Ranitidine hydrochloride stomach specific bouyant microsponge: Preparation, in-vitro characterization, and in-vivo anti-ulcer activity

Abstract

Ranitidine HCl (RTD) is the safest drug used to treat a life-threatening disease gastric ulcer. Therefore, sustained-release gastric buoyant microsponges of RTD were prepared by employing a double emulsion method. In the formulation of these microsponges eudragit (EGT) was a polymer, xanthan gum (XG) was used to impart non collapsible structure to microsponges, and tween 80 was used as an emulgent and all prepared microsponges were characterized for in-vitro studies and the best microsponge was evaluated for in-vivo antiulcer activity in albino rat model. All RTD microsponges exhibited appreciable in-vitro floating behavior and also showed initial burst release followed by sustained release of RTD in an acidic medium. However, microsponge formulation with RTD to EGT ratio (1:1) illustrated comparatively high in-vitro drug release (71.9% ± 2.79 in 12 h) and it also demonstrated appreciable production yield (81.3% ± 1.92), drug content (60.03% ± 1.81), and entrapment efficiency (68.2% ± 1.40). SEM study revealed the formation of RTD microsponge. Furthermore, In-vivo anti-ulcer activity study results showed that the studied microsponge exhibited more protective and healing effects in induced gastric ulcers in albino rats than pure RTD. Thus, it could be concluded that the gastric buoyant microsponge could be a useful approach to improve the anti-ulcer effect of RTD.