availability, short half life and high first-pass metabolism. Objective: To develop transdermal therapeutic systems for LD and to evaluate its in vivo performance in rabbits. Methodology: Transdermal patches of LD were formulated using the polymer blend of eudragit RL100 (ERL) and polyvinyl pyrolidone (PVP) by casting method Propylene glycol (PG) and tween 80 were used as plasticizer and permeation enhancer respectively. The pharmaco kinetic parameters of LD after the administration of transdermal patches was compared with that of oral administration. The study was carried out in a two way crossover design in male New Zealand albino rabbits. Results: The formulation with ERL: PVP ratio 1:4 with 15% w/w PG as plasticizer and 4% w/w tween 80 as permeation enhancer showed the best drug release results. The pharmacokinetic parameters such as Cmax, tmax, mean residence time (MRT) and area under the curve (AUC 0-∞) were significantly different following transdermal administration compared to oral administration. The terminal half life of transdermally administered LD was found to similar that of oral administration. A sustained drug release over a period of 24 hrs was observed after transdermal administration. Conclusion: The fabricated transdermal delivery system have the potential to provide controlled and extended drug release, better bio availability and thus, this may improve the patient compliance.Keywords: transdermal therapeutic system, lercanidipine hydrochloride, eudragit, skinpermeation
Procedia PDF Downloads 6151128 Antimicrobial Evaluation of Polyphenon 60 and Ciprofloxacin Loaded Nano Emulsion against Uropathogenic Escherichia coli Bacteria and Its in vivo Analysis
Authors: Atinderpal Kaur, Shweta Dang
Abstract:
Our aim is to develop a nanoemulsion-based delivery system containing polyphenon 60 (P60) and ciprofloxacin (Cipro) for intravaginal delivery to treat urinary tract infection. In the present study Polyphenon 60 (P60) and ciprofloxacin (Cipro) were loaded in a single nano emulsion (NE) system via ultra-sonication technique and characterized for particle size, in vitro release and antibacterial efficacy against Bcl-2 level Escherichia coli bacteria. To determine in vivo pharmacokinetic parameters and intravaginal transportation of NE, gamma scintigraphy and biodistribution study was conducted by radiolabelling NE with technetium pertechnetate (99mTc). The preliminary antibacterial investigation showed synergy between these compounds with FICindex of 0.42. The developed formulation showed zeta potential +55.3 and particle size of 151.7 nm, with PDI of 0.196. The in vitro release percentage of P60 at the end of 7th hours was 94.8 ± 0.9 % whereas the release for Cipro was 75.1± 0.15 % in simulated vaginal media. MBC was identified and the findings demonstrated that in both ESBL (Extended Spectrum β- lactamase) and MBL (Metallo β- lactamase) cultures the P60+Cipro NE showed inhibition of growth of all the isolates at 2 mg/ml dilutions. The percentage per gram of radiolabelled drug was found (3.50±0.26) and (3.81±0.30) in kidney and urinary bladder, respectively at 3 h. From the findings, it was concluded that the developed P60+Cipro NE was transported efficiently throughout the target organs, had long duration of action and high biocompatibility via intravaginal administration as compared to oral administration.Keywords: ciprofloxacin, gamma scintigraphy, intravaginal drug delivery, Polyphenon 60
Procedia PDF Downloads 320