Galactomannan gum coated mucoadhesive microspheres of glipizide for treatment of type 2 diabetes mellitus: In vitro and in vivo evaluation

Abstract

Type 2 diabetes mellitus is a heterogeneous disease of polygenic origin and involves both defective insulin secretion and peripheral insulin resistance. Studies have shown that post-meal hyperglycemic spikes are associated with increased cardiovascular mortality in type 2 diabetes. Over the past decade, a major interest in control of postprandial glucose excursion has emerged and a plethora of new medications that specifically target postprandial hyperglycemia were discovered. 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. However, hypoglycemia is a major safety concern with sulfonylureas and it is one major risk factor requiring hospitalization. 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 dose missed before meal; are 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 galactomannan having strong mucoadhesive properties and easily biodegradable could be an attractive strategy to formulate. The purpose of this research work is to formulate galactomannan coated mucoadhesive microspheres of glipizide and systematically evaluate its in vitro characteristics and in vivo performance for sustained glucose lowering effect and improvement in diabetic condition as compared to immediate release of glipizide.

Pharmaceutical suspension containing both immediate/sustained-release amoxicillin-loaded gelatin nanoparticles: preparation and in vitro characterization

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An Improvement of Efficacy of Moxifloxacin HCl for the Treatment of Bacterial Keratitis by Formulation of Ocular Mucoadhesive Microspheres

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Study of the Mucoadhesive Potential of Carbopol Polymer in the Preparation of Microbeads Containing the Antidiabetic Drug Glipizide

“…In 2009, Hosmani et al (2) optimized SR microspheres of glipizide by using the factorial design method and reported the effect of the combinations of polymers (polycarbophil and sodium alginate) on drug entrapment (75%), yield (97%) swelling index (2.2), and mucoadhesion (100%), and the release of the drug was extended up to a period of 8 h. It showed a hypoglycemic effect by the oral glucose tolerance test (OGTT) test for a period of 1-9 h. Behera et al (42) prepared microspheres of glipizide with polymethacrylate and observed dissolution of the drug in alkaline pH and reported that the release of the drug was extended up to 8 h. There are some reports on the prolonged release of GLP from microspheres up to 24 h (33,43,44) in which the method of preparation of the products was quite time consuming and expensive in comparison with that of the present investigation.…”