Formulation Development and Evaluation of Lansoprazole Mucoadhesive Microsphere

Abstract

Lansoprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but rather suppress gastric acid secretion by specific inhibition of the (H+,K+)-ATPase enzyme system at the secretary surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. The aim of the present study was to develop lansoprazole loaded thiolated chitosan microspheres were prepared by emulsifying method using liquid paraffin light and heavy in ratio of 50:50 as a dispersing medium and glutaraldehyde used as a cross-linking agent. The prepared microspheres were evaluated for mean particle size and particle size distribution, drug content, mucoadhesion measurement and in-vitro drug release. FT-IR spectroscopic analysis was performed to ascertain drug polymer interaction. The release profiles showed first order release behavior up to 12 hours where the highest drug release was 88.89 % of the lansoprazole loaded in the thiolated chitosan microspheres, indicating a strong crosslinking between chitosan and glutaraldehyde. From the results of the present investigation it may be concluded that drug loaded chitosan microspheres can be prepared by a simple technique which avoids the use of complex apparatus and special precautions.

Keywords: Lansoprazole, Thiolated chitosan, Microspheres, Glutaraldehyde, Mucoadhesion measurement