Search results for: Drug targets

Authors: D. Bhaskar, N. R. Wadehra, M. Gulati, A. Narula, R. Vishnu, G. Katyal

Abstract:

With drug resistance becoming widespread in Plasmodium falciparum infections, the development of the alternative drugs is the desired strategy for prevention and cure of malaria. Three drug targets were selected to screen promising drug molecules from the GSK library of 13469 molecules. Using an in silico structure-based drug designing approach, the differences in binding energies of the substrate and inhibitor were exploited between target sites of parasite and human to design a drug molecule against Plasmodium. The docking studies have shown several promising molecules from GSK library with more effective binding as compared to the already known inhibitors for the drug targets. Though stronger interaction has been shown by several molecules as compared to the reference, few molecules have shown the potential as drug candidates though in vitro studies are required to validate the results. In case of thymidylate synthase-dihydrofolatereductase (TS-DHFR), three compounds have shown promise for future studies as potential drugs.

Keywords: Drug resistance, Drug targets, In silico studies, Plasmodium falciparum.

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Authors: Baharak Khoshkholgh-Sima, Soroush Sardari, Jalal Izadi Mobarakeh, Ramezan Ali Khavari-Nejad

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There is an urgent need to develop novel Mycobacterium tuberculosis (Mtb) drugs that are active against drug resistant bacteria but, more importantly, kill persistent bacteria. Our study structured based on integrated analysis of metabolic pathways, small molecule screening and similarity Search in PubChem Database. Metabolic analysis approaches based on Unified weighted used for potent target selection. Our results suggest that pantothenate synthetase (panC) and and 3-methyl-2-oxobutanoate hydroxymethyl transferase (panB) as a appropriate drug targets. In our study, we used pantothenate synthetase because of existence inhibitors. We have reported the discovery of new antitubercular compounds through ligand based approaches using computational tools.

Keywords: In Silico, Ligand-based Virtual Screening, Metabolic Pathways, Mycobacterium tuberculosis

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Authors: A. Taqaddas

Abstract:

Medulloblastoma (MB) is one of the most prevalent brain tumours among paediatrics. Although its management has evolved over time still there is need to find new therapeutic targets for MB that can result in less normal tissue toxicity while improving survival and reducing recurrence. This literature review is aimed at finding new potential therapeutic targets for MB focusing on viruses that can be used as potential targets for MB. The review also gives an over-view of management of paediatric Medulloblastoma focusing on Radiotherapy management.

Keywords: Cytomegalovirus, Measles Virus, Medulloblastoma, Radiotherapy.

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Authors: Hsuan-Chia Yang, Yan-Jhih Haung, Yu-Chuan Li

Abstract:

Researchers of drug-drug interaction alert systems have often suggested that there were high overridden rate for alerts and also too false alerts. However, research about decreasing false alerts is scant. Therefore, the aim of this article attempts to proactive identification of false alert for drug-drug interaction and provide solution to decrease false alerts. This research involved retrospective analysis prescribing database and calculated false alert rate by using MYSQL and JAVA. Results of this study showed 17% of false alerts and the false alert rate in the hospitals (37%) was more than in the clinics. To conclude, this study described the importance that drug-drug interaction alert system should not only detect drug name but also detect frequency or route, as well as in providing solution to decrease false alerts.

Keywords: drug-drug interaction, proactive identification, false alert

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

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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: Dihydroxyacetone kinase, essential genes, Methicillin-resistant Staphylococcus aureus, drug target.

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Authors: Emma R. Arakelova, Stepan G. Grigoryan, Ashot M. Khachatryan, Karapet E. Avjyan, Lilia M. Savchenko, Flora G. Arsenyan

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The paper presents a new drugs delivery system, based on the thin film technology. As a model antitumor drug, highly toxic doxorubicin is chosen. The system is based on the technology of obtaining zinc oxide composite of doxorubicin by deposition of nanosize ZnO films on the surface of doxorubicin coating on glass substrate using DC magnetron sputtering of zinc targets in Ar:O₂ medium at room temperature. For doxorubicin zinc oxide compositions in the form of coatings and gels with 180-200nm thick ZnO films, higher (by a factor 2) in vivo (ascitic Ehrlich's carcinoma) antitumor activity is observed at low doses of doxorubicin in comparison with that of the initial preparation at therapeutic doses. The vector character of the doxorubicin zinc oxide composite transport to tumor tissues ensures the increase in antitumor activity as well as decrease of toxicity in comparison with the initial drug.

Keywords: Antitumor activity, doxorubicin, DC magnetron sputtering, zinc oxide.

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Authors: Pimporn Thongmuang

Abstract:

The import value of Antimicrobial drugs reached approximately fifteen million Baht in 2010, considered as the highest import value of all modern drugs, and this value is rising every year. Antimicrobials are considered the hazardous drugs by the Ministry of Public Health (No. 10). This research was conducted in order to investigate the past knowledge of drug use and Antimicrobial drug use behavior. A total of 757 students were selected as the samples out of a population of 1,800 students. This selected students had the experience of Antimicrobial drugs use a year ago. A questionnaire was utilized in this research. The findings put on the view that knowledge gained by the students about proper use of Antimicrobials drugs was not brought into practice. This suggests that the education procedure regarding drug use needs adjustment. And therefore the findings of this research are expected to be utilized as guidelines for educating people about the proper use of Antimicrobials drugs. At a broader perspective, correct drug use behavior of the public may potentially reduce drug cost of the Ministry of Public Health of Thailand.

Keywords: Drug Use Knowledge, Antimicrobial Drugs, Drug Use Behavior.

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Authors: Si Chen, Caroline Wiltshire, Bin Li

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This study statistically models the surface f0 contour and the underlying pitch target of a well-studied third sandhi tone of Mandarin Chinese. Although the growth curve analysis on the surface f0 contours indicates non-neutralization of this sandhi tone (T3) and the base T2, their underlying pitch targets do show neutralization. These results in Mandarin are also consistent with the perception of native speakers, where they cannot distinguish the third T3 from the base T2, compensating contextual variation. It is possible to use the proposed statistical procedure of testing underlying pitch targets to verify tone sandhi processes in other tonal languages.

Keywords: Growth curve analysis, tone sandhi, underlying pitch targets.

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Authors: Yanju Zhang, Joost M. Woltering, Fons J. Verbeek

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It has been established that microRNAs (miRNAs) play an important role in gene expression by post-transcriptional regulation of messengerRNAs (mRNAs). However, the precise relationships between microRNAs and their target genes in sense of numbers, types and biological relevance remain largely unclear. Dissecting the miRNA-target relationships will render more insights for miRNA targets identification and validation therefore promote the understanding of miRNA function. In miRBase, miRanda is the key algorithm used for target prediction for Zebrafish. This algorithm is high-throughput but brings lots of false positives (noise). Since validation of a large scale of targets through laboratory experiments is very time consuming, several computational methods for miRNA targets validation should be developed. In this paper, we present an integrative method to investigate several aspects of the relationships between miRNAs and their targets with the final purpose of extracting high confident targets from miRanda predicted targets pool. This is achieved by using the techniques ranging from statistical tests to clustering and association rules. Our research focuses on Zebrafish. It was found that validated targets do not necessarily associate with the highest sequence matching. Besides, for some miRNA families, the frequency of their predicted targets is significantly higher in the genomic region nearby their own physical location. Finally, in a case study of dre-miR-10 and dre-miR-196, it was found that the predicted target genes hoxd13a, hoxd11a, hoxd10a and hoxc4a of dre-miR- 10 while hoxa9a, hoxc8a and hoxa13a of dre-miR-196 have similar characteristics as validated target genes and therefore represent high confidence target candidates.

Keywords: MicroRNA targets validation, microRNA-target relationships, dre-miR-10, dre-miR-196.

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Authors: P. Thongmuang

Abstract:

The purposes of this research were 1) to survey the number of drugstores that unlawful dispense of asthma prescription drugs, in form of drug combinations in the Phaya Thai district of Bangkok, 2) to find the steroids contained in that drug combinations, 3) to find a means for informing general public about the dangers of drugs and for a campaign to stop dispensing them. Researcher collected drug combinations from 69 drugstores in Phaya Thai district from Feb 15, 2012 to Mar 15, 2012. The survey found 30.43%, 21, drug stores, sold asthma drug combinations to customers without a prescription. These collected samples were tested for steroid contamination by using Immunochromatography kits. Eleven samples, 52.38%, were found contaminated with steroids. In short, there should be control and inspection of drugstores in the distribution of steroid medications. To improve the knowledge of self health maintenance and drug usage among public, Thai Government and Department of Public Health should educate people about the side effects of using drug combinations and steroids.

Keywords: Dispensing, Drug Combinations, Steroids

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Authors: Arpa Petchsomrit, Namfa Sermkaew, Ruedeekorn Wiwattanapatapee

Abstract:

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

Keywords: Alginate, curcumin, floating drug delivery, oil entrapped bead.

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Authors: Dae Hwan Kang, Young-IL Jeong, Chung-Wook Chung

Abstract:

pH-sensitive drug targeting using nanoparticles for cancer chemotherapy have been spotlighted in recent decades. Graft copolymer composed of poly (L-histidine) (PHS) and dextran (DexPHS) was synthesized and pH-sensitive nanoparticles were fabricated for pH-responsive drug delivery of doxorubicin (DOX). Nanoparticles of DexPHS showed pH-sensitive changes in particle sizes and drug release behavior, i.e. particle sizes and drug release rate were increased at acidic pH, indicating that DexPHS nanoparticles have pH-sensitive drug delivery potentials. Antitumor activity of DOX-incorporated DexPHS nanoparticles were studied using CT26 colorectal carcinoma cells. Results indicated that fluorescence intensity was higher at acidic pH than basic pH. These results indicated that DexPHS nanoparticles have pH-responsive drug targeting.

Keywords: pH-sensitive polymer, nanoparticles, block copolymer, poly (L-histidine).

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

Abstract:

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

Keywords: Anti-cancer drug, center of Mass, interaction energy, molecular dynamics simulation, nanocarrier.

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Authors: Yong Ren, Yaping Zhang

Abstract:

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

Keywords: Phase change material, drug release kinetics, double emulsion, microfluidics.

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

Abstract:

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

Keywords: Piperine, Marichyadi Vati, Gastroretentive drug delivery, Floating tablet.

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Authors: Jayashree Ramana

Abstract:

An alarming emergence of multidrug-resistant strains of the tuberculosis pathogen Mycobacterium tuberculosis and continuing high worldwide incidence of tuberculosis has invigorated the search for novel drug targets. The enzyme glutamate racemase (MurI) in bacteria catalyzes the stereoconversion of L-glutamate to D-glutamate which is a component of the peptidoglycan cell wall of the bacterium. The inhibitors targeted against MurI from several bacterial species have been patented and are advocated as promising antibacterial agents. However there are none available against MurI from Mycobacterium tuberculosis, due to the lack of its threedimensional structure. This work accomplished two major objectives. First, the tertiary structure of MtMurI was deduced computationally through homology modeling using the templates from bacterial homologues. It is speculated that like in other Gram-positive bacteria, MtMurI exists as a dimer and many of the protein interactions at the dimer interface are also conserved. Second, potent candidate inhibitors against MtMurI were identified through docking against already known inhibitors in other organisms.

Keywords: Glutamate racemase, homology modeling, docking, drug resistance.

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Authors: Eric Huang, Coleman DeLude, Justin Romberg, Saibal Mukhopadhyay, Madhavan Swaminathan

Abstract:

High-performance computing (HPC) based emulators can be used to model the scattering from multiple stationary and moving targets for RADAR applications. These emulators rely on the RADAR Cross Section (RCS) of the targets being available in complex scenarios. Representing the RCS using tables generated from EM simulations is oftentimes cumbersome leading to large storage requirements. In this paper, we proposed a spherical harmonic based anisotropic scatterer model to represent the RCS of complex targets. The problem of finding the locations and reflection profiles of all scatterers can be formulated as a linear least square problem with a special sparsity constraint. We solve this problem using a modified Orthogonal Matching Pursuit algorithm. The results show that the spherical harmonic based scatterer model can effectively represent the RCS data of complex targets.

Keywords: RADAR, RCS, high performance computing, point scatterer model

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Authors: P. S. Rajinikanth, Yeoh Suyu, Sanjay Garg

Abstract:

The present study is aim to prepare and evaluate the selfnanoemulsifying drug delivery (SNEDDS) system of a poorly water soluble drug valsartan in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. The present research work describes a SNEDDS of valsartan using labrafil M 1944 CS, Tween 80 and Transcutol HP. The pseudoternary phase diagrams with presence and absence of drug were plotted to check for the emulsification range and also to evaluate the effect of valsartan on the emulsification behavior of the phases. The mixtures consisting of oil (labrafil M 1944 CS) with surfactant (tween 80), co-surfactant (Transcutol HP) were found to be optimum formulations. Prepared formulations were evaluated for its particle size distribution, nanoemulsifying properties, robustness to dilution, self emulsication time, turbidity measurement, drug content and invitro dissolution. The optimized formulations are further evaluated for heating cooling cycle, centrifugation studies, freeze thaw cycling, particle size distribution and zeta potential were carried out to confirm the stability of the formed SNEDDS formulations. The prepared formulation revealed t a significant improvement in terms of the drug solubility as compared with marketed tablet and pure drug.

Keywords: Self Emulsifying Drug Delivery System, Valsartan, Bioavailability, poorly soluble drug.

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Authors: Aditi Shukla, Ambarish S. Vidyarthi, Subir Samanta

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The worldwide prevalence of H3N2 influenza virus and its increasing resistance to the existing drugs necessitates for the development of an improved/better targeting anti-influenza drug. H3N2 influenza neuraminidase is one of the two membrane-bound proteins belonging to group-2 neuraminidases. It acts as key player involved in viral pathogenicity and hence, is an important target of anti-influenza drugs. Oseltamivir is one of the potent drugs targeting this neuraminidase. In the present work, we have taken subtype N2 neuraminidase as the receptor and probable analogs of oseltamivir as drug molecules to study the protein-drug interaction in anticipation of finding efficient modified candidate compound. Oseltamivir analogs were made by modifying the functional groups using Marvin Sketch software and were docked using Schrodinger-s Glide. Oseltamivir analog 10 was detected to have significant energy value (16% less compared to Oseltamivir) and could be the probable lead molecule. It infers that some of the modified compounds can interact in a novel manner with increased hydrogen bonding at the active site of neuraminidase and it might be better than the original drug. Further work can be carried out such as enzymatic inhibition studies; synthesis and crystallizing the drug-target complex to analyze the interactions biologically.

Keywords: H3N2 Influenza, Neuraminidase, Oseltamiviranalogs, structure based drug designing

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Authors: Jin Sun Oh, Kyung Ho Lee, S ang Gug Chung, Kyehan Rhee

Abstract:

Microbubbbles incorporating ultrasound have been used to increase the efficacy of targeted drug delivery, because microstreaming induced by cavitating bubbles affects the drug perfusion into the target cells and tissues. In order to clarify the physical effects of microstreaming on drug perfusion into tissues, a preliminary experimental study of perfusion enhancement by a stably oscillating microbubble was performed. Microstreaming was induced by an oscillating bubble at 15 kHz, and perfusion of dye into an agar phantom was optically measured by histology on agar phantom. Surface color intensity and the penetration length of dye in the agar phantom were increased more than 70% and 30%, respectively, due to the microstreaming induced by an oscillating bubble. The mass of dye perfused into a tissue phantom for 30 s was increased about 80% in the phantom with an oscillating bubble. This preliminary experiment shows the physical effects of steady streaming by an oscillating bubble can enhance the drug perfusion into the tissues while minimizing the biological effects.

Keywords: Bubble, Mass Transfer, Microstreaming, Drug Delivery, Acoustic Wave.

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Authors: Zohreh Bayat, Dariush Minai-Tehrani

Abstract:

Lipases constitute one of the most important groups of industrial enzymes that catalyze the hydrolysis of triacylglycerol to glycerol and fatty acids. Muscarinic antagonist relieves smooth muscle spasm of the gastrointestinal tract and effect on the cardiovascular system. In this research the effect of a muscarinic antagonist on the lipase activity of Pseudomonas aeruginosa was studied. Lineweaver–Burk plot showed that the drug inhibited the enzyme by competitive inhibition. The IC50 value (0.16 mM) and Ki (0.03 mM) of the drug revealed the drug bound to enzyme with high affinity. Determination of enzyme activity in various pH and temperature showed that the maximum activity of lipase was at pH 8 and 60oC both in presence and absence of the drug.

Keywords: Bacteria, inhibition, kinetics, lipase.

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Authors: Hadi Hasanzadeh, Manijhe Mokhtari-Dizaji, S.Zahra Bathaie, Zuhair M. Hassan, Hamid R. Miri, Mahbobe Alamolhoda, Vahid Nilchiani, Hamid Goudarzi

Abstract:

The nanosized polymeric micelles release the drug due to acoustic cavitation, which is enhanced in dual frequency ultrasonic fields. In this study, adult female Balb/C mice were transplanted with spontaneous breast adenocarcinoma tumors and were injected with a dose of 1.3 mg/kg doxorubicin in one of three forms: free doxorubicin, micellar doxorubicin without sonication and micellar doxorubicin with sonication. To increase cavitation yield, the tumor region was sonicated with low level dual frequency of 3 MHz and 28 kHz. The animals were sacrificed 24 h after injection, and their tumor, heart, spleen, liver, kidneys and plasma were separated and homogenized. The drug content in their tumor, heart, spleen, liver, kidneys and plasma was determined using tissue fluorimetry. The results show that in the group that received micellar doxorubicin with sonication, the drug concentration in the tumor tissue was nine and three times higher than in the free doxorubicin group and the micellar doxorubicin without sonication group, respectively. In the micellar doxorubicin with sonication group, the drug concentration in other tissues was lower than other groups (p<0.05). We conclude that dual frequency sonication improves drug release from micelles and increases the drug uptake by tumors due to sonoporation.

Keywords: Nanomicelles, Dual frequency ultrasound, Drug delivery

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Authors: Ghulam Murtaza, Kalsoom Farzana

Abstract:

The aim of this article is to narrate the utility of novel simulation approach i.e. convolution method to predict blood concentration of drug utilizing dissolution data of salbutamol sulphate microparticulate formulations with different release patterns (1:1, 1:2 and 1:3, drug:polymer). Dissolution apparatus II USP 2007 and 900 ml double distilled water stirrd at 50 rpm was employed for dissolution analysis. From dissolution data, blood drug concentration was determined, and in return predicted blood drug concentration data was used to calculate the pharmacokinetic parameters i.e. Cmax, Tmax, and AUC. Convolution is a good biwaiver technique; however its better utility needs it application in the conditions where biorelevant dissolution media are used.

Keywords: Convolution, Dissolution, Pharmacokinetics, Salbutamol sulphate

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Authors: Huiming Peng, Jianguo Wen, Hongwei Li, Jeff Chang, Xiaobo Zhou

Abstract:

NFκB activation plays a crucial role in anti-apoptotic responses in response to the apoptotic signaling during tumor necrosis factor (TNFa) stimulation in Multiple Myeloma (MM). Although several drugs have been found effective for the treatment of MM by mainly inhibiting NFκB pathway, there are no any quantitative or qualitative results of comparison assessment on inhibition effect between different single drugs or drug combinations. Computational modeling is becoming increasingly indispensable for applied biological research mainly because it can provide strong quantitative predicting power. In this study, a novel computational pathway modeling approach is employed to comparably assess the inhibition effects of specific single drugs and drug combinations on the NFκB pathway in MM, especially the prediction of synergistic drug combinations.

Keywords: Computational modeling, drug combination, inhibition effect, multiple myeloma, NFkB pathway.

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Authors: Tasnuva Tamanna, Aimin Yu

Abstract:

Application of nanoscience in biomedical field has come across as a new era. This study involves the synthesis of nano drug carrier with antibiotic loading. Based on the founding that polydopamine (PDA) nanoparticles could be formed via self-polymerization of dopamine at alkaline pH, one-step synthesis of rifampicin coupled polydopamine (PDA-R) nanoparticles was achieved by adding rifampicin into the dopamine solution. The successful yield of PDA nanoparticles with or without the presence of rifampicin during the polymerization process was characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, and Raman spectroscopy. Drug loading was monitored by UV-vis spectroscopy and the loading efficiency of rifampicin was calculated to be 76%. Such highly capacious nano-reservoir was found very stable with little drug leakage at pH 3.

Keywords: Drug loading, nanoparticles, polydopamine, rifampicin.

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Authors: Nagasamy Venkatesh Dhandapani

Abstract:

The objective of the present study was to develop sustained release oral matrix tablets of anti epileptic drug levetiracetam. The sustained release matrix tablets of levetiracetam were prepared using hydrophilic matrix hydroxypropyl methylcellulose (HPMC) as a release retarding polymer by wet granulation method. Prior to compression, FTIR studies were performed to understand the compatibility between the drug and excipients. The study revealed that there was no chemical interaction between drug and excipients used in the study. The tablets were characterized by physical and chemical parameters and results were found in acceptable limits. In vitro release study was carried out for the tablets using 0.1 N HCl for 2 hours and in phosphate buffer pH 7.4 for remaining time up to 12 hours. The effect of polymer concentration was studied. Different dissolution models were applied to drug release data in order to evaluate release mechanisms and kinetics. The drug release data fit well to zero order kinetics. Drug release mechanism was found as a complex mixture of diffusion, swelling and erosion.

Keywords: Levetiracetam, sustained-release, hydrophilic matrix tablet, HPMC grade K 100 MCR, wet granulation, zero order release kinetics.

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Authors: Azam Bayat, Aref Khalkhali, Ali Reza Mahjoub

Abstract:

In this research, a type of drug supplement was synthesized by a green route. This organic biomaterial was named Nutrition Bio-Shield Superfood (NBS). Due to the destructive effects of various infectious diseases, their increasing prevalence and the lack of appropriate medication for treatment, the present study aimed to evaluate antimicrobial properties of the NBS dietary supplement. In the study of the simple effect of concentrations on the inhibitory diameter of the growth of the common bacteria involved in infectious diseases of the human body, the highest diameter of the halo was related to the concentration of 100 mg/ml and the least of them was the concentration of 12.5 mg/ml dietary supplement. In general, the NBS drug supplement increases the level of immunity in human body.

Keywords: Drug supplement, biomaterial, antimicrobial, human body.

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Authors: Azwin Lubis, Rika Hapsari, Zahrah Hikmah, Anang Endaryanto, Ariyanto Harsono

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Erythema Multiforme Exudativum Major (EMEM) is one of the drug allergy diseases. Drug allergies caused by isoniazid rarely causes EMEM. Cutaneous reactions caused by isoniazid were obtained in 0.98% of patients, but the precise occurrence of Steven Johnson’s Syndrome (SJS) and Toxic Epidermolisis Necrolisis (TEN) due to isoniazid is not known for certain. We present this case to show hypersensitivity of isoniazid in a child. Based on the history of drug intake, physical diagnostic tests, drug elimination and provocation; we established the diagnosis of isoniazid hypersensitivity. The child showed improvement on skin manifestation after stopped isoniazid therapy.

Keywords: Erythema Multiforme Exudativum Major, hypersensitivity, elimination test, provocation test.

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Authors: Nagasamy Venkatesh Dhandapani, Amged Awad El-Gied

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

Keywords: Cefixime, β-Cyclodextrin, solid dispersions, kneading method, dissolution, release kinetics.

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Authors: Qin Wei

Abstract:

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

Keywords: Approaches, barriers, drug abuse, Canada, immigrant youth.

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