Search results for: drug users
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 4451

Search results for: drug users

4211 Cellular Uptake and Endocytosis of Doxorubicin Loaded Methoxy Poly (Ethylene Glycol)-Block-Poly (Glutamic Acid) [DOX/mPEG-b-PLG] Nanoparticles against Human Breast Cancer Cell Lines

Authors: Zaheer Ahmad, Afzal Shah

Abstract:

pH responsive block copolymers consist of mPEG and glutamic acid units were syntheiszed in different formulations. The synthesized polymers were structurally investigated. Doxorubicin Hydrocholide (DOX-HCl) as a chemotherapy medication for the treatment of cancer was selected. DOX-HCl was loaded and their drug loading content and drug loading efficiency were determined. The nanocarriers were obtained in small size, well shaped and slightly negative surface charge. The release study was carried out both at pH 7.4 and 5.5 and it was revealed that the release was sustained and in controlled manner and there was no initial burst release. The in vitro release study was further carried out for different formulations with different glutamic acid moieties. Time dependent cell proliferation inhibition of the free drug and drug loaded nanoparticles against human breast cancer cell lines MCF-7 and Zr-75-30 was observed. Cellular uptakes and endocytosis were investigated by confocal laser scanning microscopy (CLSM) and flow cytometery. The biocompatibility, optimum size, shape and surface charge of the developed nanoparticles make the nanoparticles an efficient drug delivery carrier.

Keywords: doxorubicin, glutamic acid, cell proliferation inhibition, breast cancer cell

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4210 Development of Agomelatine Loaded Proliposomal Powders for Improved Intestinal Permeation: Effect of Surface Charge

Authors: Rajasekhar Reddy Poonuru, Anusha Parnem

Abstract:

Purpose: To formulate proliposome powder of agomelatine, an antipsychotic drug, and to evaluate physicochemical, in vitro characters and effect of surface charge on ex vivo intestinal permeation. Methods: Film deposition technique was employed to develop proliposomal powders of agomelatin with varying molar ratios of lipid Hydro Soy PC L-α-phosphatidylcholine (HSPC) and cholesterol with fixed sum of drug. With the aim to derive free flowing and stable proliposome powder, fluid retention potential of various carriers was examined. Liposome formation and number of vesicles formed for per mm3 up on hydration, vesicle size, and entrapment efficiency was assessed to deduce an optimized formulation. Sodium cholate added to optimized formulation to induce surface charge on formed vesicles. Solid-state characterization (FTIR, DSC, and XRD) was performed with the intention to assess native crystalline and chemical behavior of drug. The in vitro dissolution test of optimized formulation along with pure drug was evaluated to estimate dissolution efficiency (DE) and relative dissolution rate (RDR). Effective permeability co-efficient (Peff(rat)) in rat and enhancement ratio (ER) of drug from formulation and pure drug dispersion were calculated from ex vivo permeation studies in rat ileum. Results: Proliposomal powder formulated with equimolar ratio of HSPC and cholesterol ensued in higher no. of vesicles (3.95) with 90% drug entrapment up on hydration. Neusilin UFL2 was elected as carrier because of its high fluid retention potential (4.5) and good flow properties. Proliposome powder exhibited augmentation in DE (60.3 ±3.34) and RDR (21.2±01.02) of agomelation over pure drug. Solid state characterization studies demonstrated the transformation of native crystalline form of drug to amorphous and/or molecular state, which was in correlation with results obtained from in vitro dissolution test. The elevated Peff(rat) of 46.5×10-4 cm/sec and ER of 2.65 of drug from charge induced proliposome formulation with respect to pure drug dispersion was assessed from ex vivo intestinal permeation studies executed in ileum of wistar rats. Conclusion: Improved physicochemical characters and ex vivo intestinal permeation of drug from charge induced proliposome powder with Neusilin UFL2 unravels the potentiality of this system in enhancing oral delivery of agomelatin.

Keywords: agomelatin, proliposome, sodium cholate, neusilin

Procedia PDF Downloads 136
4209 Effectiveness of Group Therapy Based on Acceptance and Commitment on Self-Criticism and Coping Mechanism in People with Addiction

Authors: Mohamad Reza Khodabakhsh

Abstract:

Drug use and addiction are major biological, psychological, and social problems. In drug abuse treatment, it is important to pay attention to personality problems and coping methods of patients. Today, the third-wave treatments in psychotherapy emphasize people's awareness and acceptance of feelings and emotions, cognitions, and behaviors instead of challenging cognitions. For this reason, this research was conducted with the aim of investigating the effectiveness of group therapy based on acceptance and commitment to self-criticism and coping strategies of people with drug use disorder. This research was a quasi-experimental type of research (pre-test-post-test design with an unequal control group), and the statistical population of this research included all men with drug use disorder in Mashhad, 174 of whom among the 75 people eligible for this research, 30 of them were selected by available sampling method and randomly assigned to two experimental and control groups. In this research, Gilbert's self-criticism scale was used to measure self-criticism, and Andler and Barker's coping strategies questionnaire was used to measure coping strategies. Therapeutic intervention (treatment based on acceptance and commitment) was performed on the experimental group for eight sessions of 90 minutes, and then post-tests were taken from both groups, and multivariate analysis of covariance (MANCOVA) was used to analyze the data. The results showed that treatment based on acceptance and commitment significantly reduced self-criticism and improved coping strategies used by patients with drug use disorder (p>0.01). Therefore, treatment based on acceptance and commitment has been effective in reducing self-criticism and improving the coping strategies of patients with drug use disorder due to teaching clients to accept thoughts and conditions.

Keywords: treatment based on acceptance and commitment, self-criticism, coping strategies, addiction

Procedia PDF Downloads 88
4208 The importance of Clinical Pharmacy and Computer Aided Drug Design

Authors: Peter Edwar Mortada Nasif

Abstract:

The use of CAD (Computer Aided Design) technology is ubiquitous in the architecture, engineering and construction (AEC) industry. This has led to its inclusion in the curriculum of architecture schools in Nigeria as an important part of the training module. This article examines the ethical issues involved in implementing CAD (Computer Aided Design) content into the architectural education curriculum. Using existing literature, this study begins with the benefits of integrating CAD into architectural education and the responsibilities of different stakeholders in the implementation process. It also examines issues related to the negative use of information technology and the perceived negative impact of CAD use on design creativity. Using a survey method, data from the architecture department of Chukwuemeka Odumegwu Ojukwu Uli University was collected to serve as a case study on how the issues raised were being addressed. The article draws conclusions on what ensures successful ethical implementation. Millions of people around the world suffer from hepatitis C, one of the world's deadliest diseases. Interferon (IFN) is treatment options for patients with hepatitis C, but these treatments have their side effects. Our research focused on developing an oral small molecule drug that targets hepatitis C virus (HCV) proteins and has fewer side effects. Our current study aims to develop a drug based on a small molecule antiviral drug specific for the hepatitis C virus (HCV). Drug development using laboratory experiments is not only expensive, but also time-consuming to conduct these experiments. Instead, in this in silicon study, we used computational techniques to propose a specific antiviral drug for the protein domains of found in the hepatitis C virus. This study used homology modeling and abs initio modeling to generate the 3D structure of the proteins, then identifying pockets in the proteins. Acceptable lagans for pocket drugs have been developed using the de novo drug design method. Pocket geometry is taken into account when designing ligands. Among the various lagans generated, a new specific for each of the HCV protein domains has been proposed.

Keywords: drug design, anti-viral drug, in-silicon drug design, hepatitis C virus, computer aided design, CAD education, education improvement, small-size contractor automatic pharmacy, PLC, control system, management system, communication

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4207 Comparison of User Experience in VR When Hand Gestures Are Used vs. Using Controller

Authors: Sanu Muhammed C., Nihal Vadakkan, Sahil Athrij, Sasi Gopalan

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Currently, the content entertainment industry is dominated by mobile devices. As the trends slowly shift towards AR/VR applications, the user experience on these devices should be considered, and we are trying to improve user experience in VR. This paper proposes a survey-based solution to improve user experience in VR. By creating a VR environment where users can move a ball from one position to another using a remote controller and another VR environment where users can move a ball from one place to another using hand gestures/ By allowing a set of audience to use these two environments, we can get their feedback. There are two steps in this comparison, 1) Using Hand Gestures To Move Ball In VR Environment: Here, we create a VR environment where two baskets are there, and one ball will be there in a basket. Here users can transfer the ball to another basket using hand gestures. They will be able to move the ball using hand gestures. 2) Using Remote Control To Move Ball In VR Environment: Here, we create a VR environment where two baskets are there, and one ball will be there in a basket. Here users can transfer the ball to another basket using a remote control. They will be able to move the ball using a remote controller. The above two environments are given to users to experience, and their responses will be recorded to compare the user experience in the above two environments.

Keywords: virtual reality, user experience, hand gestures, remote control

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4206 Effects of Pharmaceutical Drugs on Fish (koi) Behaviour and Muscle Function

Authors: Gayathri Vijayakumar, Preethi Baskaran

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The effluents that are let down by the industries mix with the water bodies and drastically affect the aquatic life, which leads to pollution and bio magnifications. Effluents mostly contain chemicals, heavy metals etc., and cause toxicity to the environment. The pharmaceutical industries too contribute. The by-products and other unwanted waste are discharged without any treatment; these causes DNA damage and affect behavior of aquatic life. The study was conducted on koi carp (Cyprinus carpio) the ornamental variety of common carp. A two week long study was conducted on them using common anti-depressant drug (Diazepam) in various concentrations. These drugs are known to cause behavioral damage and organ malfunctions (muscle twitch). The histopathological study conducted showed permanent muscle twitching and lesions in the fish samples studied. The sociability was also affected in the span of 14 days. Higher concentrations of this drug showed severe damage in the muscle structures. Thus, this drug can cause adverse effects on marine ecosystem and eventually cause bio magnification of drug by running through the food chain.

Keywords: pollution, toxicity, bio-magnifications, koi carp, muscle twitch, diazepam, histopathology

Procedia PDF Downloads 100
4205 Exploring the Potential of Replika: An AI Chatbot for Mental Health Support

Authors: Nashwah Alnajjar

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This research paper provides an overview of Replika, an AI chatbot application that uses natural language processing technology to engage in conversations with users. The app was developed to provide users with a virtual AI friend who can converse with them on various topics, including mental health. This study explores the experiences of Replika users using quantitative research methodology. A survey was conducted with 12 participants to collect data on their demographics, usage patterns, and experiences with the Replika app. The results showed that Replika has the potential to play a role in mental health support and well-being.

Keywords: Replika, chatbot, mental health, artificial intelligence, natural language processing

Procedia PDF Downloads 86
4204 Drug Sensitivity Pattern of Organisms Causing Suppurative Otitis Media

Authors: Nagat M. Saeed, Mabruka S. Elashheb, Fatma M. Ben Rabaha, Aisha M Edrah

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The aim of the study was to determine the type and pattern of antibiotic susceptibility of the pathogenic microorganisms causing chronic suppurative otitis media (CSOM), which could lead to better therapeutic decisions and consequently avoidance of appearance of resistance to specific antibiotics. Most frequently isolated agents were Pseudomonas aeruginosa 28.5%; followed by Staphylococcus aureus 18.2%; proteus mirabilis 13.9%; Providencia stuartti 6.7%; Bacteroides melaninogenicus, Aspergillus sp., candida sp., 4.2% each; and other microorganisms were represented in 3-0.2%. Drug sensitivities pattern of Pseudomonas aeruginosa showed that ciprofloxacin was active against the majority of isolates (93.9%) followed by ceftazidime 86.2%, amikacin 76.2% and gentamicin 40.8%. However, Staphylococcus aureus isolates were resistant to penicillin 72.7%, erythromycin 28.6%, cephalothin 18.2%, cloxacillin 8.3% and ciprofloxacin was active against 96.2% of isolates. The resistance pattern of proteus mirabilis was 55.6% to ampicillin, 47.1% to carbencillin, 29.4% to cephalothin, 14.3% to gentamicin and 4.8% to amikacin while 100% were sensitive to ciprofloxacin. We conclude that ciprofloxacin is the best drug of choice in the treatment of CSOM caused by the common microorganisms.

Keywords: otitis media, chronic suppurative otitis media (CSOM), microorganisms, drug sensitivity

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4203 Improving the Aqueous Solubility of Taxol through Altering XLOGP3

Authors: Arianna Zhu, Thomas Bakupog

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Taxol (generic name paclitaxel) is an antineoplastic drug used to treat breast, lung, and ovarian cancer. It performs exceptionally well against a wide variety of tumors, including B16 melanoma, L1210 and P388 leukemias, MX-1 mammary tumors, and CX-1 colon tumor xenografts. However, despite taxol’s efficacy in antitumor activity, its aqueous solubility is extremely poor, decreasing its bioavailability and making it difficult for the body to absorb. The objective of this study is to improve the solubility of taxol, thus increasing the bioavailability of the drug in preventing cancer. By modifying the structure of taxol, four novel taxol derivatives were created with improved solubilities. Two of the derivatives were given an additional hydrogen donor and acceptor and thus showed a pronounced positive change in solubility. The results of this work solve the issue of taxol’s inadequate solubility and show potential in increasing the absorption of the drug.

Keywords: Taxol, Solubility, improving bioavailability, logP

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4202 Fabrication and Characterization of Transdermal Spray Using Film Forming Polymer

Authors: Paresh Patel, Harshit Patel

Abstract:

Superficial fungal skin infection is among the most common skin disease. The drug administration through skin has received attention due to several advantages: Avoidance of significant pre-systemic metabolism, drug levels within the therapeutic window, drugs with short biological half-lives, decreased side effects, the non-invasive character, and very high acceptance.

Keywords: transdermal spray, ketoconazole, Eudragit® RLPO, therapeutic window

Procedia PDF Downloads 399
4201 The Tariffs of Water Service for Productive Users: A Model for Defining Fare Classes

Authors: M. Macchiaroli, V. Pellecchia, L. Dolores

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The water supply for production users (craft, commercial, industrial), understood as the set of water supply and wastewater collection services becomes an increasingly felt problem in a water scarcity regime. In fact, disputes are triggered between the different social parties for the fair and efficient use of water resources. Within this aspect, the problem arises of the different pricing of services between civil users and production users. Of particular interest is the question of defining the tariff classes depending on consumption levels. If for civil users, this theme is strongly permeated by social profiles (a topic dealt with by the author in a forthcoming research contribution) connected with the inalienability of the right to have water and with the reconciliation of the needs of the weakest groups of the population, for consumers in the production sector the logic adopted by the manager may be inspired by criteria of greater corporate rationality. This work illustrates the Italian regulatory framework and shows an optimization model of tariff classes in the production sector that reconciles the public objective of sustainable use of the resource and the needs of a production system in search of recovery after the depressing effects caused by COVID-19 pandemic.

Keywords: decision making, economic evaluation, urban water management, water tariff

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4200 Nano-emulsion/Nano-suspension as Precursors for Oral Dissolvable Film to Enhance Bioavalabilty for Poor-water Solubility Drugs

Authors: Yuan Yang, Mickey Lam

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Oral dissolvable films have been considered as a unique alternative approach to conventional oral dosage forms. The films could be administrated via the gastrointestinal tract as conventional dosages or through sublingual/buccal mucosa membranes, which could enhance drug bioavailability by avoiding the first-pass effect and improving permeability due to high blood flow and lymphatic circulation. This work has described a state-of-art technic using nano-emulsion/nano-suspension as a precursor for the film to enhance the bioavailability of BCS class II drugs. The drug molecules are consequentially processed through the emulsification, gelation, and film-casting processes. The gelation process is critical to stabilizing the nano-emulsion for the film-casting as well as controlling the drug release process. Furthermore, the size of the nanoparticle on the film has a strong correlation with the size of the micelles in the precursor and the condition of the gelation process. It has been discovered that nanoparticle from 200 nm to 300 nm has shown the highest permeability for sublingual administration. In one example shown in work, the bioavailability of a low solubilize drug has been increased from 10% to 24% via sublingual administration of the film. The increasing of the bioavailability was thought to be associated with the enhancement of the diffusion process of the drug in the saliva layer above the mucosa membrane and the fact that the presents of the emulsifier help lose the rigid junction of the mucosa cells.

Keywords: oral dissolvable film, nano-suspension, nano-emulsion, bioavailability

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4199 Potential Impact of Sodium Salicylate Nanoemulsion on Expression of Nephrin in Nephrotoxic Experimental Rat

Authors: Nadia A. Mohamed, Zakaria El-Khayat, Wagdy K. B. Khalil, Mehrez E. El-Naggar

Abstract:

Drug nephrotoxicity is still a problem for patients who have taken drugs for elongated periods or permanently. Ultrasound-assisted sol−gel method was used to prepare hollow structured poroussilica nanoemulsion loaded with sodium salicylate as a model drug. The work was extended to achieve the target of the current work via investigating the protective role of this nanoemulsion model as anti-inflammatory drug or ginger for its antioxidant effect against cisplatin-induced nephrotoxicity in male albino rats. The results clarify that the nanoemulsion model was synthesized using ultrasonic assisted with small size and well stabilization as proved by TEM and DLS analysis. Additionally, blood urea nitrogen (BUN), Serum creatinine (SC) and Urinary total protein (UTP) were increased, and the level of creatinine clearance (Crcl) was decreased. All those were met with disorders in oxidative stress and downregulation in the expression of the nephrin gene. Also, histopathological changes of the kidney tissue were observed. These changes back to normal by treatment with silica nanoparticles loaded sodium salicylate (Si-Sc-NPs), ginger or both. Conclusions oil/water nanoemulsion of (Si-Sc NPs) and ginger showed a protective and promising preventive strategy against nephrotoxicity due to their antioxidant and anti-inflammatory effects, and that offers a new approach in attenuating drug induced nephrotoxicity.

Keywords: sodium salicylate nanoencapsulation, nephrin mRNA, drug nephrotoxicity, cisplatin, experimental rats

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4198 Lipid-polymer Nanocarrier Platform Enables X-Ray Induced Photodynamic Therapy against Human Colorectal Cancer Cells

Authors: Rui Sang, Fei Deng, Alexander Engel, Ewa M. Goldys, Wei Deng

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In this study, we brought together X-ray induced photodynamic therapy (X-PDT) and chemo-drug (5-FU) for the treatment on colorectal cancer cells. This was achieved by developing a lipid-polymer hybrid nanoparticle delivery system (FA-LPNPs-VP-5-FU). It was prepared by incorporating a photosensitizer (verteporfin), chemotherapy drug (5-FU), and a targeting moiety (folic acid) into one platform. The average size of these nanoparticles was around 100 nm with low polydispersity. When exposed to clinical doses of 4 Gy X-ray radiation, FA-LPNPs-VP-5-FU generated sufficient amounts of reactive oxygen species, triggering the apoptosis and necrosis pathway of cancer cells. Our combined X-PDT and chemo-drug strategy was effective in inhibiting cancer cells’ growth and proliferation. Cell cycle analyses revealed that our treatment induced G2/M and S phase arrest in HCT116 cells. Our results indicate that this combined treatment provides better antitumour effect in colorectal cancer cells than each of these modalities alone. This may offer a novel approach for effective colorectal cancer treatment with reduced off-target effect and drug toxicity.

Keywords: pdt, targeted lipid-polymer nanoparticles, verteporfin, colorectal cancer

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4197 Privacy Policy Prediction for Uploaded Image on Content Sharing Sites

Authors: Pallavi Mane, Nikita Mankar, Shraddha Mazire, Rasika Pashankar

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Content sharing sites are very useful in sharing information and images. However, with the increasing demand of content sharing sites privacy and security concern have also increased. There is need to develop a tool for controlling user access to their shared content. Therefore, we are developing an Adaptive Privacy Policy Prediction (A3P) system which is helpful for users to create privacy settings for their images. We propose the two-level framework which assigns the best available privacy policy for the users images according to users available histories on the site.

Keywords: online information services, prediction, security and protection, web based services

Procedia PDF Downloads 358
4196 A New Cytoprotective Drug on the Basis of Cytisine: Phase I Clinical Trial Results

Authors: B. Yermekbayeva, A. Gulyayaev, T. Nurgozhin, C. Bektur

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Cytisine aminophosphonate under the name "Cytafat" was approved for clinical trials in Republic of Kazakhstan as a putative liver protecting drug for the treatment of acute toxic hepatitis. A method of conducting the clinical trial is a double blind study. Total number of patients -71, aged from 16 to 56 years. Research on healthy volunteers determined the maximal tolerable doze of "Cytafat" as 200 mg/kg. Side effects when administered at high dozes (100-200 mg/kg) are tachycardia and increase of arterial blood pressure. The drug is tested in the treatment of 28 patients with a syndrome of hepatocellular failure (a poisoning with substitutes of alcohol, rat poison, or medical products). "Cytafat" was intravenously administered at a dose of 10 mg/kg in 200 ml of 5 % glucose solution once daily. The number of administrations: 1-3. In the comparison group, 23 patients were treated intravenously once a day with “Essenciale H” at a dose of 10 ml. 20 patients received a placebo (10 ml of glucose intravenously). In all cases of toxic hepatopathology the significant positive clinical effect of the testing drug distinguishable from placebo and surpassing the alternative was observed. Within a day after administration a sharp reduction of cytolitic syndrome parameters (ALT, AST, alkaline phosphatase, thymol turbidity test, GGT) was registered, a reduction of the severity of cholestatic syndrome (bilirubin decreased) was recorded, significantly decreased indices of lipid peroxidation. The following day, in all cases the positive dynamics was determined with ultrasound study (reduction of diffuse changes and events of reactive pancreatitis), hepatomegaly disappeared. Normalization of all parameters occurred in 2-3 times faster, than when using the drug "Essenciale H" and placebo. Average term of elimination of toxic hepatopathy when using the drug "Cytafat" -2,8 days, "Essenciale H" -7,2 days, and placebo -10,6 days. The new drug "Cytafat" has expressed cytoprotective properties.

Keywords: cytisine, cytoprotection, hepatopathy, hepatoprotection

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4195 Conjugated Chitosan-Carboxymethyl-5-Fluorouracil Nanoparticles for Skin Delivery

Authors: Mazita Mohd Diah, Anton V. Dolzhenko, Tin Wui Wong

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Nanoparticles, being small with a large specific surface area, increase solubility, enhance bioavailability, improve controlled release and enable precision targeting of the entrapped compounds. In this study, chitosan as polymeric permeation enhancer was conjugated to a polar pro-drug, carboxymethyl-5-fluorouracil (CMFU) to increase the skin drug permeation. Chitosan-CMFU conjugate was synthesized using chemical conjugation process through succinate linker. It was then transformed into nanoparticles via spray drying method. The conjugation was elucidated using Fourier Transform Infrared and Proton Nuclear Magnetic Resonance techniques. The nanoparticle size, size distribution, zeta potential, drug content, skin permeation and retention profiles were characterized. The conjugation was denoted using 1H NMR by new peaks at signal δ = 4.184 ppm (singlet, 2H for CH2) and 7.676-7.688 ppm (doublet, 1H for C6) attributed to CMFU in chitosan-CMFU NMR spectrum. The nanoparticles had profiles of particle size: 93.97 ±35.11 nm, polydispersity index: 0.40 ± 0.14, zeta potential: +18.25 ±2.95 mV and drug content: 6.20 ± 1.98 % w/w. Almost 80 % w/w CMFU in the form of nanoparticles permeated through the skin in 24 hours and close to 50 % w/w permeation occurred in first 1-2 hours. Without conjugation to chitosan and nanoparticulation, less than 40 % w/w CMFU permeated through the skin in 24 hours. The skin drug retention likewise was higher with chitosan-CMFU nanoparticles (15.34 ± 5.82 % w/w) than CMFU (2.24 ± 0.57 % w/w). CMFU, through conjugation with chitosan permeation enhancer and processed in nanogeometry, had its skin permeation and retention degree promoted.

Keywords: carboxymethyl-5-fluorouracil, chitosan, conjugate, skin permeation, skin retention

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4194 DeepLig: A de-novo Computational Drug Design Approach to Generate Multi-Targeted Drugs

Authors: Anika Chebrolu

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Mono-targeted drugs can be of limited efficacy against complex diseases. Recently, multi-target drug design has been approached as a promising tool to fight against these challenging diseases. However, the scope of current computational approaches for multi-target drug design is limited. DeepLig presents a de-novo drug discovery platform that uses reinforcement learning to generate and optimize novel, potent, and multitargeted drug candidates against protein targets. DeepLig’s model consists of two networks in interplay: a generative network and a predictive network. The generative network, a Stack- Augmented Recurrent Neural Network, utilizes a stack memory unit to remember and recognize molecular patterns when generating novel ligands from scratch. The generative network passes each newly created ligand to the predictive network, which then uses multiple Graph Attention Networks simultaneously to forecast the average binding affinity of the generated ligand towards multiple target proteins. With each iteration, given feedback from the predictive network, the generative network learns to optimize itself to create molecules with a higher average binding affinity towards multiple proteins. DeepLig was evaluated based on its ability to generate multi-target ligands against two distinct proteins, multi-target ligands against three distinct proteins, and multi-target ligands against two distinct binding pockets on the same protein. With each test case, DeepLig was able to create a library of valid, synthetically accessible, and novel molecules with optimal and equipotent binding energies. We propose that DeepLig provides an effective approach to design multi-targeted drug therapies that can potentially show higher success rates during in-vitro trials.

Keywords: drug design, multitargeticity, de-novo, reinforcement learning

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4193 Tunable Control of Therapeutics Release from the Nanochannel Delivery System (nDS)

Authors: Thomas Geninatti, Bruno Giacomo, Alessandro Grattoni

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Nanofluidic devices have been investigated for over a decade as promising platforms for the controlled release of therapeutics. The nanochannel drug delivery system (nDS), a membrane fabricated with high precision silicon techniques, capable of zero-order release of drugs by exploiting diffusion transport at the nanoscale originated from the interactions between molecules with nanochannel surfaces, showed the flexibility of the sustained release in vitro and in vivo, over periods of time ranging from weeks to months. To improve the implantable bio nanotechnology, in order to create a system that possesses the key features for achieve the suitable release of therapeutics, the next generation of nDS has been created. Platinum electrodes are integrated by e-beam deposition onto both surfaces of the membrane allowing low voltage (<2 V) and active temporal control of drug release through modulation of electrostatic potentials at the inlet and outlet of the membrane’s fluidic channels. Hence, a tunable administration of drugs is ensured from the nanochannel drug delivery system. The membrane will be incorporated into a peek implantable capsule, which will include drug reservoir, control hardware and RF system to allow suitable therapeutic regimens in real-time. Therefore, this new nanotechnology offers tremendous potential solutions to manage chronic disease such as cancer, heart disease, circadian dysfunction, pain and stress.

Keywords: nanochannel membrane, drug delivery, tunable release, personalized administration, nanoscale transport, biomems

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4192 Double-Spear 1-H2-1 Oncolytic-Immunotherapy for Refractory and Relapsing High-Risk Human Neuroblastoma and Glioma

Authors: Lian Zeng

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Double-Spear 1-H2-1 (DS1-H2-1) is an oncolytic virus and an innovative biological drug candidate. The chemical composition of the drug product is a live attenuated West Nile virus (WNV) containing the human T cell costimulator (CD86) gene. After intratumoral injection, the virus can rapidly self-replicate in the injected site and lyse/kill the tumor by repeated infection among tumor cells. We also established xenograft tumor models in mice to evaluate the drug candidate's efficacy on those tumors. The results from preclinical studies on transplanted tumors in immunodeficient mice showed that DS1-H2-1 had significant oncolytic effects on human-origin cancers: it completely (100%) shrieked human glioma; limited human neuroblastoma growth reached as high as 95% growth inhibition rate (%TGITW). The safety data of preclinical animal experiments confirmed that DS1-H2-1 is safe as a biological drug for clinical use. In the preclinical drug efficacy experiment, virus-drug administration with different doses did not show abnormal signs and disease symptoms in more than 300 tested mice, and no side effects or death occurred through various administration routes. Intravenous administration did not cause acute infectious disease or other side effects. However, the replication capacity of the virus in tumor tissue via intravenous administration is only 1% of that of direct intratumoral administration. The direct intratumoral administration of DS1-H2-1 had a higher rate of viral replication. Therefore, choosing direct intratumoral injection can ensure both efficacy and safety.

Keywords: oncolytic virus, WNV-CD86, immunotherapy drugs, glioma, neuroblastoma

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4191 Clarification of Taxonomic Confusions among Adulterated Drugs Coffee Seena and Seena Weed through Systematic and Pharmaceutical Markers

Authors: Shabnum Shaheen, Nida Haroon, Farah Khan, Sumera Javad, Mehreen Jalal, Samina Sarwar

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Coffee Senna is pharmaceutically very important and used for multiple health disorders such as gastric pains, indigestion, snakebites, asthma and fever, tuberculosis and menstrual problems. However, its immense medicinal value and great demand lead to adulteration issue which could be injurious for users. Some times its adulterant Seena weed (Senna occidentalis L.) is used as its substitute which definitely not as effective as Coffee Senna. Hence, the present study was undertaken to provide some tools for systematic and pharmaceutical authentication of a shrubby plant Coffee Senna (Cassia occidentalis Linn.). These parameters included macro and micro morphological characters, anatomical and palynomorph characterization, solubility, fluorescence and phytochemical analysis. By the application of these parameters acquired results revealed that, these two plants are distinct from each other. The Coffee Seena was found to be an annual shrub with trilobed pollen, diacytic, paracytic and anisocytic stomata whereas the Seena weed stands out as an annual or perennial herb with spheroidal and circular pollen and paracytic type of stomata. The powdered drug of Coffee seena is dark grayish green whereas the powdered drug of Seena weed is light green in color. These findings are constructive in authentic identification of these plants.

Keywords: coffee senna, Senna weed, taxonomic evaluation, pharmaceutical markers

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4190 Current Methods for Drug Property Prediction in the Real World

Authors: Jacob Green, Cecilia Cabrera, Maximilian Jakobs, Andrea Dimitracopoulos, Mark van der Wilk, Ryan Greenhalgh

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Predicting drug properties is key in drug discovery to enable de-risking of assets before expensive clinical trials and to find highly active compounds faster. Interest from the machine learning community has led to the release of a variety of benchmark datasets and proposed methods. However, it remains unclear for practitioners which method or approach is most suitable, as different papers benchmark on different datasets and methods, leading to varying conclusions that are not easily compared. Our large-scale empirical study links together numerous earlier works on different datasets and methods, thus offering a comprehensive overview of the existing property classes, datasets, and their interactions with different methods. We emphasise the importance of uncertainty quantification and the time and, therefore, cost of applying these methods in the drug development decision-making cycle. To the best of the author's knowledge, it has been observed that the optimal approach varies depending on the dataset and that engineered features with classical machine learning methods often outperform deep learning. Specifically, QSAR datasets are typically best analysed with classical methods such as Gaussian Processes, while ADMET datasets are sometimes better described by Trees or deep learning methods such as Graph Neural Networks or language models. Our work highlights that practitioners do not yet have a straightforward, black-box procedure to rely on and sets a precedent for creating practitioner-relevant benchmarks. Deep learning approaches must be proven on these benchmarks to become the practical method of choice in drug property prediction.

Keywords: activity (QSAR), ADMET, classical methods, drug property prediction, empirical study, machine learning

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4189 Development of Site-Specific Colonic Drug Delivery System (Nanoparticles) of Chitosan Coated with pH Sensitive Polymer for the Management of Colonic Inflammation

Authors: Pooja Mongia Raj, Rakesh Raj, Alpana Ram

Abstract:

Background: The use of multiparticulate drug delivery systems in preference to single unit dosage forms for colon targeting purposes dates back to 1985 when Hardy and co-workers showed that multiparticulate systems enabled the drug to reach the colon quickly and were retained in the ascending colon for a relatively long period of time. Methods: Site-specific colonic drug delivery system (nanoparticles) of 5-ASA were prepared and coated with pH sensitive polymer. Chitosan nanoparticles (CTNP) bearing 5-Amino salicylic acid (5-ASA) were prepared, by ionotropic gelation method. Nanoparticulate dosage form consisting of a hydrophobic core enteric coated with pH-dependent polymer Eudragit S-100 by solvent evaporation method, for the effective delivery of drug to the colon for treatment of ulcerative colitis. Results: The mean diameter of CTNP and ECTNP formulations were 159 and 661 nm, respectively. Also optimum value of polydispersity index was found to be 0.249 [count rate (kcps) was 251.2] and 0.170 [count rate (kcps) was 173.9] was obtained for both the formulations respectively. Conclusion: CTNP and Eudragit chitosan nanoparticles (ECTNP) was characterized for shape and surface morphology by scanning electron microscopy (SEM) appeared to be spherical in shape. The in vitro drug release was investigated using USP dissolution test apparatus in different simulated GIT fluids showed promising release. In vivo experiments are in further proceeding for fruitful results.

Keywords: colon targeting, nanoparticles, polymer, 5-amino salicylic acid, edragit

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4188 Technological Advancement of Socratic Supported by Artificial Intelligence

Authors: Amad Nasseef, Layan Zugail, Joud Musalli, Layan Shaikan

Abstract:

Technology has become an essential part of our lives. We have also witnessed the significant emergence of artificial intelligence in so many areas. Throughout this research paper, the following will be discussed: an introduction on AI and Socratic application, we also did an overview on the application’s background and other similar applications, as for the methodology, we conducted a survey to collect results on users experience in using the Socratic application. The results of the survey strongly supported the usefulness and interest of users in the Socratic application. Finally, we concluded that Socratic is a meaningful tool for learning purposes due to it being supported by artificial intelligence, which made the application easy to use and familiar to users to deal with through a click of a button.

Keywords: Socratic, artificial intelligence, application, features

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4187 Losing Benefits from Social Network Sites Usage: An Approach to Estimate the Relationship between Social Network Sites Usage and Social Capital

Authors: Maoxin Ye

Abstract:

This study examines the relationship between social network sites (SNS) usage and social capital. Because SNS usage can expand the users’ networks, and people who are connected in this networks may become resources to SNS users and lead them to advantage in some situation, it is important to estimate the relationship between SNS usage and ‘who’ is connected or what resources the SNS users can get. Additionally, ‘who’ can be divided in two aspects – people who possess high position and people who are different, hence, it is important to estimate the relationship between SNS usage and high position people and different people. This study adapts Lin’s definition of social capital and the measurement of position generator which tells us who was connected, and can be divided into the same two aspects as well. A national data of America (N = 2,255) collected by Pew Research Center is utilized to do a general regression analysis about SNS usage and social capital. The results indicate that SNS usage is negatively associated with each factor of social capital, and it suggests that, in fact, comparing with non-users, although SNS users can get more connections, the variety and resources of these connections are fewer. For this reason, we could lose benefits through SNS usage.

Keywords: social network sites, social capital, position generator, general regression

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4186 Is Presence of Psychotic Features Themselves Carry a Risk for Metabolic Syndrome?

Authors: Rady A., Elsheshai A., Elsawy M., Nagui R.

Abstract:

Background and Aim: Metabolic syndrome affect around 20% of general population , authors have incriminated antipsychotics as serious risk factor that may provoke such derangement. The aim of our study is to assess metabolic syndrome in patients presenting psychotic features (delusions and hallucinations) whether schizophrenia or mood disorder and compare results in terms of drug naïf, on medication and healthy control. Subjects and Methods: The study recruited 40 schizophrenic patients, half of them drug naïf and the other half on antipsychotics, 40 patients with mood disorder with psychotic features, half of them drug naïf and the other half on medication, 20 healthy control. Exclusion criteria were put in order to exclude patients having already endocrine or metabolic disorders that my interfere with results obtain to minimize confusion bias. Metabolic syndrome assessed by measuring parameters including weight, body mass index, waist circumference, triglyceride level, HDL, fasting glucose, fasting insulin and insulin resistance Results: No difference was found when comparing drug naïf to those on medication in both schizophrenic and psychotic mood disorder arms, schizophrenic patients whether on medication or drug naïf should difference with control group for fasting glucose, schizophrenic patients on medication also showed difference in insulin resistance compared to control group. On the other hand, patients with psychotic mood disorder whether drug naïf or on medication showed difference from control group for fasting insulin level. Those on medication also differed from control for insulin resistance Conclusion: Our study didn’t reveal difference in metabolic syndrome among patients with psychotic features whether on medication or drug naïf. Only patients with Psychotic features on medication showed insulin resistance. Schizophrenic patients drug naïf or on medication tend to show higher fasting glucose while psychotic mood disorder whether drug naïf or on medication tend to show higher fasting insulin. This study suggest that presence of psychotic features themselves regardless being on medication or not carries a risk for insulin resistance and metabolic syndrome. Limitation: This study is limited by number of participants and larger numbers in future studies should be included in order to extrapolate results. Cohort longitudinal studies are needed in order to evaluate such hypothesis.

Keywords: schizophrenia, metabolic syndrome, psychosis, insulin, resistance

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4185 Factors Influencing Antipsychotic Drug Usage and Substitution among Nigerian Schizophrenic Patients

Authors: Ubaka Chukwuemeka Michael, Ukwe Chinwe Victoria

Abstract:

Background: The use of antipsychotic monotherapy remains the standard for schizophrenic disorders so also a prescription switch from older typical to newer atypical classes of antipsychotics on the basis of better efficacy and tolerability. However, surveys on the quality of antipsychotic drug use and substitution in developing countries are very scarce. This study was intended to evaluate quality and factors that drive the prescription and substitution of antipsychotic drugs among schizophrenic patients visiting a regional psychiatric hospital. Methods: Case files of patients visiting a federal government funded Neuropsychiatric Hospital between July 2012 and July 2014 were systematically retrieved. Patient demographic characteristics, clinical details and drug management data were collected and subjected to descriptive and inferential data analysis to determine quality and predictors of utilization. Results: Of the 600 case files used, there were more male patients (55.3%) with an overall mean age of 33.7±14.4 years. Typical antipsychotic agents accounted for over 85% of prescriptions, with majority of the patients receiving more than 2 drugs in at least a visit (80.9%). Fluphenazine (25.2%) and Haloperidol (18.8%) were mostly given as antipsychotics for treatment initiation while Olazenpine (23.0%) and Benzhexol (18.3%) were the most currently prescribed antipsychotics. Nearly half (42%, 252/600) of these patients were switched from one class to another, with 34.5% (207/600) of them switched from typical to atypical drug classes. No demographic or clinical factors influenced drug substitutions but a younger age and being married influenced being prescribed a polypharmacy regimen (more than 2 drugs) and an injectable antipsychotic agent. Conclusion: The prevalence of antipsychotic polypharmacy and use of typical agents among these patients was high. However, only age and marital status affected the quality of antipsychotic prescriptions among these patients.

Keywords: antipsychotics, drug substitution, pharmacoepidemiology, polypharmacy

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4184 Challenge Response-Based Authentication for a Mobile Voting System

Authors: Tohari Ahmad, Hudan Studiawan, Iwang Aryadinata, Royyana M. Ijtihadie, Waskitho Wibisono

Abstract:

A manual voting system has been implemented worldwide. It has some weaknesses which may decrease the legitimacy of the voting result. An electronic voting system is introduced to minimize this weakness. It has been able to provide a better result, in terms of the total time taken in the voting process and accuracy. Nevertheless, people may be reluctant to go to the polling location because of some reasons, such as distance and time. In order to solve this problem, mobile voting is implemented by utilizing mobile devices. There are many mobile voting architectures available. Overall, authenticity of the users is the common problem of all voting systems. There must be a mechanism which can verify the users’ authenticity such that only verified users can give their vote once; others cannot vote. In this paper, a challenge response-based authentication is proposed by utilizing properties of the users, for example, something they have and know. In terms of speed, the proposed system provides good result, in addition to other capabilities offered by the system.

Keywords: authentication, data protection, mobile voting, security

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4183 Lipid-Coated Magnetic Nanoparticles for Frequency Triggered Drug Delivery

Authors: Yogita Patil-Sen

Abstract:

Superparamagnetic Iron Oxide Nanoparticles (SPIONs) have become increasingly important materials for separation of specific bio-molecules, drug delivery vehicle, contrast agent for MRI and magnetic hyperthermia for cancer therapy. Hyperthermia is emerging as an alternative cancer treatment to the conventional radio- and chemo-therapy, which have harmful side effects. When subjected to an alternating magnetic field, the magnetic energy of SPIONs is converted into thermal energy due to movement of particles. The ability of SPIONs to generate heat and potentially kill cancerous cells, which are more susceptible than the normal cells to temperatures higher than 41 °C forms the basis of hyerpthermia treatement. The amount of heat generated depends upon the magnetic properties of SPIONs which in turn is affected by their properties such as size and shape. One of the main problems associated with SPIONs is particle aggregation which limits their employability in in vivo drug delivery applications and hyperthermia cancer treatments. Coating the iron oxide core with thermally responsive lipid based nanostructures tend to overcome the issue of aggregation as well as improve biocompatibility and can enhance drug loading efficiency. Herein we report suitability of SPIONs and silica coated core-shell SPIONs, which are further, coated with various lipids for drug delivery and magnetic hyperthermia applications. The synthesis of nanoparticles is carried out using the established methods reported in the literature with some modifications. The nanoparticles are characterised using Infrared spectroscopy (IR), X-ray Diffraction (XRD), Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM) and Vibrating Sample Magnetometer (VSM). The heating ability of nanoparticles is tested under alternating magnetic field. The efficacy of the nanoparticles as drug carrier is also investigated. The loading of an anticancer drug, Doxorubicin at 18 °C is measured up to 48 hours using UV-visible spectrophotometer. The drug release profile is obtained under thermal incubation condition at 37 °C and compared with that under the influence of alternating magnetic field. The results suggest that the nanoparticles exhibit superparamagnetic behaviour, although coating reduces the magnetic properties of the particles. Both the uncoated and coated particles show good heating ability, again it is observed that coating decreases the heating behaviour of the particles. However, coated particles show higher drug loading efficiency than the uncoated particles and the drug release is much more controlled under the alternating magnetic field. Thus, the results demonstrate that lipid coated SPIONs exhibit potential as drug delivery vehicles for magnetic hyperthermia based cancer therapy.

Keywords: drug delivery, hyperthermia, lipids, superparamagnetic iron oxide nanoparticles (SPIONS)

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4182 A Descriptive Preference Analysis on Waterfront Parks Neighboring Lake Shihwa

Authors: J. H. Ahn, J. W. Moon, S. J. Noh, H. K. Kim

Abstract:

Nowadays, as the ecology of Lake Shihwa has been restored significantly, the urban development is in progress around Lake Shihwa areas. Each development project includes a plan on utilizing waterfront areas, but there exist a difference on waterfront design criteria between experts and users. Therefore, it is significant to analyze preferences in design elements of existing waterfront parks around Lake Shihwa (Ansan Waterfront Park, Shihwa Reed Wetland Park, and T-Light Park) based on users’ perspectives and to reflect the result on upcoming waterfront developments. This study derives design elements on waterfront parks from literature reviews. The survey questionnaires are created based on these classified elements and the surveys are conducted to experts and users with in-depth interviews. For all three parks, several park facilities appear to be not recognized by users. Therefore, the circulation path should be introduced in guide maps and information activities and furthermore in disposition of park facilities.

Keywords: design elements, lake Shihwa, preference, waterfront park

Procedia PDF Downloads 457