Development of apigenin loaded gastroretentive microsponge for the targeting of Helicobacter pylori

• Published in: Saudi pharmaceutical journal 2023-05, Vol.31 (5), p.659-668
• Main Authors: Jafar, Mohammed, Sajjad Ahmad Khan, Mohd, Salahuddin, Mohammed, Zahoor, Saira, MohammedHesham Slais, Hanan, Ibrahim Alalwan, Layali, Radhi Alshaban, Heba
• Format: Article
• Language: English
• Subjects: Apigenin; Buoyancy; Flavonoid; H. pylori bacteria; In-vivo activity; Microencapsulation; Original
• ISSN: 1319-0164; 2213-7475
• DOI: 10.1016/j.jsps.2023.03.006

The goal of the present work was to invent an apigenin-stacked gastroretentive microsponge to target H. pylori. The quasi-emulsion technique was used to prepare microsponges, which were then tested for various physicochemical properties, in-vivo gastric retention, and in-vitro anti-H. pylori study. The microsponge that demonstrated a comparatively good product yield (76.23 ± 0.84), excellent entrapment efficiency (97.84 ± 0.85), sustained in-vitro gastric retention period, and prolonged drug release were chosen for further investigations. The microsponge's SEM analysis showed that it had a spherical form, porous surface, and interconnected spaces. No drug-polymer interactions were detected in the FTIR investigation. Apigenin was found to be dispersed in the microsponge's polymeric matrix according to DSC & XRD investigations. Moreover, the microsponge in the rat's stomach floated for 4 h, according to the ultrasonography. The antibacterial activity of apigenin against H. pylori was nearly two folds more than the pure apigenin and had a more sustained release in the best microsponge, according to the in vitro MIC data, when compared to pure apigenin. To sum up, the developed gastroretentive microsponge with apigenin offers a viable alternative for the efficient targeting of H. pylori. But more preclinical & clinical studies of our best microsponge would yield considerably more fruitful results.