Abstract. The present investigation was aimed at exploitation of the mucoadhesive potential of carbopol 934P polymer in developing microbeads of glipizide (GLP) for its effectivity in controlling blood sugar in diabetic patients. Various batches of GLP beads were prepared by an emulsion-solvent evaporation technique using the release-retarding polymer carbopol and subjected to a systematic evaluation such as physical characterization, ex vivo mucoadhesion, hydration and erosion test, and in vitro drug release; and instrumental and in vivo studies were performed with the best formulation. The highest yield and loading efficiency were observed as 94 and ∼90%, respectively. The mean particle size of the microbeads ranged from 832 to 742 μm. The oval shape of the microbeads with slight roughness was apparent in the SEM micrograph. The release period was extended till 18 h. In vitro release of the drug from the beads followed the diffusion and erosion mechanism. In the oral glucose tolerance test (OGTT), there is a significant (p<0.01) reduction in fasting blood glucose levels in Wistar rat and guinea pig in comparison with that using the marketed product. Results indicated that process parameters-drug-polymer ratio, concentration of the surfactant, and stirring speed-controlled the various characteristics of the microparticles. The mucoadhesivity test ensured strong adherence of the beads to the mucosal membrane in pH 1.2 for a prolonged period. Owing to the mucoadhesivity of carbopol 934P, prolonged release of GLP and reduction of fasting sugar in the animal model were observed to a satisfactory level, and thus, management of diabetes in a better manner is expected with this new formulation.
The present work aims at the development of a low-cost controlled release system of glipizide beads embedded in pectin to overcome the problem of frequent dosing of drug. The method of preparation has been optimised by experimental design to achieve satisfactory responses with respect to controlling variables. The controlling variables are X1, drug-polymer ratio; X2, surfactant concentration and X3, isooctane-acetone ratio. The most effective combination is X1(1:6), X2(1%), X3(50:50). Various parameters such as mucoadhesivity and swellability of beads, characterisation, dissolution, stability, ex vivo absorption and in vivo (Oral glucose tolerance test in rat) studies were performed with the optimised product. The optimised product was found quiet satisfactory that showed yield of 86.78%, drug entrapment efficiency (DEE) of 87.38% and drug release was extended up to 18 h. The present formulation of glipizide is a promising multiparticulate system of glipizide with significant hypoglycemic effect, and moreover it was prepared rapidly with ease.
I n the recent past, a major interest in the control of blood sugar had been targeted to develop plenty of new formulations.The present work aims at the development of a low cost sustained release system of metformin hydrochloride embedded in microspheres of agar (Gelidium cartilagineum) to overcome the frequent dosing of the drug. Models were developed with respect to controlling variables (X 1 , drug: Polymer, X 2 , surfactant concentration, and X 3 , pH of phosphate buffer). The most effective levels of parameters were found as X 1 (1:2), X 2 (1.25%), X 3 (phosphate buffer pH 7.4). Instrumental analysis (Fourier transforms infra-red spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy), mucoadhesion study, toxicity test and in vivo study were performed with the optimized product. The best batch (A2) exhibited a high drug entrapment efficiency of 84.82 ± 1.23%, swelling index of 3.84 ± 0.38% and 86% of mucoadhesion after 12 h. The in vitro release was also sustained for more than 12 h.
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