Posted by admin on Mar 31, 2019 in |
Chalcone based structures have many interesting biological properties like anti-malarial, anticancer, antiviral, antibacterial, antifungal, anti-hyperglycaemic and photo-cytotoxicity activities. In this study, the novel chalcone derivatives (1a-1l) have been synthesized and investigated for antimicrobial activities. The MIC results of antimicrobial activities reveal that one of the chalcone derivative (2-Br- and 4-OCH3– group) against specific bacteria are quite significant. 3D QSAR, three dimensional quantitative structure activity is one of the most powerful technique which involves the quantitative relationship between the biological activity of a set of compounds and their three dimensional structural properties, using statistical correlation methods. Pharmacophore modelling and molecular docking play an important role in drug design. To elucidate the relationship between structures and its activity, field-based 3D QSAR analysis has been carried out of novel chalcone derivatives. Structural properties such as electrostatic, hydrophobic, aromatic, and hydrogen-bond donor and acceptor have been worked out for novel chalcone derivatives. To investigate the influence of drugstore, chalcone derivatives (1a-1l) have docked with receptor 2IOK and results displayed the highest Gscore of...
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Posted by admin on Mar 31, 2019 in |
Schizophrenia is a severe and disabling disorder which needs immediate administration of a suitable drug. Olanzapine, a BCS class II atypical antipsychotics drug of thienobenzodiazepine class is frequently prescribed to treat schizophrenia. The aim of the present investigation was to formulate mouth dissolving films of Olanzapine to improve its solubility and patient compliance. An inclusion complex of Olanzapine with 2-hydroxypropyl-β-cyclodextrin at a molar ratio of 1:1 enhanced solubility of the drug. A patient compliant MDF using Pullalan as a film-forming polymer was developed using the design of the experiment, 32 factorial design. The independent variables selected for optimization of MDF containing inclusion complex of 2-hydroxypropyl-β-cyclodextrin and Olanzapine were polymer concentration (3-5%) and plasticizer concentration (25-35%). The optimized film demonstrated optimum tensile strength of 3.91(gm/cm2), the disintegration time of 15.45 seconds and fast dissolution of 99.3% in 6 minutes. All the films formulated using solvent casting method were smooth and elegant in appearance. Rapid release of Olanzapine from MDFs indicated its suitability as an oral delivery system in the management...
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Posted by admin on Mar 31, 2019 in |
Indomethacin, an anti-inflammatory drug, exhibits poor water solubility and flow properties. Spherical agglomerates were prepared by crystallo-co agglomeration technique. Crystallization medium used for spherical agglomerates of Indomethacin consisted of acetone (good solvent); water (poor solvent); dichloromethane (bridging liquid). HPMC, PVP and PEG6000 this polymer were used in the agglomeration process. Spherical agglomerates were characterized by DSC, IR, XRD, and SEM. Micromeritic, dissolution behavior and compression studies were carried out. For optimization study Box Behnken Design used. Heckle plot studies showed low mean yield pressure and a low value indicating excellent compressibility and compatibility of agglomerates. Process variables such as an amount of bridging liquid, stirring speed and polymer ratio were optimized. The dissolution profile of the spherical agglomerates was compared with pure Indomethacin. Spherical agglomerates exhibited decreased crystallinity and improved micromeritic properties. The dissolution of the spherical agglomerates was improved compared with pure Indomethacin sample....
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Posted by admin on Mar 31, 2019 in |
Cyclobenzaprine hydrochloride (CBZ) is a muscle relaxant. It has 33% bioavailability due to its first pass effect and hence posses problems in the development of oral sustained release formulations. Mucoadhesive thermo reversible in-situ nasal gel of Cyclobenzaprine HCl was designed and developed to sustain its release due to the increased nasal residence time of the formulation. Poloxamer 407 (PF 127) was selected as it has excellent thermo sensitive gelling properties. HPMCK4M was added to impart mucoadhesive to the formulation, and PEG 400 was used to enhance the drug release. 32 Factorial designs were employed to assess the effect of concentration of HPMCK4M and PEG 400 on the performance of in-situ nasal gel systematically and to optimize the formulation. An optimized in-situ nasal gel was evaluated for appearance, pH, drug content, gelation temperature, mucoadhesive force, viscosity and ex-vivo permeability of drug through nasal mucosa of a goat. Additionally, this formulation was proved to be safe as histopathological studies revealed no deleterious effect on nasal mucosa of a goat after prolonged...
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Posted by admin on Mar 31, 2019 in |
Biofilms are protective organic extracellular polymeric substances secreted by a microbial population which prevents the penetration of antimicrobial substances such as antibiotics. The existence of biofilms has become a significant problem in the case of infections as well as industrial processes. Although, biofilms may act as an advantage to the microbial community, they are found to cause food spoilage, unpleasant odors, pipe blockage, infections, etc. Biofilms play a crucial role in causing persistent UTIs which undergo frequent relapses, seen most commonly in women, children and aging adults. In the present investigation, bacterial samples isolated from UTI samples of infected patients were characterized. The capacity of the UTI isolates to form biofilms is analyzed using biofilm assay done by subjection of samples to primary and secondary screening by ELISA plate reader. Further on, N-acyl homoserine lactone (AHL), an autoinducer responsible for the formation of biofilms in gram-negative bacteria was extracted and estimated colorimetrically and spectroscopically by using Fourier Transform Infrared Spectroscopy (FT-IR). The AHL that was extracted showed a characteristic...
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