Formulation and Characterization of Gastroretentive Mucoadhesive Tablets for Treatment of Gastroparesis

Resumo

The aim of the present research work was to formulate and characterize gastroretentive mucoadhesive tablets of lacidipine (LCDP) intended for the treatment of gastroparesis. Polymers such as sodium alginate, HPMC K4M, carbopol 974P, and chitosan were utilized in LCDP formulation to ensure gastric retention up to 8 h. Direct compression method was adopted in preparation of mucoadhesive tablets. Prior to compression, powder blends were evaluated in order to check their flow and compression properties. Fourier transform infrared spectroscopy and differential scanning calorimetry measurements were performed to assess the compatibility of LCDP with polymers. Tablets were characterized with respect to the uniformity of weight, hardness, friability, drug content, swelling index, surface pH and in-vitro drug release. All formulations exhibited acceptable physicochemical properties. Formulation F4 exhibiting in-vitro drug release of 95.510% was selected as the optimized formulation and was further characterized by scanning electron microscopy. In vitro dissolution data was fitted to various kinetic models, and formulation F4 was found to display non-Fickian mechanism of drug release. No major change was observed in drug release and drug content upon storage of optimized formulation under accelerated aging conditions. The obtained results revealed that carbopol 974P and chitosan can be used in combination to formulate gastroretentive mucoadhesive LCDP tablets.