Search results for: drug chart

Authors: Jay Ananth

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The drug discovery process currently requires numerous years of clinical testing as well as money just for a single drug to earn FDA approval. For drugs that even make it this far in the process, there is a very slim chance of receiving FDA approval, resulting in detrimental hurdles to drug accessibility. To minimize these inefficiencies, numerous studies have implemented computational methods, although few computational investigations have focused on a crucial feature of drugs: lipophilicity. Lipophilicity is a physical attribute of a compound that measures its solubility in lipids and is a determinant of drug efficacy. This project leverages Artificial Intelligence to predict the impact of a drug’s lipophilicity on its performance by accounting for factors such as binding affinity and toxicity. The model predicted lipophilicity and binding affinity in the validation set with very high R² scores of 0.921 and 0.788, respectively, while also being applicable to a variety of target receptors. The results expressed a strong positive correlation between lipophilicity and both binding affinity and toxicity. The model helps in both drug development and discovery, providing every pharmaceutical company with recommended lipophilicity levels for drug candidates as well as a rapid assessment of early-stage drugs prior to any testing, eliminating significant amounts of time and resources currently restricting drug accessibility.

Keywords: drug discovery, lipophilicity, ligand-receptor interactions, machine learning, drug development

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Authors: Nishank Raisinghani

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Efficiently predicting drug response remains a challenge in the realm of drug discovery. To address this issue, we propose four model architectures that combine graphical representation with varying positions of multiheaded self-attention mechanisms. By leveraging two types of multi-omics data, transcriptomics and genomics, we create a comprehensive representation of target cells and enable drug response prediction in precision medicine. A majority of our architectures utilize multiple transformer models, one with a graph attention mechanism and the other with a multiheaded self-attention mechanism, to generate latent representations of both drug and omics data, respectively. Our model architectures apply an attention mechanism to both drug and multiomics data, with the goal of procuring more comprehensive latent representations. The latent representations are then concatenated and input into a fully connected network to predict the IC-50 score, a measure of cell drug response. We experiment with all four of these architectures and extract results from all of them. Our study greatly contributes to the future of drug discovery and precision medicine by looking to optimize the time and accuracy of drug response prediction.

Keywords: drug discovery, transformers, graph neural networks, multiomics

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Authors: Reza Ferdousi, Reza Safdari, Yadollah Omidi

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Drug-drug interactions (DDIs) are main cause of the adverse drug reactions and nature of the functional and molecular complexity of drugs behavior in human body make them hard to prevent and treat. With the aid of new technologies derived from mathematical and computational science the DDIs problems can be addressed with minimum cost and efforts. Market basket analysis is known as powerful method to identify co-occurrence of thing to discover patterns and frequency of the elements. In this research, we used market basket analysis to identify important bio-elements in DDIs occurrence. For this, we collected all known DDIs from DrugBank. The obtained data were analyzed by market basket analysis method. We investigated all drug-enzyme, drug-carrier, drug-transporter and drug-target associations. To determine the importance of the extracted bio-elements, extracted rules were evaluated in terms of confidence and support. Market basket analysis of the over 45,000 known DDIs reveals more than 300 important rules that can be used to identify DDIs, CYP 450 family were the most frequent shared bio-elements. We applied extracted rules over 2,000,000 unknown drug pairs that lead to discovery of more than 200,000 potential DDIs. Analysis of the underlying reason behind the DDI phenomena can help to predict and prevent DDI occurrence. Ranking of the extracted rules based on strangeness of them can be a supportive tool to predict the outcome of an unknown DDI.

Keywords: drug-drug interaction, market basket analysis, rule discovery, important bio-elements

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Authors: Arpa Petchsomrit, Namfa Sermkaew, Ruedeekorn Wiwattanapatapee

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Oil entrapped floating alginate beads of curcumin were developed and characterized. Cremophor EL, Cremophor RH and Tween 80 were utilized to improve the solubility of the drug. The oil-loaded floating gel beads prepared by emulsion gelation method contained sodium alginate, mineral oil and surfactant. The drug content and % encapsulation declined as the ratio of surfactant was increased. The release of curcumin from 1% alginate beads was significantly more than for the 2% alginate beads. The drug released from the beads containing 25% of tween 80 was about 70% while a higher drug release was observed with the beads containing Cremophor EL or Cremohor RH (approximately 90%). The developed floating beads of curcumin powder with surfactant provided a superior drug release than those without surfactant. Floating beads based on oil entrapment containing the drug solubilized in surfactants is a new delivery system to enhance the dissolution of poorly soluble drugs.

Keywords: alginate, curcumin, floating drug delivery, oil entrapped bead

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Authors: Mary Moner Botros Fanawel

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Many companies use the statistical tool named as statistical quality control, and which can have a high cost for the companies interested on these statistical tools. The evaluation of the quality of products and services is an important topic, but the reduction of the cost of the implantation of the statistical quality control also has important benefits for the companies. For this reason, it is important to implement a economic design for the various steps included into the statistical quality control. In this paper, we describe some relevant aspects related to the economic design of a quality control chart for the proportion of defective items. They are very important because the suggested issues can reduce the cost of implementing a quality control chart for the proportion of defective items. Note that the main purpose of this chart is to evaluate and control the proportion of defective items of a production process.

Keywords: model predictive control, hierarchical control structure, genetic algorithm, water quality with DBPs objectives proportion, type I error, economic plan, distribution function bootstrap control limit, p-value method, out-of-control signals, p-value, quality characteristics

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Authors: Romasa Qasim, G. M. Sayedur Rahman, Nahid Hasan, M. Shazzad Hosain

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Millions of people worldwide suffer from Hepatitis C, one of the fatal diseases. Interferon (IFN) and ribavirin are the available treatments for patients with Hepatitis C, but these treatments have their own side-effects. Our research focused on the development of an orally taken small molecule drug targeting the proteins in Hepatitis C Virus (HCV), which has lesser side effects. Our current study aims to the Pharmacophore based drug development of a specific small molecule anti-viral drug for Hepatitis C Virus (HCV). Drug designing using lab experimentation is not only costly but also it takes a lot of time to conduct such experimentation. Instead in this in silico study, we have used computer-aided techniques to propose a Pharmacophore-based anti-viral drug specific for the protein domains of the polyprotein present in the Hepatitis C Virus. This study has used homology modeling and ab initio modeling for protein 3D structure generation followed by pocket identification in the proteins. Drug-able ligands for the pockets were designed using de novo drug design method. For ligand design, pocket geometry is taken into account. Out of several generated ligands, a new Pharmacophore is proposed, specific for each of the protein domains of HCV.

Keywords: pharmacophore-based drug design, anti-viral drug, in-silico drug design, Hepatitis C virus (HCV)

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Authors: Donna L. Roberts

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2019 marked 23 years since Purdue Pharma launched its flagship drug, OxyContin, that unleashed an unprecedented epidemic touching both celebrities and common citizens, metropolitan, suburbia and rural areas and all levels of socioeconomic status. From rural Appalachia to East LA individuals, families and communities have been devastated by a trajectory of addiction that often began with the legitimate prescription of a pain killer for anything from a tooth extraction to a sports injury to recovery from surgery or chronic arthritis. Far from being a serendipitous progression of events, the proliferation of this new breed of 'miracle drug' was instead a carefully crafted marketing program aimed at both the medical community and common citizens. This research represents and in-depth investigation of the evolution of the marketing, distribution and promotion of prescription opioids by pharmaceutical companies and its relationship to the propagation of the opioid crisis. Specifically, key components of Purdue Pharma’s aggressive marketing campaign, including its bonus system and sales incentives, were analyzed in the context of the sociopolitical environment that essential created the proverbial 'perfect storm' for the changing manner in which pain is treated in the U.S. The analyses of these series of events clearly indicate their role in first, the increase in prescription of opioids for non-terminal pain relief and subsequently, the incidence of related addiction, overdose, and death. Through this examination of the conditions that facilitated and maintained this drug crisis, perhaps we can begin to chart a course toward its resolution.

Keywords: addiction, opioid, opioid crisis, Purdue Pharma

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Authors: V. Balamuralidhara

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The aim of the present work was to develop Paclitaxel loaded polyacrylamide grafted guar gum nanoparticles as pH responsive nanoparticle systems for targeting colon. The pH sensitive nanoparticles were prepared by modified ionotropic gelation technique. The prepared nanoparticles showed mean diameters in the range of 264±0.676 nm to 726±0.671nm, and a negative net charge 10.8 mV to 35.4mV. Fourier Transformed Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) studies suggested that there was no chemical interaction between drug and polymers. The encapsulation efficiency of the drug was found to be 40.92% to 48.14%. The suitability of the polyacrylamide grafted guar gum ERN’s for the release of Paclitaxel was studied by in vitro release at pH 1.2 and 7.4. It was observed that, there was no significant amount of drug release at gastric pH and 97.63% of drug release at pH 7.4 was obtained for optimized formulation F3 at the end of 12 hrs. In vivo drug targeting performance for the prepared optimized formulation (F3) and pure drug Paclitaxel was evaluated by HPLC. It was observed that the polyacrylamide grafted guar gum can be used to prepare nanoparticles for targeting the drug to the colon. The release performance was greatly affected by the materials used in ERN’s preparation, which allows maximum release at colon’s pH. It may be concluded that polyacrylamide grafted guar gum nanoparticles loaded with paclitaxel have desirable release responsive to specific pH. Hence it is a unique approach for colonic delivery of drug having appropriate site specificity and feasibility and controlled release of drug.

Keywords: colon targeting, polyacrylamide grafted guar gum nanoparticles, paclitaxel, nanoparticles

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Authors: Yi-Fan Lin, Peter P. Howley, Frank A. Tuyl

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Quality measurement and reporting systems are used in healthcare internationally. In Australia, the Australian Council on Healthcare Standards records and reports hundreds of clinical indicators (CIs) nationally across the healthcare system. These CIs are measures of performance in the clinical setting, and are used as a screening tool to help assess whether a standard of care is being met. Existing analysis and reporting of these CIs incorporate Bayesian methods to address sampling variation; however, such assessments are retrospective in nature, reporting upon the previous six or twelve months of data. The use of Bayesian methods within statistical process control for monitoring systems is an important pursuit to support more timely decision-making. Our research has developed and assessed a new graphical monitoring tool, similar to a control chart, based on the beta-binomial posterior predictive (BBPP) distribution to facilitate the real-time assessment of health care organizational performance via CIs. The BBPP charts have been compared with the traditional Bernoulli CUSUM (BC) chart by simulation. The more traditional “central” and “highest posterior density” (HPD) interval approaches were each considered to define the limits, and the multiple charts were compared via in-control and out-of-control average run lengths (ARLs), assuming that the parameter representing the underlying CI rate (proportion of cases with an event of interest) required estimation. Preliminary results have identified that the BBPP chart with HPD-based control limits provides better out-of-control run length performance than the central interval-based and BC charts. Further, the BC chart’s performance may be improved by using Bayesian parameter estimation of the underlying CI rate.

Keywords: average run length (ARL), bernoulli cusum (BC) chart, beta binomial posterior predictive (BBPP) distribution, clinical indicator (CI), healthcare organization (HCO), highest posterior density (HPD) interval

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Authors: M. Rahimnejad, B. Vahidi, B. Ebrahimi Hoseinzadeh, F. Yazdian, P. Motamed Fath, R. Jamjah

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In this study, we developed and simulated nano-drug delivery systems efficacy in compare to free drug prescription. Computational models can be utilized to accelerate experimental steps and control the experiments high cost. Molecular dynamics simulation (MDS), in particular NAMD was utilized to better understand the anti-cancer drug interaction with cell membrane model. Paclitaxel (PTX) and dipalmitoylphosphatidylcholine (DPPC) were selected for the drug molecule and as a natural phospholipid nanocarrier, respectively. This work focused on two important interaction parameters between molecules in terms of center of mass (COM) and van der Waals interaction energy. Furthermore, we compared the simulation results of the PTX interaction with the cell membrane and the interaction of DPPC as a nanocarrier loaded by the drug with the cell membrane. The molecular dynamic analysis resulted in low energy between the nanocarrier and the cell membrane as well as significant decrease of COM amount in the nanocarrier and the cell membrane system during the interaction. Thus, the drug vehicle showed notably better interaction with the cell membrane in compared to free drug interaction with the cell membrane.

Keywords: anti-cancer drug, center of mass, interaction energy, molecular dynamics simulation, nanocarrier

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Authors: D. R. Rama Brahma Reddy, A. Vijaya Sarada Reddy

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Nanoparticles represent a promising drug delivery system of controlled and targeted drug release. They are specially designed to release the drug in the vicinity of target tissue. The aim of this study was to prepare and evaluate polymethacrylic acid nanoparticles containing Zidovudine in different drug to polymer ratio by nanoprecipitation method. SEM indicated that nanoparticles have a discrete spherical structure without aggregation. The average particle size was found to be 120 ± 0.02 - 420 ± 0.05 nm. The particle size of the nanoparticles was gradually increased with increase in the proportion of polymethacrylic acid polymer. The drug content of the nanoparticles was increasing on increasing polymer concentration up to a particular concentration. No appreciable difference was observed in the extent of degradation of product during 60 days in which, nanoparticles were stored at various temperatures. FT-IR studies indicated that there was no chemical interaction between drug and polymer and stability of drug. The in-vitro release behavior from all the drug loaded batches was found to be zero order and provided sustained release over a period of 24 h. The developed formulation overcome and alleviates the drawbacks and limitations of Zidovudine sustained release formulations and could possibility be advantageous in terms of increased bio availability of Zidovudine.

Keywords: nanoparticles, zidovudine, biodegradable, polymethacrylic acid

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Authors: Stanely Nsubuga

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Background In Uganda, injection drug use is a growing but less studied problem. Preventing the transition to injection drug use may help prevent blood-borne viral transmission, but little is known about when and how people transition to injection drug use. A greater understanding of this transition process may aid in the country’s efforts to prevent the continued growth of injection drug use, HIV, and hepatitis C Virus (HCV) infection among people who inject drugs (PWID). Methods Using a rapid situation assessment framework, we conducted semi-structured interviews among 125 PWID (102 males and 23 females)—recruited through outreach and snow-ball sampling. Participants were interviewed about their experiences on when and how they transitioned into injection drug use and these issues were also discussed in 12 focus groups held with the participants. Results All the study participants started their drug use career with non-injecting forms including chewing, smoking, and sniffing before transitioning to injecting. Transitioning was generally described as a peer-driven and socially learnt behavior. The participants’ social networks and accessibility to injectable drugs on the market and among close friends influenced the time lag between first regular drug use and first injecting—which took an average of 4.5 years. By the age of 24, at least 81.6% (95.7% for females and 78.4% for males) had transitioned into injecting. Over 84.8% shared injecting equipment during their first injection, 47.2% started injecting because a close friend was already injecting, 26.4% desired to achieve a greater “high” (26.4%) which could reflect drug-tolerance, and 12% out of curiosity.

Keywords: People who Use Drugs, transition, injection drug use, Uganda

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Authors: Maryam Hamedanlou, Shahla Hajializadeh

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The transdermal drug delivery system is one of the types of novel drug delivery system that the drug is absorbed into the skin. The major considerations for designing and producing transdermal patch are small size, suitable drug release and good adhering. In this study, drug-in-adhesive transdermal patch contained non-steroidal anti-inflammatory ketoprofen is prepared. Also, the effect of non-woven fabric and plastic backing layers on adhesion properties is assessed. The results of the test, demonstrated the use of plastic backing layer increases tack and peel rather than non-woven fabric type. The balance tack with plastic backing layer patch is 6.7 (N/mm2), and the fabric one is 3.8 (N/mm2), and their peel is 9.2 (N/25mm) and 8.3 (N/25mm) by arrangement.

Keywords: transdermal drug delivery system, single layer patch of ketoprofen, plastic layer, fabric backing layer

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Authors: Ran Etgar

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The process of rounding off measurements in continuous variables is commonly encountered. Although it usually has minor effects, sometimes it can lead to poor outcomes in statistical process control using X̄ chart. The traditional control limits can cause incorrect conclusions if applied carelessly. This study looks into the limitations of classical control limits, particularly the impact of asymmetry. An approach to determining the distribution function of the measured parameter ȳ is presented, resulting in a more precise method to establish the upper and lower control limits. The proposed method, while slightly more complex than Shewhart's original idea, is still user-friendly and accurate and only requires the use of two straightforward tables.

Keywords: SPC, round-off data, control limit, rounding error

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Authors: Yong Ren, Yaping Zhang

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A numerical model has been developed to investigate the thermally triggered release kinetics for drug delivery using phase change material as shell of microcapsules. Biocompatible material n-Eicosane is used as demonstration. PCM shell of microcapsule will remain in solid form after the drug is taken, so the drug will be encapsulated by the shell, and will not be released until the target body part of lesion is exposed to external heat source, which will thermally trigger the release kinetics, leading to solid-to-liquid phase change. The findings can lead to better understanding on the key effects influencing the phase change process for drug delivery applications. The facile approach to release drug from core/shell structure of microcapsule can be well integrated with organic solvent free fabrication of microcapsules, using double emulsion as template in microfluidic aqueous two phase system.

Keywords: phase change material, drug release kinetics, double emulsion, microfluidics

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Authors: Lali Khurtsia, Vano Tsertsvadze

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Georgian drug policy is directed to reduce the supply of drugs. Retrospective analysis has shown that law enforcement activities have been followed by the expulsion of particular injecting drugs. The demand remains unchanged and drugs are substituted by the hand-made, even more dangerous homemade drugs entered the market. To find out expected new trends on the Georgian drug market, qualitative study was conducted with Georgian drug users to determine drug supply routes. It turned out that drug suppliers and consumers for safety reasons and to protect their anonymity, use Skype to make deals. IT in illegal drug trade is even more sophisticated in the worldwide. Trading with Bitcoins in the Darknet ensures high confidentiality of money transactions and the safe circulation of drugs. In 2014 largest Bitcoin mining enterprise in the world was built in Georgia. We argue that the use of Bitcoins and Darknet by Georgian drug consumers and suppliers will be an incentive to response adequately to the government's policy of restricting supply in order to satisfy market demand for drugs.

Keywords: bitcoin, darknet, drugs, policy

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Authors: Imran Khan Pathan, Anil Bhandari, Peeyush K. Sharma, Rakesh K. Patel, Suresh Purohit

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Floating tablets of Marichyadi Vati were developed with an aim to prolong its gastric residence time and increase the bioavailability of drug. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by wet granulation technique, using HPMC E50 LV act as Matrixing agent, Carbopol as floating enhancer, microcrystalline cellulose as binder, sodium bi carbonate as effervescent agent with other excipients. The simplex lattice design was used for selection of variables for tablets formulation. Formulation was optimized on the basis of floating time and in vitro drug release. The results showed that the floating lag time for optimized formulation was found to be 61 second with about 97.32 % of total drug release within 3 hours. The in vitro release profiles of drug from the formulation could be best expressed zero order with highest linearity r2 = 0.9943. It was concluded that the gastroretentive drug delivery system can be developed for Marichyadi Vati containing piperine to increase the residence time of the drug in the stomach and thereby increasing bioavailability.

Keywords: piperine, Marichyadi Vati, gastroretentive drug delivery, floating tablet

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Authors: Mina Boroujerdi, Javad Tavakoli

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Hydrogels are extensively studied as matrices for the controlled release of drugs. To evaluate the mobility of embedded molecules, these drug delivery systems are usually characterized by release studies. In this contribution, an electronic device for swelling pressure measurement during drug release from hydrogel network was developed. Also, poly acrylic acid micro particles were prepared for prolonged and sustained controlled acetaminophen release. Effect of swelling pressure on drug release from micro particles studied under different environment pH in order to predict release profile in gastro-intestine medium. Swelling ratio and swelling pressure were measured in different pH.

Keywords: swelling pressure, drug delivery, hydrogel, polyelectrolyte

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Authors: Shideh Mohseni Movahed, Mansoureh Safari

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Intelligent drug delivery systems (IDDS) are innovative technological innovations and clinical way to advance current treatments. These systems differ in technique of therapeutic administration, intricacy, materials and patient compliance to address numerous clinical conditions that require different pharmacological therapies. IDDS capable of releasing an active molecule at the proper site and at a amount that adjusts in response to the progression of the disease or to certain functions/biorhythms of the organism is particularly appealing. In this paper, we describe the most recent advances in the development of intelligent drug delivery systems.

Keywords: drug delivery systems, IDDS, medicine, health

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Authors: Fanjun Zhou

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In today's drug-ridden society, drug injection is gradually becoming more popular and has hidden danger to IDUs (injection drug users) such as infectious diseases. According to reports, 67% of IDUs reported improper disposal at some point over the prior 30 days, leading to a proliferation of injection needles on the streets. In recent years, the number of cases of children or ordinary people unintentionally picking up needles have increased. Various needle remover inventions have begun to surface, but the existing ones are either expensive, unportable, or risky for IDUs. In order to effectively alleviate the proliferation of drug injection needles and improve the invention of needle removers, a miniature portable needle remover and receptacle is invented. The device for capturing and storing syringe needles contains an upper lid portion mounted tightly onto the lower box portion through an interlock system on the opposing sides of the device with a breaking-twisting mechanism to remove the needle. The invention is intended to be affordable to the general public, safe enough for IDUs to use, reliable enough not to harm others, and effective in breaking needles from the syringe. This report is conducted in the hope of spreading awareness of the dangers of drug injection and to provide a way to mitigate this drug rampant situation.

Keywords: needle remover, drug injection, injection drug users, portable, receptacle

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Authors: M. A. Khanday, Aasma Rafiq, Khalid Nazir

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This paper is an attempt to establish the mathematical models to understand the distribution of drug administration in the human body through oral and intravenous routes. Three models were formulated based on diffusion process using Fick’s principle and the law of mass action. The rate constants governing the law of mass action were used on the basis of the drug efficacy at different interfaces. The Laplace transform and eigenvalue methods were used to obtain the solution of the ordinary differential equations concerning the rate of change of concentration in different compartments viz. blood and tissue medium. The drug concentration in the different compartments has been computed using numerical parameters. The results illustrate the variation of drug concentration with respect to time using MATLAB software. It has been observed from the results that the drug concentration decreases in the first compartment and gradually increases in other subsequent compartments.

Keywords: Laplace transform, diffusion, eigenvalue method, mathematical model

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Authors: K. S. Hemant Yadav, H. G. Shivakumar

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The present study investigation was to prepare and evaluate the mucoadhesive multi-particulate system for nasal drug delivery of anti-histaminic drug. Ebastine was chosen as the model drug. Drug loaded nanoparticles of Ebastine were prepared by ionic gelation method using chitosan as polymer using the drug-polymer weight ratios 1:1, 1:2, 1:3. Sodium tripolyphosphate (STPP) was used as the cross-linking agent in the range of 0.5 and 0.7% w/v. FTIR and DSC studies indicated that no chemical interaction occurred between the drug and polymers. Particle size ranged from 169 to 500 nm. The drug loading and entrapment efficiency was found to increase with increase in chitosan concentration and decreased with increase in poloxamer 407 concentration. The results of in vitro mucoadhesion carried out showed that all the prepared formulation had good mucoadhesive property and mucoadhesion increases with increase in the concentration of chitosan. The in vitro release pattern of all the formulations was observed to be in a biphasic manner characterized by slight burst effect followed by a slow release. By the end of 8 hrs, formulation F6 showed a release of only 86.9% which explains its sustained behaviour. The ex-vivo permeation of the pure drug ebastine was rapid than the optimized formulation(F6) indicating the capability of the chitosan polymer to control drug permeation rate through the sheep nasal mucosa. The results indicated that the mucoadhesive nanoparticulate system can be used for the nasal delivery of antihistaminic drugs in an effective manner.

Keywords: nasal, nanoparticles, ebastine, anti-histaminic drug, mucoadhesive multi-particulate system

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Authors: Blessing A. Aderibigbe

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Combination therapy is a treatment approach that is used to prevent the emergence of drug resistance. This approach is used for the treatment of many chronic and infectious diseases. Potentiating agents are currently explored in combination therapy, resulting in excellent therapeutic outcomes. Breast cancer and malaria are two chronic conditions responsible globally for high death rates. In this research, a class of polymer-drug conjugates containing potentiating agents with either antimalarial or anticancer drugs were prepared by Michael Addition Polymerization reaction and ring-opening polymerization reaction. Conjugation of potentiating agents with bioactive compounds into the polymers resulted in conjugates with good water solubility, highly selective and non-toxic. In vitro cytotoxicity and in vitro antiplasmodial evaluation on the conjugates revealed that the conjugates were more effective when compared to the free drugs. The drug release studies further showed that the release profile of the drugs from the conjugates was sustained. The findings revealed the potential of polymer-drug conjugates to overcome drug toxicity and drug resistance, which is common with the currently used antimalarial and anticancer drugs.

Keywords: anticancer, antimalarials, combination therapy, polymer-drug conjugates

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Authors: Weitao Zhou, Qing Wang, Jianxin He, Shizhong Cui

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Mesoporous Tussah silk fibroin (TSF) spheres were fabricated via the self-assembly of TSF molecules in aqueous solutions. The results showed that TSF particles were approximately three-dimensional spheres with the diameter ranging from 500nm to 6μm without adherence. More importantly, the surface morphology is mesoporous structure with nano-pores of 20nm - 200nm in size. Fourier transform infrared (FT-IR) and X-ray diffraction (XRD) studies demonstrated that mesoporous TSF spheres mainly contained beta-sheet conformation (44.1 %) as well as slight amounts of random coil (13.2 %). Drug release test was performed with 5-fluorouracil (5-Fu) as a model drug and the result indicated the mesoporous TSF microspheres had a good capacity of sustained drug release. It is expected that these stable and high-crystallinity mesoporous TSF sphere produced without organic solvents, which have significantly improved drug release properties, is a very promising material for controlled gene medicines delivery.

Keywords: Tussah silk fibroin, porous materials, microsphere, drug release

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Authors: Abraham J. Domb

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Nearly every eye disorder and treatment of post operated eyes evolve around ocular drug delivery. Most ocular diseases are treated with repeated topical applications administered as eye drops. Various attempts have been made to improve drug bioavailability by increasing both the retention of the drug in the pre-corneal area and the penetration of the drug through the cornea. However, currently marketed products are associated with vision blurring, irritability, patient discomfort, toxicity, low drug bioavailability, manufacturing difficulties and inadequate aqueous stability. It has been suggested to use iontophoresis for the non-invasive delivery of drugs. The iontophoretic device is composed of a control panel, two electrodes, a cylindrical well for the insertion of a disposable hydrogel, and a disposable hydrogel pellet. The drug-loaded hydrogel is attached to a cylindrical well at the edge of the electrode of the device and placed onto the eye. The device applies a variable electrical current that can vary from 0.1 mA to 1.5 mA for pre-set periods from 10 seconds to 300 seconds. The iontophoretic device developed in the lab was found to be effective in the delivery of the drugs: gentamicin, water-soluble steroids, and various anticancer agents. When testing in rabbits for safety, the device was considered to be non-toxic and effective.

Keywords: iontophoresis, eye disorder, drug delivery, hydrogel

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Authors: Jasper Kevin C. Dionisio, Denise Mae M. Unsay

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In a manufacturing firm, controlling the process ensures that optimum efficiency, productivity, and quality in an organization are achieved. An operation with no standardized procedure yields a poor productivity, inefficiency, and an out of control process. This study focuses on controlling the small intestine processing of a chicken dressing plant through the use of Statistical Process Control (SPC). Since the operation does not employ a standard procedure and does not have an established standard time, the process through the assessment of the observed time of the overall operation of small intestine processing, through the use of X-Bar R Control Chart, is found to be out of control. In the solution of this problem, the researchers conduct a motion and time study aiming to establish a standard procedure for the operation. The normal operator was picked through the use of Westinghouse Rating System. Instead of utilizing the traditional motion and time study, the researchers used the X-Bar R Control Chart in determining the process average of the process that is used for establishing the standard time. The observed time of the normal operator was noted and plotted to the X-Bar R Control Chart. Out of control points that are due to assignable cause were removed and the process average, or the average time the normal operator conducted the process, which was already in control and free form any outliers, was obtained. The process average was then used in determining the standard time of small intestine processing. As a recommendation, the researchers suggest the implementation of the standard time established which is with consonance to the standard procedure which was adopted from the normal operator. With that recommendation, the whole operation will induce a 45.54 % increase in their productivity.

Keywords: motion and time study, process controlling, statistical process control, X-Bar R Control chart

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Authors: Dwarakanadha Reddy Peram, D. Swarnalatha, C. Gopinath

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The main aim of this research work was to design and development characterization of Pioglitazone transdermal drug delivery system by using various polymers such as Olibanum with different concentration by solvent evaporation technique. The prepared formulations were evaluated for different physicochemical characteristics like thickness, folding endurance, drug content, percentage moisture absorption, percentage moisture loss, percentage elongation break test and weight uniformity. The diffusion studies were performed by using modified Franz diffusion cells. The result of dissolution studies shows that formulation, F3 (Olibanum with 50 mg) showed maximum release of 99.95 % in 12hrs, whereas F1 (Olibanum and EC backing membrane) showed minimum release of 93.65% in 12 hr. Based on the drug release and physicochemical values obtained the formulation F3 is considered as an optimized formulation which shows higher percentage of drug release of 99.95 % in 12 hr. The developed transdermal patches increase the therapeutic efficacy and reduced toxic effect of pioglitazone.

Keywords: pioglitazone, olibanum, transdermal drug delivery system, drug release percantage

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Authors: G. Agrawal, R. Agrawal, A. Pich

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The pH and temperature responsive biodegradable poly(N-vinylcaprolactam) (PVCL) based microgels functionalized with itaconic acid (IA) units are prepared via precipitation polymerization for drug delivery applications. Volume phase transition temperature (VPTT) of the obtained microgels is influenced by both IA content and pH of the surrounding medium. The developed microgels can be degraded under acidic conditions due to the presence of hydrazone based crosslinking points inside the microgel network. The microgel particles are able to effectively encapsulate doxorubicin (DOX) drug and exhibit low drug leakage under physiological conditions. At low pH, rapid DOX release is observed due to the changes in electrostatic interactions along with the degradation of particles. The results of the cytotoxicity assay further display that the DOX-loaded microgel exhibit effective antitumor activity against HeLa cells demonstrating their great potential as drug delivery carriers for cancer therapy.

Keywords: degradable, drug delivery, hydrazone linkages, microgels, responsive

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Authors: Vishal Kumar Gupta

Abstract:

Purpose: This study has been undertaken to develop novel pH sensitive interpenetrating network hydrogel beads. Methods: The pH sensitive PAAM-g-Guar gum copolymer was synthesized by free radical polymerization followed by alkaline hydrolysis. Beads of guar gum-grafted-polyacrylamide and sodium Carboxy methyl cellulose (Na CMC) loaded with Pantoprazole sodium were prepared and evaluated for pH sensitivity, swelling properties, drug entrapment efficiency and in vitro drug release characteristics. Seven formulations were prepared for the drug with varying polymer and cross linker concentrations. Results: The grafting and alkaline hydrolysis reactions were confirmed by FT-IR spectroscopy. Differential scanning calorimetry was carried out to know the compatibility of encapsulated drug with the polymers. Scanning electron microscopic study revealed that the IPN beads were spherical. The entrapment efficiency was found to be in the range of 85-92%. Particle size analysis was carried out by optical microscopy. As the pH of the medium was changed from 1.2 to 7.4, a considerable increase in swelling was observed for all beads. Increase in the copolymer concentration showed sustained the drug release up to 12 hrs. Drug release from the beads followed super case II transport mechanism. Conclusion: It was concluded that guar gum-acrylamide beads, cross-linked with aluminum chloride offer an opportunity for controlled drug release of pantoprazole sodium.

Keywords: IPN, hydrogels, DSC, SEM

Procedia PDF Downloads 250

Authors: Fateme Nokhodchi Bonab

Abstract:

Studies related to magnetic resonance imaging (MRI) and drug delivery are reviewed in this study to demonstrate the role of transport theory in porous media in facilitating advances in biomedical applications. Diffusion processes are believed to be important in many therapeutic modalities such as: B. Delivery of drugs to the brain. We analyse the progress in the development of diffusion equations using the local volume average method and the evaluation of applications related to diffusion equations. Torsion and porosity have significant effects on diffusive transport. In this study, various relevant models of torsion are presented and mathematical modeling of drug release from biodegradable delivery systems is analysed. In this study, a new model of drug release kinetics from porous biodegradable polymeric microspheres under bulk and surface erosion of the polymer matrix is presented. Solute drug diffusion, drug dissolution from the solid phase, and polymer matrix erosion have been found to play a central role in controlling the overall drug release process. This work paves the way for MRI and drug delivery researchers to develop comprehensive models based on porous media theory that use fewer assumptions compared to other approaches.

Keywords: MRI, porous media, drug delivery, biomedical applications

Procedia PDF Downloads 57