Search results for: recurrent drug
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 2284

Search results for: recurrent drug

2164 Proniosomes as a Drug Carrier for Topical Delivery of Tolnaftate

Authors: Mona Mahmoud Abou Samra, Alaa Hamed Salama, Ghada Awad, Soheir Said Mansy

Abstract:

Proniosomes are well documented for topical drug delivery and preferred over other vesicular systems because they are biodegradable, biocompatible, non-toxic, possess skin penetration ability and prolong the release of drugs by acting as depot in deeper layers of skin. Proniosome drug delivery was preferred due to improved stability of the system than niosomes. The present investigation aimed at formulation development and performance evaluation of proniosomal gel as a vesicular drug carrier system for antifungal drug tolnaftate. Proniosomes was developed using different nonionic surfactants such as span 60 and span 65 with cholesterol in different molar ratios by the Coacervation phase separation method in presence or absence of either lecithin or phospholipon 80 H. Proniosomal gel formulations of tolnaftate were characterized for vesicular shape & size, entrapment efficiency, rheological properties and release study. The effect of surfactants and additives on the entrapment efficiency, particle size and percent of drug released was studied. The selected proniosomal formulations for topical delivery of tolnaftate was subjected to a microbiological study in male rats infected with Trichophyton rubrum; the main cause of Tinea Pedis compared to the free drug and a market product and the results was recorded.

Keywords: fungal infection, proniosome, tolnaftate, trichophyton rubrum

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2163 Release of Calcein from Liposomes Using Low and High Frequency Ultrasound

Authors: Ghaleb A. Husseini, Salma E. Ahmed, Hesham G. Moussa, Ana M. Martins, Mohammad Al-Sayah, Nasser Qaddoumi

Abstract:

This abstract aims to investigate the use of targeted liposomes as anticancer drug carriers in vitro in combination with ultrasound applied as drug trigger; in order to reduce the side effects caused by traditional chemotherapy. Pegylated liposomes were used to encapsulate calcein and then release this model drug when 20-kHz, 40-kHz, 1-MHz and 3-MHz ultrasound were applied at different acoustic power densities. Fluorescence techniques were then used to measure the percent drug release of calcein from these targeted liposomes. Results showed that as the power density increases, at the four frequencies studied, the release of calcein also increased. Based on these results, we believe that ultrasound can be used to increase the rate and amount of chemotherapeutics release from liposomes.

Keywords: liposomes, calcein release, high frequency ultrasound, low frequency ultrasound, fluorescence techniques

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2162 In-silico Design of Riboswitch Based Potent Inhibitors for Vibrio cholera

Authors: Somdutt Mujwar, Kamal Raj Pardasani

Abstract:

Cholera pandemics are caused by facultative pathogenic Vibrio cholera bacteria persisting in the countries having warmer climatic conditions as well as the presence of large water bodies with huge amount of organic matter, it is responsible for the millions of deaths annually. Presently the available therapy for cholera is Oral Rehydration Therapy (ORT) with an antibiotic drug. Excessive utilization of life saving antibiotics drugs leads to the development of resistance by the infectious micro-organism against the antibiotic drugs resulting in loss of effectiveness of these drugs. Also, many side effects are also associated with the use of these antibiotic drugs. This riboswitch is explored as an alternative drug target for Vibrio cholera bacteria to overcome the problem of drug resistance as well as side effects associated with the antibiotics drugs. The bacterial riboswitch is virtually screened with 24407 legends to get possible drug candidates. The 10 ligands showing best binding with the riboswitch are selected to design a pharmacophore, which can be utilized to design lead molecules by using the phenomenon of bioisosterism.

Keywords: cholera, drug design, ligand, riboswitch, pharmacophore

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2161 Measure of Pleasure of Drug Users

Authors: Vano Tsertsvadze, Marina Chavchanidze, Lali Khurtsia

Abstract:

Problem of drug use is often seen as a combination of psychological and social problems, but this problem can be considered as economically rational decision in the process of buying pleasure (looking after children, reading, harvesting fruits in the fall, sex, eating, etc.). Before the adoption of the decisions people face to a trade-off - when someone chooses a delicious meal, she takes a completely rational decision, that the pleasure of eating has a lot more value than the pleasure which she will experience after two months diet on the summer beach showing off her beautiful body. This argument is also true for alcohol, drugs and cigarettes. Smoking has a negative effect on health, but smokers are not afraid of the threat of a lung cancer after 40 years, more valuable moment is a pleasure from smoking. Our hypothesis - unsatisfied pleasure and frustration, probably determines the risk of dependence on drug abuse. The purpose of research: 1- to determine the relative measure unit of pleasure, which will be used to measure and assess the intensity of various human pleasures. 2- to compare the intensity of the pleasure from different kinds of activity, with pleasures received from drug use. 3- Based on the analysis of data, to identify factors affecting the rational decision making. Research method: Respondents will be asked to recall the greatest pleasure of their life, which will be used as a measure of the other pleasures. The study will use focus groups and structured interviews.

Keywords: drug, drug-user, measurement, satisfaction

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2160 Vision-Based Collision Avoidance for Unmanned Aerial Vehicles by Recurrent Neural Networks

Authors: Yao-Hong Tsai

Abstract:

Due to the sensor technology, video surveillance has become the main way for security control in every big city in the world. Surveillance is usually used by governments for intelligence gathering, the prevention of crime, the protection of a process, person, group or object, or the investigation of crime. Many surveillance systems based on computer vision technology have been developed in recent years. Moving target tracking is the most common task for Unmanned Aerial Vehicle (UAV) to find and track objects of interest in mobile aerial surveillance for civilian applications. The paper is focused on vision-based collision avoidance for UAVs by recurrent neural networks. First, images from cameras on UAV were fused based on deep convolutional neural network. Then, a recurrent neural network was constructed to obtain high-level image features for object tracking and extracting low-level image features for noise reducing. The system distributed the calculation of the whole system to local and cloud platform to efficiently perform object detection, tracking and collision avoidance based on multiple UAVs. The experiments on several challenging datasets showed that the proposed algorithm outperforms the state-of-the-art methods.

Keywords: unmanned aerial vehicle, object tracking, deep learning, collision avoidance

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2159 Solid Dispersions of Cefixime Using β-Cyclodextrin: Characterization and in vitro Evaluation

Authors: Nagasamy Venkatesh Dhandapani, Amged Awad El-Gied

Abstract:

Cefixime, a BCS class II drug, is insoluble in water but freely soluble in acetone and in alcohol. The aqueous solubility of cefixime in water is poor and exhibits exceptionally slow and intrinsic dissolution rate. In the present study, cefixime and β-Cyclodextrin (β-CD) solid dispersions were prepared with a view to study the effect and influence of β-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of cefixime was increased in the presence of β-CD and was classified as AL-type. Effect of variable, such as drug:carrier ratio, was studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR) and Differential scanning calorimetry (DSC). These studies revealed that a distinct loss of drug crystallinity in the solid molecular dispersions is ostensibly accounting for enhancement of dissolution rate in distilled water. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersions of cefixime showed a 6.77 times fold increase in dissolution rate over the pure drug.

Keywords: β-cyclodextrin, cefixime, dissolution, Kneading method, solid dispersions, release kinetics

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2158 Drug Therapy Problem and Its Contributing Factors among Pediatric Patients with Infectious Diseases Admitted to Jimma University Medical Center, South West Ethiopia: Prospective Observational Study

Authors: Desalegn Feyissa Desu

Abstract:

Drug therapy problem is a significant challenge to provide high quality health care service for the patients. It is associated with morbidity, mortality, increased hospital stay, and reduced quality of life. Moreover, pediatric patients are quite susceptible to drug therapy problems. Thus this study aimed to assess drug therapy problem and its contributing factors among pediatric patients diagnosed with infectious disease admitted to pediatric ward of Jimma university medical center, from April 1 to June 30, 2018. Prospective observational study was conducted among pediatric patients with infectious disease admitted from April 01 to June 30, 2018. Drug therapy problems were identified by using Cipolle’s and strand’s drug related problem classification method. Patient’s written informed consent was obtained after explaining the purpose of the study. Patient’s specific data were collected using structured questionnaire. Data were entered into Epi data version 4.0.2 and then exported to statistical software package version 21.0 for analysis. To identify predictors of drug therapy problems occurrence, multiple stepwise backward logistic regression analysis was done. The 95% CI was used to show the accuracy of data analysis and statistical significance was considered at p-value < 0.05. A total of 304 pediatric patients were included in the study. Of these, 226(74.3%) patients had at least one drug therapy problem during their hospital stay. A total of 356 drug therapy problems were identified among two hundred twenty six patients. Non-compliance (28.65%) and dose too low (27.53%) were the most common type of drug related problems while disease comorbidity [AOR=3.39, 95% CI= (1.89-6.08)], Polypharmacy [AOR=3.16, 95% CI= (1.61-6.20)] and more than six days stay in hospital [AOR=3.37, 95% CI= (1.71-6.64) were independent predictors of drug therapy problem occurrence. Drug therapy problems were common in pediatric patients with infectious disease in the study area. Presence of comorbidity, polypharmacy and prolonged hospital stay were the predictors of drug therapy problem in study area. Therefore, to overcome the significant gaps in pediatric pharmaceutical care, clinical pharmacists, Pediatricians, and other health care professionals have to work in collaboration.

Keywords: drug therapy problem, pediatric, infectious disease, Ethiopia

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2157 Fabrication and Characterization of Dissolvable Microneedle Patches Using Different Compositions and Ratios of Hyaluronic Acid and Zinc Oxide Nanoparticles

Authors: Dada Kolawole Segun

Abstract:

Transdermal drug delivery has gained popularity as a non-invasive method for controlled drug release compared to traditional delivery routes. Dissolvable transdermal patches have emerged as a promising platform for delivering a variety of drugs due to their ease of use. The objective of this research was to create and characterize dissolvable transdermal patches using various compositions and ratios of hyaluronic acid and zinc oxide nanoparticles. A micromolding technique was utilized to fabricate the patches, which were subsequently characterized using scanning electron microscopy, atomic force microscopy, and tensile strength testing. In vitro drug release studies were conducted to evaluate the drug release kinetics of the patches. The study found that the mechanical strength and dissolution properties of the patches were influenced by the hyaluronic acid and zinc oxide nanoparticle ratios used in the fabrication process. Moreover, the patches demonstrated controlled delivery of model drugs through the skin, highlighting their potential for transdermal drug delivery applications. The results suggest that dissolvable transdermal patches can be tailored to meet specific requirements for drug delivery applications using different compositions and ratios of hyaluronic acid and zinc oxide nanoparticles. This development has the potential to improve treatment outcomes and patient compliance in various therapeutic areas.

Keywords: transdermal drug delivery, characterization, skin permeation, biodegradable materials

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2156 A Diagnostic Challenge of Drug Resistant Childhood Tuberculosis in Developing World

Authors: Warda Fatima, Hasnain Javed

Abstract:

The emerging trend of Drug resistance in childhood Tuberculosis is increasing worldwide and now becoming a priority challenge for National TB Control Programs of the world. Childhood TB accounts for 10-15% of total TB burden across the globe and same proportion is quantified in case of drug resistant TB. One third population suffering from MDR TB dies annually because of non-diagnosis and unavailability of appropriate treatment. However, true Childhood MDR TB cannot be estimated due to non-confirmation. Diagnosis of Pediatric TB by sputum Smear Microscopy and Culture inoculation are limited due to paucibacillary nature and difficulties in obtaining adequate sputum specimens. Diagnosis becomes more difficult when it comes to HIV infected child. New molecular advancements for early case detection of TB and MDR TB in adults have not been endorsed in children. Multi centered trials are needed to design better diagnostic approaches and efficient and safer treatments for DR TB in high burden countries. The aim of the present study is to sketch out the current situation of the childhood Drug resistant TB especially in the developing world and to highlight the classic and novel methods that are to be implemented in high-burden resource-limited locations.

Keywords: drug resistant TB, childhood, diagnosis, novel methods

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2155 Protein Tertiary Structure Prediction by a Multiobjective Optimization and Neural Network Approach

Authors: Alexandre Barbosa de Almeida, Telma Woerle de Lima Soares

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Protein structure prediction is a challenging task in the bioinformatics field. The biological function of all proteins majorly relies on the shape of their three-dimensional conformational structure, but less than 1% of all known proteins in the world have their structure solved. This work proposes a deep learning model to address this problem, attempting to predict some aspects of the protein conformations. Throughout a process of multiobjective dominance, a recurrent neural network was trained to abstract the particular bias of each individual multiobjective algorithm, generating a heuristic that could be useful to predict some of the relevant aspects of the three-dimensional conformation process formation, known as protein folding.

Keywords: Ab initio heuristic modeling, multiobjective optimization, protein structure prediction, recurrent neural network

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2154 Self-Carried Theranostic Nanoparticles for in vitro and in vivo Cancer Therapy with Real-Time Monitoring of Drug Release

Authors: Jinfeng Zhang, Chun-Sing Lee

Abstract:

The use of different nanocarriers for delivering hydrophobic pharmaceutical agents to tumor sites has garnered major attention. Despite the merits of these nanocarriers, further studies are needed for improving their drug loading capacities (typically less than 10%) and reducing their potential systemic toxicity. So development of alternative self-carried nanodrug delivery strategies without using any inert carriers is highly desirable. In this study, we developed a self-carried theranostic curcumin (Cur) nanodrug for highly effective cancer therapy in vitro and in vivo with real-time monitoring of drug release. With a biocompatible C18PMH-PEG functionalization, the Cur nanoparticles (NPs) showed excellent dispersibility and outstanding stability in physiological environment, with drug loading capacity higher than 78 wt.%. Both confocal microscopy and flow cytometry confirmed the cellular fluorescent “OFF-ON” activation and real-time monitoring of Cur molecule release, showing its potential for cancer diagnosis. In vitro and in vivo experiments clearly show that therapeutic efficacy of the PEGylated Cur NPs is much better than that of free Cur. This self-carried theranostic strategy with real-time monitoring of drug release may open a new way for simultaneous cancer therapy and diagnosis.

Keywords: drug delivery, in vitro and in vivo cancer therapy, real-time monitoring, self-carried

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2153 Pattern of Adverse Drug Reactions with Platinum Compounds in Cancer Chemotherapy at a Tertiary Care Hospital in South India

Authors: Meena Kumari, Ajitha Sharma, Mohan Babu Amberkar, Hasitha Manohar, Joseph Thomas, K. L. Bairy

Abstract:

Aim: To evaluate the pattern of occurrence of adverse drug reactions (ADRs) with platinum compounds in cancer chemotherapy at a tertiary care hospital. Methods: It was a retrospective, descriptive case record study done on patients admitted to the medical oncology ward of Kasturba Hospital, Manipal from July to November 2012. Inclusion criteria comprised of patients of both sexes and all ages diagnosed with cancer and were on platinum compounds, who developed at least one adverse drug reaction during or after the treatment period. CDSCO proforma was used for reporting ADRs. Causality was assessed using Naranjo Algorithm. Results: A total of 65 patients was included in the study. Females comprised of 67.69% and rest males. Around 49.23% of the ADRs were seen in the age group of 41-60 years, followed by 20 % in 21-40 years, 18.46% in patients over 60 years and 12.31% in 1-20 years age group. The anticancer agents which caused adverse drug reactions in our study were carboplatin (41.54%), cisplatin (36.92%) and oxaliplatin (21.54%). Most common adverse drug reactions observed were oral candidiasis (21.53%), vomiting (16.92%), anaemia (12.3%), diarrhoea (12.3%) and febrile neutropenia (0.08%). The results of the causality assessment of most of the cases were probable. Conclusion: The adverse effect of chemotherapeutic agents is a matter of concern in the pharmacological management of cancer as it affects the quality of life of patients. This information would be useful in identifying and minimizing preventable adverse drug reactions while generally enhancing the knowledge of the prescribers to deal with these adverse drug reactions more efficiently.

Keywords: adverse drug reactions, platinum compounds, cancer, chemotherapy

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2152 Formulation and Evaluation of TDDS for Sustained Release Ondansetron HCL Patches

Authors: Baljinder Singh, Navneet Sharma

Abstract:

The skin can be used as the site for drug administration for continuous transdermal drug infusion into the systemic circulation. For the continuous diffusion/penetration of the drugs through the intact skin surface membrane-moderated systems, matrix dispersion type systems, adhesive diffusion controlled systems and micro reservoir systems have been developed. Various penetration enhancers are used for the drug diffusion through skin. In matrix dispersion type systems, the drug is dispersed in the solvent along with the polymers and solvent allowed to evaporate forming a homogeneous drug-polymer matrix. Matrix type systems were developed in the present study. In the present work, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising of ondansetron-HCl with different ratios of hydrophilic and hydrophobic polymeric combinations using solvent evaporation technique. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. The patches were further subjected to various physical evaluations along with the in-vitro permeation studies using rat skin. On the basis of results obtained form the in vitro study and physical evaluation, the patches containing hydrophilic polymers i.e. polyvinyl alcohol and poly vinyl pyrrolidone with oleic acid as the penetration enhancer(5%) were considered as suitable for large scale manufacturing with a backing layer and a suitable adhesive membrane.

Keywords: transdermal drug delivery, penetration enhancers, hydrophilic and hydrophobic polymers, ondansetron HCl

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2151 Pharmacovigilance: An Empowerment in Safe Utilization of Pharmaceuticals

Authors: Pankaj Prashar, Bimlesh Kumar, Ankita Sood, Anamika Gautam

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Pharmacovigilance (PV) is a rapidly growing discipline in pharmaceutical industries as an integral part of clinical research and drug development over the past few decades. PV carries a breadth of scope from drug manufacturing to its regulation with safer utilization. The fundamental steps of PV not only includes data collection and verification, coding of drugs with adverse drug reactions, causality assessment and timely reporting to the authorities but also monitoring drug manufacturing, safety issues, product quality and conduction of due diligence. Standardization of adverse event information, collaboration of multiple departments in different companies, preparation of documents in accordance to both governmental as well as non-governmental organizations (FDA, EMA, GVP, ICH) are the advancements in discipline of PV. De-harmonization, lack of predictive drug safety models, improper funding by government, non-reporting, and non-acceptability of ADRs by developing countries and reports directly from patients to the monitoring centres respectively are the major road backs of PV. Mandatory pharmacovigilance reporting, frequent inspections, funding by government, educating and training medical students, pharmacists and nurses in this segment can bring about empowerment in PV. This area needs to be addressed with a sense of urgency for the safe utilization of pharmaceuticals.

Keywords: pharmacovigilance, regulatory, adverse event, drug safety

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2150 Pterygium Recurrence Rate and Influencing Factors for Recurrence of Pterygium after Pterygium Surgery at an Eastern Thai University Hospital

Authors: Luksanaporn Krungkraipetch

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Pterygium is a frequent ocular surface lesion that begins in the limbal conjunctiva within the palpebral fissure and spreads to the cornea. The lesion is more common in the nasal limbus than in the temporal, and it has a wing-like aspect. Indications for surgery, in decreasing order of significance, are growth over the corneal center, decreased vision due to corneal deformation, documented growth, sensations of discomfort, and esthetic concerns. The aim of this study is twofold: first, to determine the frequency of pterygium recurrence after surgery at the mentioned hospital, and second, to identify the factors that influence the recurrence of pterygium. The research design is a retrospective examination of 164 patient samples in an eastern Thai university hospital (Code 13766). Data analysis is descriptive statistics analysis, i.e., basic data details about pterygium surgery and the risk of recurrent pterygium, and for factor analysis, the inferential statistics chi-square and ANOVA are utilized. Twenty-four of the 164 patients who underwent surgery exhibited recurrent pterygium. Consequently, the incidence of recurrent pterygium after surgery was 14.6%. There were an equal number of men and women present. The participants' ages ranged from 41 to 60 years (62, 8 percent). According to the findings, the majority of patients were female (60.4%), over the age of 60 (51.2%), did not live near the beach (83.5%), did not have an underlying disease (92.1%), and 95.7% did not have any other eye problems. Gender (X² = 1.26, p = .289), age (X² = 5.86, p = .119), an address near the sea (X² = 3.30, p = .081)), underlying disease (X² = 0.54, p = .694), and eye disease (X² = 0.00, p = 1.00) had no effect on pterygium recurrence. Recurrences occurred in 79.1% of all surgical procedures and 11.6% of all patients using the bare sclera technique. The recurrence rate for conjunctival autografts was 20.9% for all procedures and 3.0% for all participants. Mitomycin-C and amniotic membrane transplant techniques had no recurrence following surgery. Comparing the surgeries done on people with recurrent pterygium did not show anything important (F = 1.13, p = 0.339). In conclusion, the prevalence of pterygium recurrence following pterygium, 14.6%, does not differ from earlier research. Underlying disease, other eye conditions, and surgical procedures such as pterygium recurrence are unaffected by pterygium surgery.

Keywords: pterygium, recurrence pterygium, pterygium surgery, excision pterygium

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2149 PEG-b-poly(4-vinylbenzyl phosphonate) Coated Magnetic Iron Oxide Nanoparticles as Drug Carrier System: Biological and Physicochemical Characterization

Authors: Magdalena Hałupka-Bryl, Magdalena Bednarowicz, Ryszard Krzyminiewski, Yukio Nagasaki

Abstract:

Due to their unique physical properties, superparamagnetic iron oxide nanoparticles are increasingly used in medical applications. They are very useful carriers for delivering antitumor drugs in targeted cancer treatment. Magnetic nanoparticles (PEG-PIONs/DOX) with chemotherapeutic were synthesized by coprecipitation method followed by coating with biocompatible polymer PEG-derivative (poly(ethylene glycol)-block-poly(4-vinylbenzylphosphonate). Complete physicochemical characterization was carried out (ESR, HRTEM, X-ray diffraction, SQUID analysis) to evaluate the magnetic properties of obtained PEG-PIONs/DOX. Nanoparticles were investigated also in terms of their stability, drug loading efficiency, drug release and antiproliferative effect on cancer cells. PEG-PIONs/DOX have been successfully used for the efficient delivery of an anticancer drug into the tumor region. Fluorescent imaging showed the internalization of PEG-PIONs/DOX in the cytoplasm. Biodistribution studies demonstrated that PEG-PIONs/DOX preferentially accumulate in tumor region via the enhanced permeability and retention effect. The present findings show that synthesized nanosystem is promising tool for potential magnetic drug delivery.

Keywords: targeted drug delivery, magnetic properties, iron oxide nanoparticles, biodistribution

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2148 Effect of Different Sterilization Processes on Drug Loaded Silicone-Hydrogel

Authors: Raquel Galante, Marina Braga, Daniela Ghisleni, Terezinha J. A. Pinto, Rogério Colaço, Ana Paula Serro

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The sensitive nature of soft biomaterials, such as hydrogels, renders their sterilization a particularly challenging task for the biomedical industry. Widely used contact lenses are now studied as promising platforms for topical corneal drug delivery. However, to the best of the authors knowledge, the influence of sterilization methods on these systems has yet to be evaluated. The main goal of this study was to understand how different pairs drug-hydrogel would interact under an ozone-based sterilization method in comparison with two conventional processes (steam heat and gamma irradiation). For that, Si-Hy containing hydroxylethyl methacrylate (HEMA) and [tris(trimethylsiloxy)silyl]propyl methacrylate (TRIS) was produced and soaked in different drug solutions, commonly used for the treatment of ocular diseases (levofloxacin, chlorhexidine, diclofenac and timolol maleate). The drug release profiles and main material properties were evaluated before and after the sterilization. Namely, swelling capacity was determined by water uptake studies, transparency was accessed by UV-Vis spectroscopy, surface topography/morphology by scanning electron microscopy (SEM) and mechanical properties by performing tensile tests. The drug released was quantified by high performance liquid chromatography (HPLC). The effectiveness of the sterilization procedures was assured by performing sterility tests. Ozone gas method led to a significant reduction of drug released and to the formation of degradation products specially for diclofenac and levofloxacin. Gamma irradiation led to darkening of the loaded Si-Hys and to the complete degradation of levofloxacin. Steam heat led to smoother surfaces and to a decrease of the amount of drug released, however, with no formation of degradation products. This difference in the total drug released could be the related to drug/polymer interactions promoted by the sterilization conditions in presence of the drug. Our findings offer important insights that, in turn, could be a useful contribution to the safe development of actual products.

Keywords: drug delivery, silicone hydrogels, sterilization, gamma irradiation, steam heat, ozone gas

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2147 Development of Drug Delivery Systems for Endoplasmic Reticulum Amino Peptidases Modulators Using Electrospinning

Authors: Filipa Vasconcelos

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The administration of endoplasmic reticulum amino peptidases (ERAP1 or ERAP2) inhibitors can be used for therapeutic approaches against cancer and auto-immune diseases. However, one of the main shortcomings of drug delivery systems (DDS) is associated with the drug off-target distribution, which can lead to an increase in its side effects on the patient’s body. To overcome such limitations, the encapsulation of four representative compounds of ERAP inhibitors into Polycaprolactone (PCL), Polyvinyl-alcohol (PVA), crosslinked PVA, and PVA with nanoparticles (liposomes) electrospun fibrous meshes is proposed as a safe and controlled drug release system. The use of electrospun fibrous meshes as a DDS allows efficient solvent evaporation giving limited time to the encapsulated drug to recrystallize, continuous delivery of the drug while the fibers degrade, prevention of initial burst release (sustained release), tunable dosages, and the encapsulation of other agents. This is possible due to the fibers' small diameters and resemblance to the extracellular matrix (confirmed by scanning electron microscopy results), high specific surface area, and good mechanical strength/stability. Furthermore, release studies conducted on PCL, PVA, crosslinked PVA, and PVA with nanoparticles (liposomes) electrospun fibrous meshes with each of the ERAP compounds encapsulated demonstrated that they were capable of releasing >60%, 50%, 40%, and 45% of the total ERAP concentration, respectively. Fibrous meshes with ERAP_E compound encapsulated achieved higher released concentrations (75.65%, 62.41%, 56.05%, and 65.39%, respectively). Toxicity studies of fibrous meshes with encapsulated compounds are currently being accessed in vitro, as well as pharmacokinetics and dynamics studies. The last step includes the implantation of the drug-loaded fibrous meshes in vivo.

Keywords: drug delivery, electrospinning, ERAP inhibitors, liposomes

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2146 Stressful Events and Serious Mood Disorders

Authors: Horesh Reinman Netta

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Objectives: To examine the relationship between stressful life events and recurrent major depressive disorders Methods: Three groups of 50 subjects were assessed. One group had a recurrent major depressive disorder with melancholic features; the second group met the criteria for borderline personality disorder, and the third consisted of healthy controls. The Structured Clinical Interview for AXIS I DSM-IV Disorders sand the Structured Clinical Interview for AXIS II DSM-IV Disorders were used for diagnosis. The Israel Psychiatric Epidemiology Research Interview (IPERI) Life Event Scale and the Coddington Life Events Schedule (CLES) were used to measure life events which were confirmed with a confirmatory semi-structured interview. The Beck Depression Inventory and the Satisfaction from Life scales were also administered. Results : The total number of loss-related events in childhood and in the year preceding the first episode was significantly higher in the affective disorder group than in the two control groups. Total number of LE, uncontrolled and independent events were also more common in the depressed patients in the year preceding the first episode. No category of SLE was differentiated among any of the three groups during any period of time following the first depressive episode. Conclusions: SLE play an important role in the onset of affective disorders. There appear to be specific kinds of SLE occurring in childhood and in the year preceding a first episode that have particular significance. SLE may have a lesser role in the maintenance of this illness.

Keywords: modd dosorders, recurrent depression, stress, life events

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2145 Iontophoretic Drug Transport of Some Anti-Diabetic Agents

Authors: Ashish Jain, Satish Nayak

Abstract:

Transdermal iontophoretic drug delivery system is viable drug delivery platform technology and has a strong market worldwide. Transdermal drug delivery system is particularly desirable for therapeutic agents that need prolonged administration at controlled plasma level. This makes appropriateness to antihypertensive and anti-diabetic agents for their transdermal development. Controlled zero order absorption, easily termination of drug delivery and easy to administration also support for popularity of transdermal delivery. In this current research iontophoretic delivery of various anti diabetic agents like glipizide, glibenclamide and glimepiride were carried out. The experiments were carried out at different drug concentrations and different current densities using cathodal iontophoresis. Diffusion cell for iontophoretic permeation study was modified according to Glikfield Design. Pig skin was used for in vitro permeation study and for the in-vivo study New Zealand rabbits were used. At all concentration level iontophoresis showed enhanced permeation rate compared to passive controls. Iontophoretic transports of selected drugs were found to be increased with the current densities. Results showed that target permeation rate for selected drugs could be achieved with the aid of iontophoresis by increasing the area in an appreciable range.

Keywords: transdermal, iontophoresis, pig skin, rabbits, glipizide, glibeclamide

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2144 Current Practices of Permitted Daily Exposure (PDE) Calculation and Selection

Authors: Annie Ramanbhai Mecwan

Abstract:

Cleaning validation in a pharmaceutical manufacturing facility is documented evidence that a cleaning process has effectively removed contaminants, residues from previous drug products and cleaning agents below a pre-defined threshold from the reusable tools and parts of equipment. In shared manufacturing facilities more than one drug product is prepared. After cleaning of reusable tools and parts of equipment after one drug product manufacturing, there are chances that some residues of drug substance from previously manufactured drug products may be retained on the equipment and can carried forward to the next drug product and thus cause cross-contamination. Health-based limits through the derivation of a safe threshold value called permitted daily exposure (PDE) for the residues of drug substances should be employed to identify the risks posed at these manufacturing facilities. The PDE represents a substance-specific dose that is unlikely to cause an adverse effect if an individual is exposed to or below this dose every day for a lifetime. There are different practices to calculate PDE. Data for all APIs in the public domain are considered to calculate PDE value though, company to company may vary the final PDE value based on different toxicologist’s perspective or their subjective evaluation. Hence, Regulatory agencies should take responsibility for publishing PDE values for all APIs as it is done for elemental PDEs. This will harmonize the PDE values all over the world and prevent the unnecessary load on manufacturers for cleaning validation

Keywords: active pharmaceutical ingredient, good manufacturing practice, NOAEL, no observed adverse effect level, permitted daily exposure

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2143 Drug Abuse among Immigrant Youth in Canada

Authors: Qin Wei

Abstract:

There has been an increased number of immigrants arriving in Canada and a concurrent rise in the number of immigrant youth suffering from drug abuse. Immigrant youths’ drug abuse has become a significant social and public health concern for researchers. This literature review explores the nature of immigrant youths’ drug abuse by examining the factors influencing the onset of substance misuse, the barriers that discourage youth to seek out treatment, and how to resolve addictions amidst immigrant youth. Findings from the literature demonstrate that diminished parental supervision, acculturation challenges, peer conformity, discrimination, and ethnic marginalization are all significant factors influencing youth to use drugs as an outlet for their pain, while culturally competent care and fear of family and culture-based addiction stigma act as barriers discouraging youth from seeking out addiction support. To resolve addiction challenges amidst immigrant youth, future research should focus on promoting and implementing culturally sensitive practices and psychoeducational initiatives into immigrant communities and within public health policies.

Keywords: approaches, barriers, drug abuse, Canada, immigrant youth, reasons

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2142 Iontophoretic Drug Transport: An Non-Invasive Transdermal Approach

Authors: Ashish Jain, Shivam Tayal

Abstract:

There has been great interest in the field of Iontophoresis since few years due to its great applications in the field of controlled transdermal drug delivery system. It is an technique which is used to enhance the transdermal permeation of ionized high molecular weight molecules across the skin membrane especially Peptides & Proteins by the application of direct current of 1-4 mA for 20-40 minutes whereas chemical must be placed on electrodes with same charge. Iontophoresis enhanced the delivery of drug into the skin via pores like hair follicles, sweat gland ducts etc. rather than through stratum corneum. It has wide applications in the field of experimental, Therapeutic, Diagnostic, Dentistry etc. Medical science is using it to treat Hyperhidrosis (Excessive sweating) in hands and feet and to treat other ailments like hypertension, Migraine etc. Nowadays commercial transdermal iontophoretic patches are available in the market to treat different ailments. Researchers are keen to research in this field due to its vast applications and advantages.

Keywords: iontophoresis, novel drug delivery, transdermal, permeation enhancer

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2141 Development and in vitro Characterization of Loteprednol Etabonate-Loaded Polymeric Nanoparticles for Ocular Delivery

Authors: Abhishek Kumar Sah, Preeti K. Suresh

Abstract:

Effective drug delivery to the eye is a massive challenge, due to complicated physiological ocular barriers, rapid washout by tear and nasolachrymal drainage. Thus, most of the conventional ophthalmic formulations face the problem of low ocular bioavailability. Ophthalmic drug therapy can be improved by enhancing the precorneal drug retention along with improved drug penetration. The aim of the present investigation was to develop and evaluate a biodegradable polymer poly (D, L-lactide-co-glycolide) (PLGA) coated nanoparticulate carrier of loteprednol etabonate. PLGA nanoparticles were prepared by modified emulsification/solvent diffusion method using high-speed homogenizer followed by sonication. The nanoparticles were characterized for various parameters such as particle size, zeta potential, polydispersity index, X-ray powder diffraction (XRD), Transmission electron microscopy (TEM), in vitro drug release profile and stability. The prepared nanocarriers displayed mean particle size in the range of 271.7 to 424.4 nm, with zeta potential less than –10 mV. In vitro release in simulated tear fluid (STF) nanocarrier showed an extended release profile of loteprednol etabonate. TEM confirmed the spherical morphology and smooth surface of the particles. All the prepared formulations were found to be stable at varying temperatures.

Keywords: drug delivery, ocular delivery, polymeric nanoparticles, loteprednol etabonate

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2140 Development of Lipid Architectonics for Improving Efficacy and Ameliorating the Oral Bioavailability of Elvitegravir

Authors: Bushra Nabi, Saleha Rehman, Sanjula Baboota, Javed Ali

Abstract:

Aim: The objective of research undertaken is analytical method validation (HPLC method) of an anti-HIV drug Elvitegravir (EVG). Additionally carrying out the forced degradation studies of the drug under different stress conditions to determine its stability. It is envisaged in order to determine the suitable technique for drug estimation, which would be employed in further research. Furthermore, comparative pharmacokinetic profile of the drug from lipid architectonics and drug suspension would be obtained post oral administration. Method: Lipid Architectonics (LA) of EVR was formulated using probe sonication technique and optimized using QbD (Box-Behnken design). For the estimation of drug during further analysis HPLC method has been validation on the parameters (Linearity, Precision, Accuracy, Robustness) and Limit of Detection (LOD) and Limit of Quantification (LOQ) has been determined. Furthermore, HPLC quantification of forced degradation studies was carried out under different stress conditions (acid induced, base induced, oxidative, photolytic and thermal). For pharmacokinetic (PK) study, Albino Wistar rats were used weighing between 200-250g. Different formulations were given per oral route, and blood was collected at designated time intervals. A plasma concentration profile over time was plotted from which the following parameters were determined:

Keywords: AIDS, Elvitegravir, HPLC, nanostructured lipid carriers, pharmacokinetics

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2139 Studies on Modified Zinc Oxide Nanoparticles as Potential Drug Carrier

Authors: Jolanta Pulit-Prociak, Olga Dlugosz, Marcin Banach

Abstract:

The toxicity of bare zinc oxide nanoparticles used as drug carriers may be the result of releasing zinc ions. Thus, zinc oxide nanoparticles modified with galactose were obtained. The process of their formation was conducted in the microwave field. The physicochemical properties of the obtained products were studied. The size and electrokinetic potential were defined by using dynamic light scattering technique. The crystalline properties were assessed by X-ray diffractometry. In order to confirm the formation of the desired products, Fourier-transform infrared spectroscopy was used. The releasing of zinc ions from the prepared products when comparing to the bare oxide was analyzed. It was found out that modification of zinc oxide nanoparticles with galactose limits the releasing of zinc ions which are responsible for the toxic effect of the whole carrier-drug conjugate.

Keywords: nanomaterials, zinc oxide, drug delivery system, toxicity

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2138 Treatment of Drug-Induced Oral Ulceration with Hyaluronic Acid Gel: A Case Report

Authors: Meltem Koray, Arda Ozgon, Duygu Ofluoglu, Mehmet Yaltirik

Abstract:

Oral ulcerations can be seen as a side effect of different drugs. These ulcers usually appear within a few weeks following drug treatment. In most of cases, these ulcers resist to conventional treatments, such as anesthetics, antiseptics, anti-inflammatory agents, cauterization, topical tetracycline and corticosteroid treatment. The diagnosis is usually difficult, especially in patients receiving multiple drug therapies. Hyaluronan or hyaluronic acid (HA) is a biomaterial that has been introduced as an alternative approach to enhance wound healing and also used for oral ulcer treatment. The aim of this report is to present the treatment of drug-induced oral ulceration on maxillary mucosa with HA gel. 60-year-old male patient was referred to Department of Oral and Maxillofacial Surgery complaining of oral ulcerations during few weeks. He had received chemotherapy and radiotherapy in 2014 with the diagnosis of nasopharyngeal carcinoma, and he has accompanying systemic diseases such as; cardiological, neurological diseases and gout. He is medicated with Escitalopram (Cipralex® 20mg), Quetiapine (Seroquel® 100mg), Mirtazapine (Zestat® 15mg), Acetylsalicylic acid (Coraspin® 100mg), Ramipril-hydrochlorothiazide (Delix® 2.5mg), Theophylline anhydrous (Teokap Sr® 200mg), Colchicine (Colchicum Dispert® 0.5mg), Spironolactone (Aldactone® 100mg), Levothyroxine sodium (Levotiron® 50mg). He had painful oral ulceration on the right side of maxillary mucosa. The diagnosis was 'drug-induced oral ulceration' and HA oral gel (Aftamed® Oral gel) was prescribed 3 times a day for 2 weeks. Complete healing was achieved within 3 weeks without any side effect and discomfort. We suggest that HA oral gel is a potentially useful local drug which can be an alternative for management of drug-induced oral ulcerations.

Keywords: drug-induced, hyaluronic acid, oral ulceration, maxillary mucosa

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2137 Design, Development and Evaluation of Ketoconazole Loaded Nanosponges in Hydrogel for the Management of Topical Fungal Infections

Authors: Nagasamy Venkatesh Dhandapani

Abstract:

This work aims at investigating the use of β-Cyclodextrin as a cross linker, in an attempt to formulate nanosponges containing ketoconazole. The nanosponges were prepared by cross-linking method. The excipients used in this study did not alter the physicochemical properties of a drug as revealed by FTIR spectroscopy. Studies on various formulation variables revealed that all the variables are inter-related with the formulation. The ideal batch among the formulation was selected based on the higher entrapment efficiency and drug loading. The in vitro release studies of ketoconazole nanosponges in hydrogel exhibited a sustained release over a period of 24 hours. Mathematical analysis of drug release from the formulation followed non-Fickian diffusion obeying first order kinetics. The anti-fungal activity of the formulation exhibited better zone of inhibition when compared to pure drug (ketoconazole) against Tinea corporis.

Keywords: nanosponges, beta-cyclodextrin, ketoconazole, tinea corporis

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2136 Design and Development of Buccal Delivery System for Atenolol Tablets by Using Different Bioadhesive Polymers

Authors: Venkatalakshmi Ranganathan, Ong Hsin Ju, Tan Yinn Ming, Lim Kien Sin, Wong Man Ting, Venkata Srikanth Meka

Abstract:

The mucoadhesive buccal tablet is an oral drug delivery system which attached to the buccal surface for direct drug absorption into the systemic circulation and the unidirectional drug release is ensured by formulating a hydrophobic backing layer. The objective of present study was to formulate mucoadhesive atenolol bilayer buccal tablets by using sodium alginate, hydroxyethyl cellulose, and xanthan gum as mucoadhesive polymer and the technique applied was direct compression method. Ethyl cellulose was used as backing layer of the tablet. FTIR and DSC analysis were carried out to identify the drug polymer interactions. The prepared tablets were evaluated for physicochemical parameters, ex vivo mucoadhesion time and in-vitro drug release. The formulated tablets showed the average surface pH 6-7 which is favourable for oral mucosa. The formulation containing sodium alginate showed more than 90 % of drug release at the end of the 7 hours in vitro dissolution studies. The formulation containing xanthan gum showed more than 8 hours of mucoadhesion time and all formulation exhibited non fickian release kinetics. The present study indicates enormous potential of erodible mucoadhesive buccal tablet containing atenolol for systemic delivery with an added advantage of circumventing the hepatic first pass metabolism.

Keywords: atenolol, mucoadhesion, in vitro drug release, direct compression, ethyl cellulose

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2135 Solid Lipid Nanoparticles of Levamisole Hydrochloride

Authors: Surendra Agrawal, Pravina Gurjar, Supriya Bhide, Ram Gaud

Abstract:

Levamisole hydrochloride is a prominent anticancer drug in the treatment of colon cancer but resulted in toxic effects due poor bioavailability and poor cellular uptake by tumor cells. Levamisole is an unstable drug. Incorporation of this molecule in solid lipids may minimize their exposure to the aqueous environment and partly immobilize the drug molecules within the lipid matrix-both of which may protect the encapsulated drugs against degradation. The objectives of the study were to enhance bioavailability by sustaining drug release and to reduce the toxicities associated with the therapy. Solubility of the drug was determined in different lipids to select the components of Solid Lipid Nanoparticles (SLN). Pseudoternary phase diagrams were created using aqueous titration method. Formulations were subjected to particle size and stability evaluation to select the final test formulations which were characterized for average particle size, zeta potential, and in-vitro drug release and percentage transmittance to optimize the final formulation. SLN of Levamisole hydrochloride was prepared by Nanoprecipitation method. Glyceryl behenate (Compritol 888 ATO) was used as core comprising of Tween 80 as surfactant and Lecithin as co-surfactant in (1:1) ratio. Entrapment efficiency (EE) was found to be 45.89%. Particle size was found in the range of 100-600 nm. Zeta potential of the formulation was -17.0 mV revealing the stability of the product. In-vitro release study showed that 66 % drug released in 24 hours in pH 7.2 which represent that formulation can give controlled action at the intestinal environment. In pH 5.0 it showed 64% release indicating that it can even release drug in acidic environment of tumor cells. In conclusion, results revealed SLN to be a promising approach to sustain the drug release so as to increase bioavailability and cellular uptake of the drug with reduction in toxic effects as dose has been reduced with controlled delivery.

Keywords: SLN, nanoparticulate delivery of levamisole, pharmacy, pharmaceutical sciences

Procedia PDF Downloads 403