Posted by admin on Apr 30, 2015 in |
Enzymes are identified as key catalysts in various processes occurring within the living cells. The role of various enzymes is constantly investigated to find their novel applications. Nitrilase is one such enzyme which carries out the hydrolysis of carbon-nitrogen bonds except for amides. This catalytic property of nitrilase is exploited to generate corresponding chiral carboxylic acids. These chiral molecules can be employed in various drug synthesis schemes. Nitrilase have been reported from various microorganisms with variable catalytic properties. With an objective to explore microorganisms which produce nitrilases and able to catalyze aromatic nitriles, screening of microorganisms from soil was carried out. Out of five soil sampling sites, screening from the soil sample taken from benzonitrile manufacturing industry (Anami Organics Ltd. Valsad, Gujarat-India) resulted in isolation of microorganism which was able to use benzonitrile as substrate and was positive for nitrilase enzyme assay which was done by modified indophenol method. The microorganism was later identified to be Bacillus thuringiensis using 16s rRNA and biochemical analysis. Nitrilase is present as an...
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Posted by admin on Apr 30, 2015 in |
The main aim of the present investigation was to evaluate transdermal potential ethosomes bearing anti-diabetic drug Gliclazide. Total eight formulations (F1-F8) of ethosomes were prepared by using cold method with three different concentrations of phospholipid (0.5, 1, 2 % w/w) and ethanol (10, 20, 30 % v/v) and it was compared with hydroethanolic solution. They were evaluated for vesicular shape, size, entrapment efficiency and in-vitro studies. The formulation F6 (ethanol 20 % v/v and phospholipid (1 % w/w) was selected as the best formulation due to its optimum vesicle size, entrapment efficiency, less turbidity and maximum in- vitro release. The stability studies performed on F6 formulation at two different temperatures of 25º ± 2ºC and 4º ± 2ºC for the period of 6 months also shows the satisfactory results. It was further incorporated into gel using carbopol 934 (1, 1.5, 2 % w/w) as a base. The carbopol concentration of 1.5% w/w gives the maximum in-vitro release of 96.06 ± 0.16 % in dialysis membrane and ex-vivo release of...
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Posted by admin on Apr 30, 2015 in |
This research work deals with the development and evaluation of a floating pulsatile drug delivery system used in the treatment of hypertension intended as chronopharmacotherapy. Serious cardiovascular complications have been seen in majority of individuals with early morning-surge in blood pressure. The floating- pulsatile concept can help to deliver the drug at definite place and time when symptoms of disease are more critical. The system consisted of three different parts, a core tablet, containing the active ingredient, an erodible outer shell and a top cover buoyant layer. The dry coated tablet consists in a drug-containing core, coated by a hydrophilic erodible polymer (HPMC E50 and lactose) which is responsible for a lag phase in the onset of pulsatile release. The buoyant layer, prepared with Methocel E50, Carbopol 934P and sodium bicarbonate, provides buoyancy to increase the retention of the oral dosage form in the stomach applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The developed formulations were evaluated for...
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Posted by admin on Apr 30, 2015 in |
Matrix metalloproteinase 12 (MMP-12) inhibitions is an important research topic because of its wide range of associated health implications. The interaction mode of a series of pyridinone compounds with MMP-12 has been studied using molecular docking and 3D-QSAR approaches. Flexible docking was used for the determination of active conformation and molecular alignment. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used to develop 3D-QSAR models of 64 pyridinone-based compounds. The q2 values were 0.552and 0.542 for both CoMFA and CoMSIA models, respectively. The ability of these models was validated by 16 compounds of the test set. The resulting contour maps produced by the best CoMFA and CoMSIA models were used to identify the structural features relevant to the biological activity in this series of compounds. FlexX were employed to dock the inhibitors into the active site of the MMP-12 and these docking studies revealed the vital interactions and binding conformation of the inhibitors. The results demonstrate that combination of ligand-based and receptor-based modeling is...
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Posted by admin on Apr 30, 2015 in |
Ficus cyathistipula Warb. growing in Egypt is an evergreen tree, reaching up to six meters high. The macro- and micromorphological characters of the stem, leaf and fruit of the plant have been studied with the aim to find the diagnostic features and pointed towards their identification in both entire and powdered forms: partly united, leafy and conspicuous stipules, numerous ca-oxalate crystals, collateral vascular bundles with group of intraxylary phloem, mucilage and tannin cells, laticiferous vessels were the most significant. A total of 60 RAPD fragments have been recorded when DNA of the plant under investigation was amplified using eleven decamer primers designed for the genetic characterization. Furthermore, proximate analysis for the leaves was carried out to facilitate the detection of the quality and uniformity of the plant where the results (g %) showed a total ash (13.06), acid insoluble ash (0.58), water soluble ash (12.39), crude fiber (38) and moisture content...
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