Search results for: drug rewarding behavior
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 8159

Search results for: drug rewarding behavior

7799 Time Dependent Biodistribution Modeling of 177Lu-DOTATOC Using Compartmental Analysis

Authors: M. Mousavi-Daramoroudi, H. Yousefnia, F. Abbasi-Davani, S. Zolghadri

Abstract:

In this study, 177Lu-DOTATOC was prepared under optimized conditions (radiochemical purity: > 99%, radionuclidic purity: > 99%). The percentage of injected dose per gram (%ID/g) was calculated for organs up to 168 h post injection. Compartmental model was applied to mathematical description of the drug behaviour in tissue at different times. The biodistribution data showed the significant excretion of the radioactivity from the kidneys. The adrenal and pancreas, as major expression sites for somatostatin receptor (SSTR), had significant uptake. A pharmacokinetic model of 177Lu-DOTATOC was presented by compartmental analysis which demonstrates the behavior of the complex.

Keywords: biodistribution, compartmental modeling, ¹⁷⁷Lu, Octreotide

Procedia PDF Downloads 194
7798 The Effect of the Flow Pipe Diameter on the Rheological Behavior of a Polymeric Solution (CMC)

Authors: H. Abchiche, M. Mellal

Abstract:

The aim of this work is to study the parameters that influence the rheological behavior of a complex fluid (sodium Carboxyméthylcellulose solution), on a capillary rheometer. An installation has been made to be able to vary the diameter of trial conducts. The obtained results allowed us to deduce that: the diameter of trial conducts have a remarkable effect on the rheological responds.

Keywords: bingham’s fluid, CMC, cylindrical conduit, rheological behavior

Procedia PDF Downloads 309
7797 In vitro P-Glycoprotein Modulation: Combinatorial Approach Using Natural Products

Authors: Jagdish S. Patel, Piyush Chudasama

Abstract:

Context: Over-expression of P-glycoprotein (P-gp) plays critical role in absorption of many drug candidates which results into lower bioavailability of the drug. P-glycoprotein also over expresses in many pathological conditions like diabetes, affecting the drug therapy. Modulation of P-gp expression using inhibitors can help in designing novel formulation enhancing the bioavailability of the drug in question. Objectives: The main focus of the study was to develop advanced glycation end products (AGEs) induced P-gp over expression in Caco-2 cells. Curcumin, piperine and epigallocatechin gallate were used to evaluate their P-gp inhibitory action using combinatorial approach. Materials and methods: Methylglyoxal (MG) induced P-gp over expression was checked in Caco-2 cells using real time PCR. P-gp inhibitory effects of the phytochemicals were measured after induction with MG alone and in combination of any two compounds. Cytotoxicity of each of the phytochemical was evaluated using MTT assay. Results: Induction with MG (100mM) significantly induced the over expression of P-glycoprotein in Caco-2 cells after 24 hr. Curcumin, piperine and epigallocatechin gallate alone significantly reduced the level of P-gp within 6 hr of treatment period monitored by real time PCR. The combination of any two phytochemical also down regulated the expression of P-gp in cells. Combinations of Curcumin and epigallocatechin gallate have shown significant down regulation when compared with other two combinations. Conclusions: Combinatorial approach for down regulating the expression of P-gp, in pathological conditions like diabetes, has demonstrated promising approach for therapeutic purpose.

Keywords: p-glycoprotein, curcumin, piperine, epigallocatechin gallate, p-gp inhibition

Procedia PDF Downloads 311
7796 Rapid Nanoparticle Formulation Development and Screening Using NanoFabTxTM Platform

Authors: Zhen Ye, Maryam Zaroudi, Elizabeth Aisenbrey, Nicolynn E. Davis, Peng Gao

Abstract:

Nanoparticles have been used as drug delivery systems in the treatment of life-threatening diseases for decades, but traditional formulation development methods are time consuming and labor intensive. Millipore Sigma has developed a platform¬¬– NanoFabTxTM¬¬– for rapid and reproducible formulation development and screening to ensure consistentnanoparticle characteristics. Reproducible and precise control of the development process for a range of nanoparticle formulations accelerates the introduction of novel formulations to the clinic.

Keywords: Bio platform, Formulation development, NanoFabTxTM, Drug delivery

Procedia PDF Downloads 202
7795 Bioinformatics and Molecular Biological Characterization of a Hypothetical Protein SAV1226 as a Potential Drug Target for Methicillin/Vancomycin-Staphylococcus aureus Infections

Authors: Nichole Haag, Kimberly Velk, Tyler McCune, Chun Wu

Abstract:

Methicillin/multiple-resistant Staphylococcus aureus (MRSA) are infectious bacteria that are resistant to common antibiotics. A previous in silico study in our group has identified a hypothetical protein SAV1226 as one of the potential drug targets. In this study, we reported the bioinformatics characterization, as well as cloning, expression, purification and kinetic assays of hypothetical protein SAV1226 from methicillin/vancomycin-resistant Staphylococcus aureus Mu50 strain. MALDI-TOF/MS analysis revealed a low degree of structural similarity with known proteins. Kinetic assays demonstrated that hypothetical protein SAV1226 is neither a domain of an ATP dependent dihydroxyacetone kinase nor of a phosphotransferase system (PTS) dihydroxyacetone kinase, suggesting that the function of hypothetical protein SAV1226 might be misannotated on public databases such as UniProt and InterProScan 5.

Keywords: Methicillin-resistant Staphylococcus aureus, dihydroxyacetone kinase, essential genes, drug target, phosphoryl group donor

Procedia PDF Downloads 383
7794 Controlled Release of Glucosamine from Pluronic-Based Hydrogels for the Treatment of Osteoarthritis

Authors: Papon Thamvasupong, Kwanchanok Viravaidya-Pasuwat

Abstract:

Osteoarthritis affects a lot of people worldwide. Local injection of glucosamine is one of the alternative treatment methods to replenish the natural lubrication of cartilage. However, multiple injections can potentially lead to possible bacterial infection. Therefore, a drug delivery system is desired to reduce the frequencies of injections. A hydrogel is one of the delivery systems that can control the release of drugs. Thermo-reversible hydrogels can be beneficial to the drug delivery system especially in the local injection route because this formulation can change from liquid to gel after getting into human body. Once the gel is in the body, it will slowly release the drug in a controlled manner. In this study, various formulations of Pluronic-based hydrogels were synthesized for the controlled release of glucosamine. One of the challenges of the Pluronic controlled release system is its fast dissolution rate. To overcome this problem, alginate and calcium sulfate (CaSO4) were added to the polymer solution. The characteristics of the hydrogels were investigated including the gelation temperature, gelation time, hydrogel dissolution and glucosamine release mechanism. Finally, a mathematical model of glucosamine release from Pluronic-alginate-hyaluronic acid hydrogel was developed. Our results have shown that crosslinking Pluronic gel with alginate did not significantly extend the dissolution rate of the gel. Moreover, the gel dissolution profiles and the glucosamine release mechanisms were best described using the zeroth-order kinetic model, indicating that the release of glucosamine was primarily governed by the gel dissolution.

Keywords: controlled release, drug delivery system, glucosamine, pluronic, thermoreversible hydrogel

Procedia PDF Downloads 253
7793 Novel Wound Healing Biodegradable Patch of Bioactive

Authors: Abhay Asthana, Shally Toshkhani, Gyati Shilakari

Abstract:

The present research was aimed to develop a biodegradable dermal patch formulation for wound healing in a novel, sustained and systematic manner. The goal is to reduce the frequency of dressings with improved drug delivery and thereby enhance therapeutic performance. In present study optimized formulation was designed using component polymers and excipients (e.g. Hydroxypropyl methyl cellulose, Ethylcellulose, and Gelatin) to impart significant folding endurance, elasticity and strength. Gelatin was used to get a mixture using ethylene glycol. Chitosan dissolved in suitable medium was mixed with stirring to gelatin mixture. With continued stirring to the mixture Curcumin was added in optimized ratio to get homogeneous dispersion. Polymers were dispersed with stirring in final formulation. The mixture was sonicated casted to get the film form. All steps were carried out under under strict aseptic conditions. The final formulation was a thin uniformly smooth textured film with dark brown-yellow color. The film was found to have folding endurance was around 20 to 21 times without a crack in an optimized formulation at RT (23C). The drug content was in range 96 to 102% and it passed the content uniform test. The final moisture content of the optimized formulation film was NMT 9.0%. The films passed stability study conducted at refrigerated conditions (4±0.2C) and at room temperature (23 ± 2C) for 30 days. Further, the drug content and texture remained undisturbed with stability study conducted at RT 23±2C for 45 and 90 days. Percentage cumulative drug release was found to be 80% in 12 h and matched the biodegradation rate as drug release with correlation factor R2 > 0.9. The film based formulation developed shows promising results in terms of stability and release profiles.

Keywords: biodegradable, patch, bioactive, polymer

Procedia PDF Downloads 498
7792 Synthesis and Molecular Docking Studies of Hydrazone Derivatives Potent Inhibitors as a Human Carbonic Anhydrase IX

Authors: Sema Şenoğlu, Sevgi Karakuş

Abstract:

Hydrazone scaffold is important to design new drug groups and is found to possess numerous uses in pharmaceutical chemistry. Besides, hydrazone derivatives are also known for biological activities such as anticancer, antimicrobial, antiviral, and antifungal. Hydrazone derivatives are promising anticancer agents because they inhibit cancer proliferation and induce apoptosis. Human carbonic anhydrase IX has a high potential to be an antiproliferative drug target, and targeting this protein is also important for obtaining potential anticancer inhibitors. The protein construct was retrieved as a PDB file from the RCSB protein database. This binding interaction of proteins and ligands was performed using Discovery Studio Visualizer. In vitro inhibitory activity of hydrazone derivatives was tested against enzyme carbonic anhydrase IX on the PyRx programme. Most of these molecules showed remarkable human carbonic anhydrase IX inhibitory activity compared to the acetazolamide. As a result, these compounds appear to be a potential target in drug design against human carbonic anhydrase IX.

Keywords: cancer, carbonic anhydrase IX enzyme, docking, hydrazone

Procedia PDF Downloads 57
7791 Structure-Based Virtual Screening and in Silico Toxicity Test of Compounds against Mycobacterium tuberculosis 7,8-Diaminopelargonic Acid Aminotransferase (MtbBioA)

Authors: Junie B. Billones, Maria Constancia O. Carrillo, Voltaire G. Organo, Stephani Joy Y. Macalino, Inno A. Emnacen, Jamie Bernadette A. Sy

Abstract:

One of the major interferences in the Philippines’ tuberculosis control program is the widespread prevalence of Mtb strains that are resistant to known drugs, such as the MDR-TB (Multi Drug Resistant Tuberculosis) and XDR-TB (Extensively Drug Resistant Tuberculosis). Therefore, there is a pressing need to search for novel Mtb drug targets in order to be able to combat these drug resistant strains. The enzyme 7,8-diaminopelargonic acid aminotransferase enzyme, or more commonly known as BioA, is one such ideal target, as it is known that humans do not possess this enzyme. BioA primarily plays a key role in Mtb’s lipid biosynthesis pathway; more specifically in the synthesis of the enzyme cofactor biotin. In this study, structure-based pharmacophore screening, docking, and ADMET evaluation of compounds obtained from the DrugBank chemical database were performed against the MtbBioA enzyme. Results of the screening, docking, ADMET, and TOPKAT calculations revealed that out of the 6,516 compounds in the library, only 7 compounds indicated more favorable binding energies as compared to the enzyme’s known inhibitor, amiclenomycin (ACM), as well as good solubility and toxicity properties. Moreover, out of these 7 compounds, Molecule 6 exhibited the best solubility and toxicity properties. In the future, these lead compounds may then be subjected to bioactivity assays in vitro or in vivo for further evaluation of its therapeutic efficacy.

Keywords: 7, 8-diaminopelargonic acid aminotransferase, BioA, pharmacophore, molecular docking, ADMET, TOPKAT

Procedia PDF Downloads 436
7790 Formulation and in Vitro Evaluation of Cubosomes Containing CeO₂ Nanoparticles Loaded with Glatiramer Acetate Drug

Authors: Akbar Esmaeili, Zahra Salarieh

Abstract:

Cerium oxide nanoparticles (nano-series) are used as catalysts in industrial applications due to their free radical scavenging properties. Given that free radicals play an essential role in the pathology of many neurological diseases, we investigated the use of nanocrystals as a potential therapeutic agent for oxidative damage. This project synthesized nano-series from a new and environmentally friendly bio-pathway. Investigation of cerium nitrate in culture medium containing inoculated Lactobacillus acidophilus strain before incubation produces nano-series. Loaded with glatiramer acetate (GA) was formed by coating carboxymethylcellulose (CMC) and CeO2. FE-SEM analysis showed nano-series in the 9-11 nm range, spherical shape, and uniform particle size distribution. Cubic nanoparticles containing anti-multiple sclerosis (anti-Ms) treatment called GA were used. Glycerol monostearate (GMS) was used as a fat base, and evening primrose extract was used as an anti-inflammatory in cubosomes. Design-Expert® software was used to study the effects of different formulation factors on the properties of GAloaded cubic dispersions. Thirty GA-labeled cubic dispersions were prepared with GA-labeled carboxymethylcellulose and evaluated in vitro. The results showed an average nano-series size of 89.02 and a zeta potential of -49.9. Cubosomes containing GA-CMC/CeO2 showed a stable release profile for 180 min. The results showed that cubosomes containing GA-CMC/CeO2 could be a promising drug carrier with normal release behavior.

Keywords: ciochemistry, biotechnology, molecular, biology

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7789 Trehalose-Based Nanocarriers for Alleviation of Inflammation in Colitis

Authors: Wessam H. Abd-Elsalam, Mona M. Saber, Samar M. Abouelatta

Abstract:

Non-steroidal anti-inflammatory drugs (NSAIDs) are considered a double edged sword in inflammatory bowel diseases (IBDs). Some studies reported their advantageous effect in decreasing inflammation, and other studies reported that their use is associated with colitis aggravation. This study aimed to use specifically formulated trehalose-based nano-carriers that targets the colon in an attempt to alleviate inflammation caused by NSAIDs. L-α-phosphatidylcholine (PL), trehalose, and transcutol were used to prepare the trehalosomes (THs), which were also loaded with Tenoxicam(TXM) as a model NSAID. To optimize the formulation variables, a full 23 factorial design, using Design-Expert® software, was performed. The optimized formulation composed of trehalose: PL at a weight ratio of 1:1, 377.72 mg transcutol, and sonicated for 4 min, possessed a spherical shape with a size of 268.61 nm and EE% of 97.83% and released 70.22% of its drug content over 24 h. The superior protective action of TXM loaded THs compared to TXM suspension and drug-free THs was shown by the inhibition of the inflammatory biomarkers, namely; IL-1ß, IL-6, and TNF-alpha levels, as well as oxidative stress markers, measured as GSH and MDA. Improved histopathology of the colonic tissue in male New Zealand rabbits also confirmed the superiority of the TXM loaded THs compared to the unformulated drug or the drug free nano-carriers. Our findings highlight the prosperous role of THs in colon targeting and its anti-inflammatory characteristics in guarding against possible NSAIDs-driven exacerbation of colitis.

Keywords: inflammatory bowel disease, trehalose, trehalosomes, colon targeting

Procedia PDF Downloads 118
7788 Mannosylated Oral Amphotericin B Nanocrystals for Macrophage Targeting: In vitro and Cell Uptake Studies

Authors: Rudra Vaghela, P. K. Kulkarni

Abstract:

The aim of the present research was to develop oral Amphotericin B (AmB) nanocrystals (Nc) grafted with suitable ligand in order to enhance drug transport across the intestinal epithelial barrier and subsequently, active uptake by macrophages. AmB Nc were prepared by liquid anti-solvent precipitation technique (LAS). Poloxamer 188 was used to stabilize the prepared AmB Nc and grafted with mannose for actively targeting M cells in Peyer’s patches. To prevent shedding of the stabilizer and ligand, N,N’-Dicyclohexylcarbodiimide (DCC) was used as a cross-linker. The prepared AmB Nc were characterized for particle size, PDI, zeta potential, X-ray diffraction (XRD) and surface morphology using scanning electron microscope (SEM) and evaluated for drug content, in vitro drug release and cell uptake studies using caco-2 cells. The particle size of stabilized AmB Nc grafted with WGA was in the range of 287-417 nm with negative zeta potential between -18 to -25 mV. XRD studies revealed crystalline nature of AmB Nc. SEM studies revealed that ungrafted AmB Nc were irregular in shape with rough surface whereas, grafted AmB Nc were found to be rod-shaped with smooth surface. In vitro drug release of AmB Nc was found to be 86% at the end of one hour. Cellular studies revealed higher invasion and uptake of AmB Nc towards caco-2 cell membrane when compared to ungrafted AmB Nc. Our findings emphasize scope on developing oral delivery system for passively targeting M cells in Peyer’s patches.

Keywords: leishmaniasis, amphotericin b nanocrystals, macrophage targeting, LAS technique

Procedia PDF Downloads 282
7787 Optimization of Lercanidipine Nanocrystals Using Design of Experiments Approach

Authors: Dolly Gadhiya, Jayvadan Patel, Mihir Raval

Abstract:

Lercanidipine hydrochloride is a calcium channel blockers used for treating angina pectoris and hypertension. Lercanidipine is a BCS Class II drug having poor aqueous solubility. Absolute bioavailability of Lercanidipine is very low and the main reason ascribed for this is poor aqueous solubility of the drug. Design and formulatation of nanocrystals by media milling method was main focus of this study. In this present study preliminary optimization was carried out with one factor at a time (OFAT) approach. For this different parameters like size of milling beads, amount of zirconium beads, types of stabilizer, concentrations of stabilizer, concentrations of drug, stirring speeds and milling time were optimized on the basis of particle size, polydispersity index and zeta potential. From the OFAT model different levels for above parameters selected for Plackett - Burman Design (PBD). Plackett-Burman design having 13 runs involving 6 independent variables was carried out at higher and lower level. Based on statistical analysis of PBD it was found that concentration of stabilizer, concentration of drug and stirring speed have significant impact on particle size, PDI, zeta potential value and saturation solubility. These experimental designs for preparation of nanocrystals were applied successfully which shows increase in aqueous solubility and dissolution rate of Lercanidipine hydrochloride.

Keywords: Lercanidipine hydrochloride, nanocrystals, OFAT, Plackett Burman

Procedia PDF Downloads 185
7786 Policies to Reduce the Demand and Supply of Illicit Drugs in the Latin America: 2004 to 2016

Authors: Ana Caroline Ibrahim Lino, Denise Bomtempo Birche de Carvalho

Abstract:

The background of this research is the international process of control and monitoring of illicit psychoactive substances that has commenced in the early 20th century. This process was intensified with the UN Single Convention on Narcotic Drugs of 1961 and had its culmination in the 1970s with the "War on drugs", a doctrine undertaken by the United States of America. Since then, the phenomenon of drug prohibition has been pushing debates around alternatives of public policies to confront their consequences at a global level and in the specific context of Latin America. Previous research has answered the following key questions: a) With what characteristics and models has the international illicit drug control system consolidated in Latin America with the creation of the Organization of American States (OAS) and the Inter-American Drug Abuse Control Commission (CICAD)? b) What drug policies and programs were determined as guidelines for the member states by the OAS and CICAD? The present paper mainly addresses the analysis of the drug strategies developed by the OAS/CICAD for the Americas from 2004 to 2016. The primary sources have been extracted from the OAS/CICAD documents and reports, listed on the Internet sites of these organizations. Secondary sources refer to bibliographic research on the subject with the following descriptors: illicit drugs, public policies, international organizations, OAS, CICAD, and reducing the demand and supply of illicit drugs. The "content analysis" technique was used to organize the collected material and to choose the axes of analysis. The results show that the policies, strategies, and action plans for Latin America had been focused on anti-drug actions since the creation of the Commission until 2010. The discourses and policies to reduce drug demand and supply were of great importance for solving the problem. However, the real focus was on eliminating the substances by controlling the production, marketing, and distribution of illicit drugs. Little attention was given to the users and their families. The research is of great relevance to the Social Work. The guidelines and parameters of the Social Worker's profession are in line with the need for social, ethical, and political strengthening of any dimension that guarantees the rights of users of psychoactive substances. In addition, it contributed to the understanding of the political, economic, social, and cultural factors that structure the prohibitionism, whose matrix anchors the deprivation of rights and violence.

Keywords: illicit drug policies, international organizations, latin America, prohibitionism, reduce the demand and supply of illicit drugs

Procedia PDF Downloads 133
7785 Numerical Analysis of Effect of Crack Location on the Crack Breathing Behavior

Authors: H. M. Mobarak, Helen Wu, Keqin Xiao

Abstract:

In this work, a three-dimensional finite element model was developed to investigate the crack breathing behavior at different crack locations considering the effect of unbalance force. A two-disk rotor with a crack is simulated using ABAQUS. The duration of each crack status (open, closed and partially open/closed) during a full shaft rotation was examined to analyse the crack breathing behavior. Unbalanced shaft crack breathing behavior was found to be different at different crack locations. The breathing behavior of crack along the shaft length is divided into different regions depending on the unbalance force and crack location. The simulated results in this work can be further utilised to obtain the time-varying stiffness matrix of the cracked shaft element under the influence of unbalance force.

Keywords: crack breathing, crack location, slant crack, unbalance force, rotating shaft

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7784 Social Appearance Anxiety, Body Dissatisfaction, and Disordered Eating Behavior among Cancer Survivors

Authors: Rose J. Thazhathukunnel, A. G. Smitha

Abstract:

In the wake of social development, humans overlook the ideal physical appearance, and there is an increasing trend of criticising other’s bodies or offering tips to hide imperfections. Social appearance anxiety demonstrates the association with body dissatisfaction and disordered eating behavior. In this study, we examined the hypothesis that social appearance anxiety, body dissatisfaction, and disordered eating behavior would predict the relation between each among cancer survivors. It was observed that implicit belief to be thin was more pronounced in people with low body dissatisfaction than those with high body dissatisfaction. Results of the study indicated that overall body dissatisfaction and social appearance anxiety were correlated with disordered eating behavior for both men and women cancer survivors of all ages.

Keywords: social appearance anxiety, body dissatisfaction, disordered eating behavior, cancer survivors

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7783 Boundedness and Asymptotic Behavior of Solutions for Gierer-Meinhardt Systems

Authors: S. Henine, A. Youkana

Abstract:

This work is devoted to study the global existence and asymptotic behavior of solutions for Gierer-Meinhardt systems arising in biological phenomena. We prove that the solutions are global and uniformly bounded by a positive constant independent of the time. Our technique is based on Lyapunov functional argument. Under suitable conditions, we established a result on the asymptotic behavior of solutions. These results are valid for any positive continuous initial data, and improve some recently results established.

Keywords: asymptotic behavior, Gierer-Meinhardt systems, global existence, Lyapunov functional

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7782 Poly (3,4-Ethylenedioxythiophene) Prepared by Vapor Phase Polymerization for Stimuli-Responsive Ion-Exchange Drug Delivery

Authors: M. Naveed Yasin, Robert Brooke, Andrew Chan, Geoffrey I. N. Waterhouse, Drew Evans, Darren Svirskis, Ilva D. Rupenthal

Abstract:

Poly(3,4-ethylenedioxythiophene) (PEDOT) is a robust conducting polymer (CP) exhibiting high conductivity and environmental stability. It can be synthesized by either chemical, electrochemical or vapour phase polymerization (VPP). Dexamethasone sodium phosphate (dexP) is an anionic drug molecule which has previously been loaded onto PEDOT as a dopant via electrochemical polymerisation; however this technique requires conductive surfaces from which polymerization is initiated. On the other hand, VPP produces highly organized biocompatible CP structures while polymerization can be achieved onto a range of surfaces with a relatively straight forward scale-up process. Following VPP of PEDOT, dexP can be loaded and subsequently released via ion-exchange. This study aimed at preparing and characterising both non-porous and porous VPP PEDOT structures including examining drug loading and release via ion-exchange. Porous PEDOT structures were prepared by first depositing a sacrificial polystyrene (PS) colloidal template on a substrate, heat curing this deposition and then spin coating it with the oxidant solution (iron tosylate) at 1500 rpm for 20 sec. VPP of both porous and non-porous PEDOT was achieved by exposing to monomer vapours in a vacuum oven at 40 mbar and 40 °C for 3 hrs. Non-porous structures were prepared similarly on the same substrate but without any sacrificial template. Surface morphology, compositions and behaviour were then characterized by atomic force microscopy (AFM), scanning electron microscopy (SEM), x-ray photoelectron spectroscopy (XPS) and cyclic voltammetry (CV) respectively. Drug loading was achieved by 50 CV cycles in a 0.1 M dexP aqueous solution. For drug release, each sample was exposed to 20 mL of phosphate buffer saline (PBS) placed in a water bath operating at 37 °C and 100 rpm. Film was stimulated (continuous pulse of ± 1 V at 0.5 Hz for 17 mins) while immersed into PBS. Samples were collected at 1, 2, 6, 23, 24, 26 and 27 hrs and were analysed for dexP by high performance liquid chromatography (HPLC Agilent 1200 series). AFM and SEM revealed the honey comb nature of prepared porous structures. XPS data showed the elemental composition of the dexP loaded film surface, which related well with that of PEDOT and also showed that one dexP molecule was present per almost three EDOT monomer units. The reproducible electroactive nature was shown by several cycles of reduction and oxidation via CV. Drug release revealed success in drug loading via ion-exchange, with stimulated porous and non-porous structures exhibiting a proof of concept burst release upon application of an electrical stimulus. A similar drug release pattern was observed for porous and non-porous structures without any significant statistical difference, possibly due to the thin nature of these structures. To our knowledge, this is the first report to explore the potential of VPP prepared PEDOT for stimuli-responsive drug delivery via ion-exchange. The produced porous structures were ordered and highly porous as indicated by AFM and SEM. These porous structures exhibited good electroactivity as shown by CV. Future work will investigate porous structures as nano-reservoirs to increase drug loading while sealing these structures to minimize spontaneous drug leakage.

Keywords: PEDOT for ion-exchange drug delivery, stimuli-responsive drug delivery, template based porous PEDOT structures, vapour phase polymerization of PEDOT

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7781 Development of Self Emulsifying Drug Delivery Systems (SEDDS) of Anticancer Agents Used in AYUSH System of Medicine for Improved Oral Bioavailability Followed by Their Pharmacological Evaluation Using Biotechnological Techniques

Authors: Meenu Mehta, Munish Garg

Abstract:

The use of oral anticancer drugs from AYUSH system of medicine is widely increased among the society due to their low cost, enhanced efficacy, increased patient preference, lack of inconveniences related to infusion and they provide an opportunity to develop chronic treatment regimens. However, oral delivery of these drugs usually laid down by the limited bioavailability of the drug, which is associated with a wide variation. As most of the cytotoxic agents have a narrow therapeutic window and are dosed at or near the maximum tolerated dose, a wide variability in the bioavailability can negatively affect treatment result. It is estimated that 40% of active substances are poorly soluble in water. The improvement of bio-availability of drugs with such properties presents one of the greatest challenges in drug formulations. There are several techniques reported in literature. Among all these Self Emulsifying Drug Delivery System (SEDDS) has gained more attention due to enhanced oral bio-availability enabling a reduction in dose. Thus, SEDDS anticancer drugs will have the increased bioavailability and efficacy. These dosage form will provide societal benefit in a cost-effective manner as compared to other oral dosage forms. Present study reflects on the formulation strategies as SEDDS for oral anticancer agents of AYUSH system for enhanced bioavailability with proven efficacy by cancer cell lines.

Keywords: anticancer agents, AYUSH system, bioavailability, SEDDS

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7780 Effect of Manual Compacting and Semi-Automatic Compacting on Behavior of Stabilized Earth Concrete

Authors: Sihem Chaibeddra, Fattoum Kharchi, Fahim Kahlouche, Youcef Benna

Abstract:

In the recent years, a considerable level of interest has been developed on the use of earth in construction, led by its rediscovery as an environmentally building material. The Stabilized Earth Concrete (SEC) is a good alternative to the cement concrete, thanks to its thermal and moisture regulating features. Many parameters affect the behavior of stabilized earth concrete. This article presents research results related to the influence of the compacting nature on some SEC properties namely: The mechanical behavior, capillary absorption, shrinkage and sustainability to water erosion, and this, basing on two types of compacting: Manual and semi-automatic.

Keywords: behavior, compacting, manual, SEC, semi-automatic

Procedia PDF Downloads 336
7779 Consequences of Employees' Perception of Political Behavior in Kuwaiti Business Organizations

Authors: Ali Muhammad

Abstract:

The purpose of this study is to examine the effect of employees’ perception of political behavior on their behavior and attitudes. The model tested in this study suggests that employees’ perception of political behavior in their organizations leads to lower levels of job satisfaction, and organizational commitment, and higher levels of work-related stress, and intentions to leave the organization. A sample of 182 employees working in six Kuwaiti business organizations were surveyed using a questionnaire, and data was analyzed using correlation analysis, regression analysis, and non-parametric tests. Results reveal that employees’ perception of political behavior is negatively associated with job satisfaction and organizational commitment, and positively associated with work-related stress and employees’ intentions to leave the organization. The results of the current study are discussed and are compared to the results of previous studies in this area. Finally, the directions for future research are suggested.

Keywords: perceptions of political behavior, organizational commitment, job satisfaction, intention to leave

Procedia PDF Downloads 333
7778 Clinical Impact of Ultra-Deep Versus Sanger Sequencing Detection of Minority Mutations on the HIV-1 Drug Resistance Genotype Interpretations after Virological Failure

Authors: S. Mohamed, D. Gonzalez, C. Sayada, P. Halfon

Abstract:

Drug resistance mutations are routinely detected using standard Sanger sequencing, which does not detect minor variants with a frequency below 20%. The impact of detecting minor variants generated by ultra-deep sequencing (UDS) on HIV drug-resistance (DR) interpretations has not yet been studied. Fifty HIV-1 patients who experienced virological failure were included in this retrospective study. The HIV-1 UDS protocol allowed the detection and quantification of HIV-1 protease and reverse transcriptase variants related to genotypes A, B, C, E, F, and G. DeepChek®-HIV simplified DR interpretation software was used to compare Sanger sequencing and UDS. The total time required for the UDS protocol was found to be approximately three times longer than Sanger sequencing with equivalent reagent costs. UDS detected all of the mutations found by population sequencing and identified additional resistance variants in all patients. An analysis of DR revealed a total of 643 and 224 clinically relevant mutations by UDS and Sanger sequencing, respectively. Three resistance mutations with > 20% prevalence were detected solely by UDS: A98S (23%), E138A (21%) and V179I (25%). A significant difference in the DR interpretations for 19 antiretroviral drugs was observed between the UDS and Sanger sequencing methods. Y181C and T215Y were the most frequent mutations associated with interpretation differences. A combination of UDS and DeepChek® software for the interpretation of DR results would help clinicians provide suitable treatments. A cut-off of 1% allowed a better characterisation of the viral population by identifying additional resistance mutations and improving the DR interpretation.

Keywords: HIV-1, ultra-deep sequencing, Sanger sequencing, drug resistance

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7777 The Moderation Effect of Smart Phone Addiction in Relationship between Self-Leadership and Innovative Behavior

Authors: Gi-Ryun Park, Gye-Wan Moon, Dong-Hoon Yang

Abstract:

This study aims to explore the positive effects of self-leadership and innovative behavior that'd been proven in the existing researches proactively and understand the regulation effects of smartphone addiction which has recently become an issue in Korea. This study conducted a convenient sampling of college students attending the four colleges located at Daegu. A total of 210 questionnaires in 5-point Likert scale were distributed to college students. Among which, a total of 200 questionnaires were collected for our final analysis data. Both correlation analysis and regression analysis were carried out to verify those questionnaires through SPSS 20.0. As a result, college students' self-leadership had a significantly positive impact on innovative behavior (B= .210, P= .003). In addition, it is found that the relationship between self-leadership and innovative behavior can be adjusted depending on the degree of smartphone addiction in college students (B= .264, P= .000). This study could first understand the negative effects of smartphone addiction and find that if students' self-leadership is improved in terms of self-management and unnecessary use of smartphone is controlled properly, innovative behavior can be improved. In addition, this study is significant in that it attempts to identify a new impact of smartphone addiction with the recent environmental changes, unlike the existing researches that'd been carried out from the perspective of organizational behavior theory.

Keywords: innovative behavior, revolutionary behavior, self-leadership, smartphone addiction

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7776 The Effect of Mood and Normative Conformity on Prosocial Behavior

Authors: Antoine Miguel Borromeo, Kristian Anthony Menez, Moira Louise Ordonez, David Carl Rabaya

Abstract:

This study aimed to test if induced mood and normative conformity have any effect specifically on prosocial behavior, which was operationalized as the willingness to donate to a non-government organization. The effect of current attitude towards the object of the prosocial behavior was also considered with a covariate test. Undergraduates taking an introductory course on psychology (N = 132) from the University of the Philippines Diliman were asked how much money they were willing to donate after being presented a video about coral reef destruction and a website that advocates towards saving the coral reefs. A 3 (Induced mood: Positive vs Fear and Sadness vs Anger, Contempt, and Disgust) x 2 (Normative conformity: Presence vs Absence) between-subjects analysis of covariance was used for experimentation. Prosocial behavior was measured by presenting a circumstance wherein participants were given money and asked if they were willing to donate an amount to the non-government organization. An analysis of covariance revealed that the mood induced has no significant effect on prosocial behavior, F(2,125) = 0.654, p > 0.05. The analysis also showed how normative conformity has no significant effect on prosocial behavior, F(1,125) = 0.238, p > 0.05, as well as their interaction F(2, 125) = 1.580, p > 0.05. However, the covariate, current attitude towards corals was revealed to be significant, F(1,125) = 8.778, p < 0.05. From this, we speculate that inherent attitudes of people have a greater effect on prosocial behavior than temporary factors such as mood and conformity.

Keywords: attitude, induced mood, normative conformity, prosocial behavior

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7775 Development and In vitro Characterization of Diclofenac-Loaded Microparticles

Authors: Prakriti Diwan, S. Saraf

Abstract:

The present study involves preparation and evaluation of microparticles of diclofenac sodium. The microparticles were prepared by the emulsion solvent evaporation techniques using ethylcellulose polymer. Four different batches of microspheres were prepared by varying the concentration of polymer from 50% to 80% w/w. The microspheres were characterized for drug content, percentage yield and encapsulation efficiency, particle size analysis and surface morphology. Microsphere prepared with high drug content produces higher percentage yield and encapsulation efficiency values. It was observed the increase in concentration of the polymer, increases the mean particle size of the microspheres. The effect of polymer concentration on the in vitro release of diclofenac from the microspheres was also studied. The production microparticles yield showed 98.74%, mean particle size 956.32µm and loading efficiency 97.15%. The results were found that microparticles prepared had slower release than microparticles (p>0.05). Therefore, it may be concluded that drug loaded microparticles are suitable delivery systems for diclofenac sodium.

Keywords: diclofenac sodium, emulsion solvent evaporation, ethylcellulose, microparticles

Procedia PDF Downloads 274
7774 The Rational Design of Original Anticancer Agents Using Computational Approach

Authors: Majid Farsadrooh, Mehran Feizi-Dehnayebi

Abstract:

Serum albumin is the most abundant protein that is present in the circulatory system of a wide variety of organisms. Although it is a significant macromolecule, it can contribute to osmotic blood pressure and also, plays a superior role in drug disposition and efficiency. Molecular docking simulation can improve in silico drug design and discovery procedures to propound a lead compound and develop it from the discovery step to the clinic. In this study, the molecular docking simulation was applied to select a lead molecule through an investigation of the interaction of the two anticancer drugs (Alitretinoin and Abemaciclib) with Human Serum Albumin (HSA). Then, a series of new compounds (a-e) were suggested using lead molecule modification. Density functional theory (DFT) including MEP map and HOMO-LUMO analysis were used for the newly proposed compounds to predict the reactivity zones on the molecules, stability, and chemical reactivity. DFT calculation illustrated that these new compounds were stable. The estimated binding free energy (ΔG) values for a-e compounds were obtained as -5.78, -5.81, -5.95, -5,98, and -6.11 kcal/mol, respectively. Finally, the pharmaceutical properties and toxicity of these new compounds were estimated through OSIRIS DataWarrior software. The results indicated no risk of tumorigenic, irritant, or reproductive effects and mutagenicity for compounds d and e. As a result, compounds d and e, could be selected for further study as potential therapeutic candidates. Moreover, employing molecular docking simulation with the prediction of pharmaceutical properties helps to discover new potential drug compounds.

Keywords: drug design, anticancer, computational studies, DFT analysis

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7773 Affect and Helping Behavior as Explanatory Account of the Relationship between Psychological Safety and Supervisor Satisfaction

Authors: Mariam Musaddiq, Muhammad Ali Asadullah

Abstract:

Psychological safety is referred as a 'nonthreatening' and 'predictable' work environment leading employees, particularly interested to contribute positively to the organization, to engage and express their true selves at work without suffering negative results. We posit that the employee who is feeling psychologically safe experiences positive emotions, feels happy and shows helping behavior towards his coworkers and supervisors. Particularly, the supervisor reciprocates this helping behavior in form of greater satisfaction to the employee showing helping behavior. We tested our hypothesis in light of Feedback system theory and functional motive theory. We collected data from 453 employees and their supervisor in Pakistani hotels and restaurants through survey method. Result showed that positive affect and helping behavior mediate the relationship between psychological safety and supervisor satisfaction. Cross sectional design of the study is a major limitation of the study. Moreover, we focused on psychological safety only that is one of three dimensions of psychological conditions.

Keywords: affect, helping behavior, psychological safety, supervisor, supervisor satisfaction

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7772 Clinical Signs of River Blindness and the Efficacy of Ivermectin Therapy in Idogun, Ondo State-Nigeria

Authors: Afolabi O.J, Simon-Oke I.A., Oniya M.O., Okaka C.E.

Abstract:

River blindness is a skin, and an eye disease caused by Onchocerca volvulus and vectored by a female hematophagous blackfly. The study aims to evaluate the distribution of the clinical signs of river blindness and the efficacy of ivermectin in the treatment of river blindness in Idogun. Observational studies in epidemiology that involve the use of a structured questionnaire to obtain useful epidemiological information from the respondents, physical assessment via palpation from head to ankle was used to assess clinical signs from the respondents and skin snip test was used to evaluate the prevalence of the disease. The efficacy of the drug was evaluated and expressed in percentages. One hundred and ninety-two (192) out of the 384 respondents examined, showed various signs of river blindness. However, it was only 108 (28.1%) respondents with the clinical signs that demonstrated Onchocerca volvulus microfilariae in their skin snips. The clinical signs observed among the respondents include skin depigmentation such as dermatitis, leopard skin, papules, pruritus and self-inflicted injury, while ocular symptoms include cataract, ocular lesion and partial blindness. Among these clinical signs, papules, and pruritus were the most dominant in the community. The prevalence of the clinical signs was observed to vary significantly among the age groups and gender (P<0.05). The efficacy of the drug after 6 and 12 months of treatments shows that the drug is more effective at age groups 10-50 years than the age groups 51-90 years. Ivermectin is observed to be efficacious in the treatment of the disease. However, to achieve eradication of the disease, the drug may be administered at 0.15mg/kg twice a year.

Keywords: riverblindness, clinical signs, ivermectin, Idogun

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7771 Modeling of Coupled Mechanical State and Diffusion in Composites with Impermeable Fibers

Authors: D. Gueribiz, F. Jacquemin, S. Fréour

Abstract:

During their service life, composite materials are submitted to humid environments. The moisture absorbed by their matrix polymer induced internal stresses which can lead to multi-scale damage and may reduce the lifetime of composite structures. The estimation of internal stresses is based at a first on realistic evaluation of the diffusive behavior of composite materials. Generally, the modeling and simulation of the diffusive behavior of composite materials are extensively investigated through decoupled models based on the assumption of Fickien behavior. For these approaches, the concentration and the deformation (or stresses), the two state variables of the problem considered are governed by independent equations which are solved separately. In this study, a model coupling diffusive behavior with stresses state for a polymer matrix composite reinforced with impermeable fibers is proposed, the investigation of diffusive behavior is based on a more general thermodynamic approach which introduces a dependence of diffusive behavior on internal stresses state. The coupled diffusive behavior modeling was established in first for homogeneous and isotropic matrix and it is, thereafter, extended to impermeable unidirectional composites.

Keywords: composites materials, moisture diffusion, effective moisture diffusivity, coupled moisture diffusion

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7770 The Effect of Cognitive Restructuring and Assertive Training on Improvement of Sexual Behavior of Secondary School Adolescents in Nigeria

Authors: Azu Kalu Oko, Ugboaku Nwanpka

Abstract:

The study investigated the effect of cognitive restructuring and assertive training on improvement of sexual behavior of secondary school adolescents in Nigeria. To guide the study, three research questions and four hypothesis were formulated. The study featured a 2X3 factorial design with a sample of 48 male and female students selected by random sampling using a table of random sample numbers. The three groups are assertive training, cognitive restructuring and control group. The study identified adolescents with deviant sexual behavior using Students Sexual Behavior Inventory (S.S.B.I.) as the research instrument. Ancova and T- Test statistic were used to analyze the data. The findings revealed that: I. Assertive Training and Cognitive Restructuring significantly improved sexual behavior of subjects at post test when compared with the control group. II. The treatment gains made by the two techniques were sustained at one month follow-up interval. III. Cognitive restructuring was more effective than assertiveness training in the improvement of the sexual behavior of students. Implication for education, psychotherapy and counseling were highlighted.

Keywords: cognitive restructuring, assertiveness training, adolescents, sexual behavior

Procedia PDF Downloads 573