Jafar Mohammed, Salahuddin Mohammed, Khan Mohd Sajjad Ahmad, Alshehry Yasir, Alrwaili Nazar Radwan, Alzahrani Yazeed Ali, Imam Syed Sarim, Alshehri Sultan
Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 34212, Saudi Arabia.
Department of Clinical Pharmacy Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 34212, Saudi Arabia.
Pharmaceutics. 2021 Dec 6;13(12):2094. doi: 10.3390/pharmaceutics13122094.
The current study aimed to develop a luteolin gastric floating microsponge for targeting . The microsponge formulations were prepared by a quasi-emulsion method, and then evaluated for various physicochemical variables. The best microsponge was further assessed for drug-polymer interactions, surface morphology, in vivo floating, and in vitro anti activity. The formulation which exhibited comparatively good production yield (64.45% ± 0.83), high entrapment efficiency (67.33% ± 3.79), prolonged in vitro floating time (>8 h), and sustained in-vitro drug release was selected as the best microsponge. The SEM study revealed that the best microsponge was spherical in shape and has a porous surface with interconnecting channels. DSC and XRD studies demonstrated the dispersion of luteolin in the polymeric matrix of the microsponge. Ultrasonography confirmed that the best microsponge could in the rat stomach for 4 h. The in vitro MIC results indicate that the anti activity of the best microsponge was almost doubled and more sustained compared to pure luteolin. To conclude, it can be said that the developed luteolin gastric floating microsponge could be a better option to effectively eradicate infections and the histopathological and pharmacodynamic assessments of our best microsponge can be expected to provide a rewarding outcome.
本研究旨在开发一种用于靶向的木犀草素胃漂浮微球。通过准乳化法制备微球制剂,然后对各种物理化学变量进行评估。对最佳微球进一步评估药物 - 聚合物相互作用、表面形态、体内漂浮情况和体外抗菌活性。选择产量相对较高(64.45% ± 0.83)、包封率高(67.33% ± 3.79)、体外漂浮时间延长(>8小时)且体外药物持续释放的制剂作为最佳微球。扫描电子显微镜研究表明,最佳微球呈球形,表面有相互连通的多孔通道。差示扫描量热法和X射线衍射研究证明了木犀草素在微球聚合物基质中的分散情况。超声检查证实最佳微球可在大鼠胃内停留4小时。体外最低抑菌浓度结果表明,与纯木犀草素相比,最佳微球的抗菌活性几乎提高了一倍且更持久。总之,可以说所开发的木犀草素胃漂浮微球可能是有效根除感染的更好选择,预计对我们最佳微球的组织病理学和药效学评估将产生有益结果。