Formulation Factors in influencing The Development of Gastro-retentive Mucoadhesive Tablets

Ketoconazole (KZ) is a useful antifungal drug belonging to the imidazole group. its clinical use has been limited due to poor absorption, as it is primarily absorbed in the stomach and upper small intestine. Once the drug passes through the stomach via gastric emptying, its absorption significantly decreases, leading to reduced bioavailability. This study aimed to develop gastro-retentive mucoadhesive tablets by testing different drug-polymer ratios and assessing their physical and functional characteristics. Nine formulations (F1-F9) were created as gastro-retentive mucoadhesive tablets using sodium alginate (Na Alg) and Carbopol 934 (Carb 934). The powder blend was tested for flow properties, and the resulting tablets were assessed for thickness, hardness, weight variation, friability, mucoadhesion time, swelling index, mucoadhesive strength, and in vitro drug release. Results revealed that Carb 934's high molecular weight and cross-linking promote prolonged mucoadhesion, leading to extended drug release. Formulations with higher Na Alg contents demonstrated more swelling but less mucoadhesion time than those containing Carb 934. Together, Carb 934 and Na Alg provided controlled drug release due to the balanced properties of the polymers. This study explored mucoadhesive gastro-retentive tablets of ketoconazole, which showed enhanced gastric retention and extended release. These properties are expected to improve the drug’s absorption and bioavailability, potentially offering a more effective therapeutic option.