Posted by admin on Mar 1, 2016 in |
Human eye is a challenging subject for topical administration of the drugs because of its peculiar anatomical arrangements of surface tissue and impermeability of the cornea. Topical instillation of drugs through eye drops is the most important and well-accepted route of administration for the treatment of various eye disorders. Conventional ophthalmic drug delivery systems often result in poor bioavailability and therefore poor therapeutic response. Several new preparations have been developed to prolong the contact time of the medicament on the ocular surface. Successful results have been obtained with inserts and collagen shields. However, these preparations have some disadvantages, such as poor patient compliance, especially by geriatric patients. This problem can be overcome by using in situ gel forming systems of polymers that exhibit reversible phase transition. Such system can be formulated as eye drops suitable for administration by instillation into the eye, which upon exposure to the eye converts to the gel phase. The advantage of these formulations is that unlike inserts and films they do not require sophisticated...
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Posted by admin on Mar 1, 2016 in |
The parts of the Nicotiana tabacum plant have been known to possess a wide range of biological activities. The purpose of the present study was to investigate the antibacterial activity, phytochemical screening and the antioxidant activity of aqueous and alcoholic extracts of the stem of Nicotiana tabacum. The antibacterial activity was observed against two gram positive bacteria (Bacillus amyloiquefaciens, Staphylococcus aureus) & two gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa) in its aqueous, ethanolic, acetone and methanolic extracts by agar well diffusion method where maximum antibacterial activity found to be present in the methanolic and ethanolic extract against Staphylococcus aureus with an inhibition length of 10.667±1.527 mm and 8±1.00 mm, respectively. Phytochemical screening of aqueous, ethanolic & methanolic extract revealed the presence of saponin, flavonoids and alkaloids. Flavonoid content in stem was found to be 838 mg QE/g of extract in the 80% of ethanol extract by aluminium chloride colometric method. Antioxidant activity was observed in order to estimate the superoxide dismutase, catalase, glutathione content, glutathione s transferase &...
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Posted by admin on Mar 1, 2016 in |
Emergence of Mycobacteria that are resistant to common antibiotics necessitate development of novel antibacterial drugs. The complexity of mycobacterial cell envelope plays an important role in its defense against antimicrobial activity of human immune system. The cell wall of Mycobacteria constitutes a set of carbohydrate-containing molecules. Glycosyltransferases, the glycan processing enzymes play a significant role in assembling these moieties. Targeting these enzymes could therefore interfere with the virulence of the pathogen thus leading to non-proliferation or its death. The significant role of these enzymes makes them novel targets for drug action. Natural products are important sources of pharmacologically relevant compounds. The present study has been undertaken to evaluate the inhibition potential of selected phytochemicals against glycosyltransferases of Mycobacterium. Fourteen antimicrobial phytochemicals were selected from the NCBI Pubchem Database. These phytochemicals were further screened using Lipinski’s rule of five. Molecular docking was performed to identify new potential inhibitors against Mycobacterial glycosyltransferases using Discovery studio 4.0 with these compounds. These sets of phytochemicals were further screened for toxicity using ADMET descriptors....
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Posted by admin on Mar 1, 2016 in |
Cefixime is more effective in treating multi drug resistant typhoid fever but the major limitation was its poor bioavailability with short half- life. The present investigation was attempted to develop a natural polymer based nanoparticles containing cefixime using gum kondagogu and chitosan as polymers for customising the drug release profile to achieve an effective therapeutic concentration by increasing its solubility and bioavailability. The cefixime nanoparticles were prepared by the modified coacervation method and evaluated for particle size, zeta potential, morphological studies (SEM, TEM and AFM), entrapment efficiency, in-vitro drug release studies and in-vitro antimicrobial efficiency studies. The prepared drug nanoparticles found to be average mean particle size in range from 80.6±3.5 to 230.6±7.3nm and entrapment efficiency was found to be 78.0±1.5 to 93.2±2.5%. The in-vitro drug release showed a biphasic pattern with initial burst release followed by sustained drug release up to 32h. The MIC50 of prepared formulation was one fold lesser than pure cefixime for Salmonella Typhi isolates. The disc agar diffusion (DAD) test confers that the zone...
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Posted by admin on Mar 1, 2016 in |
The compound 3-(1-(benzo[d]thiazol-2-ylimino) ethyl)-6-methyl-2H-pyran-2, 4(3H)-dione (3BTIEMPD) and its metal complexes were prepared and characterized by spectro-analytical techniques. Irving-Rossetti pH-metric technique was employed to determine the number of dissociable protons and chelation sites of the title compound. Hyper Chem 7.5 software was used to understand donor and acceptor properties of molecule. The molecule was built and the geometry optimization was carried out by using semiemperical PM3 method. The contour maps of highest occupied molecular orbitals (HOMO) and lowest unoccupied molecular orbitals (LUMO) and corresponding binding energy values were computed. The low binding energy for ionic species evident from computed values is an indication of higher possibility of compound to bind with metal ions through deprotonation. This is augmented from the results of spectro-analytical analyses of isolated solid metal complexes wherein the participation of azomethine nitrogen and the enol oxygen of pyran ring through deprotonation is envisaged. All the compounds were investigated for their antimicrobial activities against the Gram-positive and Gram-negative bacteria by disc diffusion method. It was found that the...
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