Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Egyptian Russian University, Cairo, Egypt.
Pharm Dev Technol. 2020 Nov;25(9):1081-1089. doi: 10.1080/10837450.2020.1795192. Epub 2020 Jul 27.
Silymarin has a short half-life (4-6 hours) which leads to necessity of frequent administration. Besides, it suffers from intestinal degradation. Thus, our study aims to formulate encapsulated floating microspheres using different polymers as HPMC, EC and a blend of them. Emulsion solvent evaporation technique was applied for preparation of microspheres. Parameters considered during preparation are drug: polymer ratio and emulsifier concentration. Selected formulations were characterized by SEM and subjected for assessment by drug entrapment efficiency, buoyancy for 12 hr, drug release, kinetics of release and stability. bio-equivalence study was performed using albino rabbits. Formula F24 (treatment II) exhibited high % buoyancy (73.4), higher t (190.7 day), high C (1021.3 ng/ml) and T (6 h) with a significant difference between it and treatment I (Silymarin plus) after carrying out ANOVA study. Also formula F24 exhibited MRT (hr) equal 9.44 ± 0.03 and high relative bioavailability RB% (227%), which indicates promising microspheres that could be used for effective management of liver disease.
水飞蓟素半衰期较短(4-6 小时),需要频繁给药。此外,它还会在肠道中降解。因此,我们的研究旨在使用不同的聚合物(如 HPMC、EC 及其混合物)来制备包封的漂浮微球。采用乳化溶剂蒸发技术制备微球。在制备过程中考虑了药物:聚合物比和乳化剂浓度等参数。选择的配方通过 SEM 进行了表征,并进行了药物包封效率、12 小时漂浮率、药物释放、释放动力学和稳定性评估。使用白化兔进行了生物等效性研究。配方 F24(治疗 II)表现出高漂浮率(73.4%)、更长的 t1/2(190.7 天)、更高的 Cmax(1021.3ng/ml)和 Tmax(6 小时),与治疗 I(水飞蓟素加药)相比具有显著差异,在进行方差分析后。此外,配方 F24 还表现出 MRT(小时)等于 9.44±0.03 和高相对生物利用度 RB%(227%),这表明这种微球具有很大的潜力,可用于有效治疗肝脏疾病。