Purpose: The purpose of the present investigation was to formulate and evaluate microencapsulated glipizide produced by the emulsion-solvent evaporation method, Method: Microspheres were prepared using polymethacrylate polymers (Eudragit ® RS 100 and RL 100) by solvent evaporation method and characterized for their micromeritic properties and drug loading, as well as by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy. In vitro release studies were performed in phosphate buffer (pH 7.4). Result: The resulting microspheres obtained by solvent evaporation method were white and free flowing in nature. The mean particle size of microspheres ranged from 420-660 µm and the encapsulation efficiencies ranged from 40.27-86.67 %. The encapsulation efficiency was also found to be dependant on nature of polymer used in the formulation. The infrared spectra confirmed the stable character of glipizide in the drug-loaded microspheres. Scanning electron microscopy revealed that the microspheres were spherical in nature. From the in vitro drug dissolution studies it was found that the sustaining effect of microspheres depended on the polymer concentration, amount of dispersant used and the type of polymer used in the formulation. The mechanism of drug release from the microspheres was found to be non-Fickian type. Conclusion: Eudragit ® microspheres containing glipizide could be prepared successfully by using an emulsion solvent evaporation technique using polymethacrylate polymers, which will not only sustain the release of drug but also manage the complicacy of the diabetes in a better manner.
Lincomycin hydrochloride is a systemic antibiotic, which is active against most common gram positive bacteria. It has proved to be excellent for infectious diseases like acne, anthrax, pneumonia, and also for the treatment of furunculosis, carbuncles, impetigo, burns and wounds, carrying to gram positive bacteria. Gels were prepared using carbopol 940 as gelling agent, and isopropyl myristate and dimethyl sulfoxide as permeation enhancer. The formulations were evaluated for drug content, viscosity, pH, extrudability, homogeneity, skin irritation test, spreadability, and gel strength. A formulation containing 1.5% carbopol with 10% isopropyl myristate, showed better in vitro skin permeation through abdominal mouse skin, and was found to be the best.
Abstract. Glibenclamide (GL)-loaded microcapsules (MC) and transdermal patches (TDP) were formulated and in vitro and in vivo parameters compared to find out the best route of drug administration. The formulation TDP1 having a drug-polymer ratio 1:1 showed comparatively higher GL release and better permeation across mice skin (p<0.05). From the comparative study, it was concluded that the transdermal system of GL produced better improvement compared to oral microcapsule administration (p<0.05). The transdermal system exhibited comparatively slow and continuous supply of GL at a desired rate to systemic circulation avoiding metabolism, which improved day-to-day glycemic control in diabetic subjects. Transdermal system of GL exhibited better control of hyperglycemia and prolonged plasma half-life by transdermal systems (9.6±1.2 h) in comparison with oral microcapsule (5.84±2.1 h), indicating that the drug, when administered by transdermal systems, will remain in the body for a longer period. From the glucose tolerance test, transdermal route effectively maintained the normoglycemic levels in contrast to the oral group (MC1), which produced remarkable hypoglycemia ranging from −12.6±2.1% to −18±2.3%. The significantly high (p<0.05) area under the curve values observed with transdermal system (1,346.2±92.3 ng ml −1 h −1 ) also indicate increased bioavailability of the drug from these systems compared to the oral route (829.8±76.4 ng ml −1 h −1 ).
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