Chitosan loaded mucoadhesive microspheres of Glipizide fortreatment of type 2 diabetes mellitus: In vitro and in vivo evaluation

[摘要] The objective of the present investigation was to design chitosan loaded mucoadhesive microspheres of glipizide for treatment of type 2 diabetes mellitus: in vitro and in vivo evaluation. Type 2 diabetes mellitus is a heterogeneous disease of polygenic origin and involves both defective insulin secretion and peripheral insulin resistance. Despite the availability of new agents for treatment of type 2 diabetes mellitus, oral sulfonylureas remain a cornerstone of therapy, because they are relatively inexpensive and are well tolerated. Glipizide is a potent, rapid-acting with short duration of action and well tolerated second-generation sulfonylurea effective in reducing postprandial glucose levels. However, risk of postprandial hypoglycemia and post-meal glucose excursions, if always associated with the use of glipizide for treatment of type 2 diabetes mellitus. Since, the site of absorption of glipizide is from stomach thus dosage forms that are retained in stomach by mucoadhesion; would increase absorption, improve drug efficiency and decrease dose requirements. Microsphere carrier systems made by using polymer chitosan having strong mucoadhesive. Microspheres were prepared by simple emulsification phase separation technique. On the basis of the preliminary trials 32 full factorial designs were employed, to study the effect of independent variable X1 polymer-to-drug and the stirring speed X2 on dependent variables percentage mucoadhesion, drug entrapment efficiency and particle size. The optimized formulation exhibited a high drug entrapment efficiency of 60%, swelling index 0.42, Percentage of mucoadhesive after 1 hour 62% and the drug release was also sustained for more than 10 hours. In vivo testing of the mucoadhesive microspheres to albino Wistar rats demonstrated significant hypoglycemic effect of glipizide.

[学科分类] 药理学