DRUG DISCOVERY: AN APPRAISAL

The process of drug discovery and development has undergone radical changes over the years. Introduction of several novel technologies in genomics, proteomics and other omics areas have enabled drug target identification and validation more specific. In silico virtual screening and other computational chemistry methods like QSAR (Quantitative Structure-Activity Relationship) and QSPR (Quantitative Structure-Property Relationship) have enabled the emergence of new drugs with minimal toxicity and higher efficacy in this post-genomics era. Moreover, initiative like Open Source Drug Discovery (OSDD) is playing a promising role in accelerating the pace of drug discovery process. Better understanding of these methods and initiatives by researchers will kindle interest towards adopting it. Hence, by this review, we intend to present a comprehensive view of overall transition and modernization of the drug discovery process and it's impacts on the scientific community.Â

Cerebral protection for the preclinical evaluation of a vascular graft in sheep carotid artery model

A protocol for cerebral protection without systemic hypothermia to aid the safe, smooth and fast recovery of sheep used for the preclinical evaluation of a prosthetic vascular graft in the carotid artery is presented in this study. Ten adult Ramnad white sheep (33.

AN ASSESSMENT ON BUCCAL MUCOADHESIVE DRUG DELIVERY SYSTEM

Buccal drug delivery system (BDDS) has won a variety of exposure and traction as it possesses plenty of advantages and benefits as evaluate to different mucosal drug delivery systems. Buccal path for systemic drug delivery, the use of mucoadhesive polymers twill significantly increase the efficacy of many tablets, has been of outstanding interest over the previous couple of decades. This article affords a precise of BDDS mechanisms, consisting of a composition of the oral mucosa, delivery mechanism, numerous forms of BDDS, formulation, assessment and application of BDDS. Additionally, this text affords a precis over the patents, advertised products and destiny factors of BDDS. In this evaluation article, we've got tried to assemble the maximum significant reports (1988 to 2021) of formulation, assessment, application, patents of BDDS. This review will help pharmaceutical researchers to clarify the potential of BDDS to overcome the various existing drug delivery dispute like the efficiency of absorption, permeability and bioavailability of drugs

FIRST COMPLETE GENOME SEQUENCE OF OCULAR ISOLATE CARRYING BLAVIM-2 MEDIATED MULTI-DRUG-RESISTANT(MDR) PSEUDOMONAS AERUGINOSA VRFPA04 FROM INDIA AND TWO DRAFT GENOME SEQUENCE OF OCULAR ISOLATES PSEUDOMONAS AERUGINOSA VRFPA03 AND VRFPA05 HARBORING NOVEL BLA

Objective: Ocular infections caused by Multi-Drug resistant (MDR) Pseudomonas aeruginosa are rare but increasingly identified recently. In this context, we have applied Next Generation Sequencing (NGS) based whole genome analysis on three ocular isolates of MDR P. aeruginosa to explore the drug resistance determinants and genomic level variations.Methods: Three ocular isolates namely P. aeruginosa VRFP03, VRFPA04 from two different Keratitis patients (corneal button) and VRFPA05 isolated from the intraocular specimen (Vitreous humor) collected from an endophthalmitis patient was included in this study. Phenotypically VRFPA03, VRFPA04, VRFPA05 showed resistant to a wide group of antibiotics and hence they were taken up for Ion Torrent-PGM based whole genome study.Results: Here, we report the first complete genome sequence of MDR P. aeruginosa VRFPA04 isolated from the Indian keratitis patients clinical specimen (corneal button) submitted to L & T Microbiology Research Centre, Vision Research Foundation, Sankara Nethralaya, Chennai, Tamil Nadu, India. The circular chromosome of P aeruginosa VRFPA04 was published under the NCBI accession number CP008739.2. Two Draft genome sequences of MDR P. aeruginosa VRFPA03 and VRFPA05 were published under the NCBI accession number ATNK01000000.1 and AXZJ01000000.1 respectively.Conclusion: Preliminary genomic analysis on P. aeruginosa VRFPA03, VRFPA04 and VRFPA05 revealed the presence of Metallo Beta-lactamase (MBL) genes blaDim-1, blaVim-2 andblaGes-9 genes respectively. These MBL genes were concordance with a phenotypic pattern of carbapenem resistance among VRFPA03, VRFPA04 and VRFPA05 strains, respectively. We are proud to share that this is the first of its kind to report blaDIM-1 from an Indianisolate especially from an Ocular origin.Â

GENETIC VARIATIONS IN POLYCYSTIC OVARIAN SYNDROME DISEASE

objective: Polycystic ovary syndrome (PCOS) is one of the common endocrine disorders among women of reproductive age with a prevalence ofapproximately 5-10% worldwide. PCOS is a complex genetic disorder caused by several genes and environmental factors. The aim of this study is toprovide an overview on variations in PCOS-associated genes based on underlying geneticsMethods: Detailed literature screening was performed in PubMed. Manual curation process was adopted to extract the information on PCOS,associated genes, mechanism of association, details of the association, significance of association mentioned in the papers were carefully capturedaccording to the authors' interpretation of the results.Results: The detailed literature study revealed several genes and the genetic variations in PCOS and its critical effects, such as ovarian failure, obesity,spontaneous abortion, recurrent pregnancy loss, insulin resistance, and hyperandrogenim. The causal genetic variants were assembled at variouslevels, including mutation, single nucleotide polymorphism, etc., in PCOS and the associated phenotypic effects.Conclusion: The genetic variations play an important role in the pathogenesis of PCOS across different ethnicities, as it is associated with various otherendocrine disorders including diabetes, insulin resistance, cardiovascular diseases, hyperandrogenism, reproductive disorders, etc. The underlyingmechanism and the network help in identifying the candidate genes or biomarkers in the disease conditions.Keywords: Polycystic ovary syndrome, Gene, Mutation, Polymorphism, Single nucleotide polymorphism

Analysis of Metallised Propellant Ignition Process under Conductive Heating

Ignition of a composite aluminised propellant (AP-HTPB-Al) in stagnant hot air is analysed theoretically, based on solid phase and gas phase theories. According to solid phase theory, ignition is due to reaction of the propellant in the solid phase at elevated temperatures. One-dimensional transient solid phase energy equation is solved to obtain the surface temperature profile of the propellant. By gas phase theory, an exothermic gas phase reaction, adjacent to the propellant surface, is considered responsible for the ignition. The changes in temperature and concentrations in the gas phase and the temperature profile below the propellant surface during the pre-ignition induction period are considered. Equations of energy and concentrations of reactants have been solved to obtain the species concentration and temperature profiles in the gas phase. An experimental investigation of the ignition of AP-HTPB-Al propellant is also carried out in a shock tube under end-mount conditions. Pressure and temperature ranges were 6-16 bar and 1500-3000 K, respectively. A comparison of the experimental data with predicted results shows that the ignition in an oxidizing atmosphere is by gas phase reaction, whereas in an inert atmosphere, solid phase reaction may be predominant

Bearing Capacity of A Strip Footing Resting On Treated And Untreated Soils

Expansive soils are highly susceptible to volumetric changes leading to rapid loss in the bearing capacity of footings resting on them. Among several techniques available to treat expansive soils, lime or fly ash stabilization gained prominence during the past few decades due to its abundance and adaptability. Chemical stabilization is widely used to treat expansive soils as it develops base exchange and cementation processes between clay particles.When expansive soils are treated with chemicals, it is essential to obtain the load-settlement response of footing resting on stabilized ground. In this study, Finite Element Analysis is performed using the commercial software, PLAXIS 2D, to obtain the load-settlement response of a strip footing resting on untreated and treated expansive soil. The bearing capacity of strip footing resting on treated soil is found to be about 150% higher than that of footing resting on untreated soil

Comparison of vaginal and oral misoprostol, for the induction of labour in women with intra-uterine foetal death

Background: Misoprostol is a prostaglandin E1 analogue, a methyl-ester of prostaglandin E1 additionally methylated at C-16. Misoprostol is an effective myometrial stimulant of pregnant uterus, selectively binding to prostanoid receptors. The objective of the study was to compare the efficacy of vaginal and oral misoprostol for the induction of labour in women with intra-uterine foetal death (IUFD).Methods: A prospective randomised clinical trial, comparing 50µg oral and 50µg vaginal misoprostol, six hourlies for a maximum of four doses for the induction of labour in women with IUFD. All patients with IUFD after 28 weeks without previous uterine surgeries, without contraindications for prostaglandins are included in the study. The study was conducted in the Department of Obstetrics and Gynecology MVJ Medical College and Research Hospital, Hoskote. Bangalore from June 2012 to June 2015. It is a tertiary institution serving predominantly rural population. The primary outcome measure was the induction to delivery time, secondary all complications were noted.Results: Twenty-five women were randomised to the vaginal route and twenty-five to the oral route. The induction to delivery time was longer with vaginal misoprostol 10.5±4.03 compared to oral misoprostol (9.58±4.9). There was no significant difference in the amount of misoprostol needed to achieve successful induction in the two groups. 3 patients needed oxytocin augmentation to complete the induction of labour. There were no cases of failed induction. The systemic side effects (shivering, diarrhoea, vomiting and pyrexia) were more common with oral misoprostol (44.5%) compared to vaginal misoprostol (20%).Conclusions: Oral misoprostol achieved successful induction of labour in women with IUFD in a shorter time than vaginal misoprostol. Both routes are equally effective in termination of pregnancy. Sublingual route is easy to administer, patient compliant, no need for internal examination, less chance of labour dysfunction, less chance of post-partum sepsis

Polarization-Current-Based FDTD Near-to-Far-Field Transformation

A new near-to-far-field transformation algorithm for three-dimensional finite-different time-domain is presented in this article. This new approach is based directly on the polarization current of the scatterer, not the scattered near fields. It therefore eliminates the numerical errors originating from the spatial offset of the E and H fields, inherent in the standard near-to-far-field transformation. The proposed method is validated via direct comparisons with the analytical Lorentz-Mie solutions of plane waves scattered by large dielectric and metallic spheres with strong forward-scattering lobes.Comment: 8 pages, 2 figures. Submitted to publis