Enhanced oral bioavailability and sustained delivery of glimepiride via niosomal encapsulation: in-vitro characterization and in-vivo evaluation
Enhanced oral bioavailability and sustained delivery of glimepiride via niosomal encapsulation: in-vitro characterization and in-vivo evaluation
复制标题
DOI：
10.1080/03639045.2017.1310224
复制
发表时间：
2017-01-01
影响因子：
3.4
通讯作者：
ElShebiney, Shaimaa Ahmed
中科院分区：
文献类型：
--
作者：
Mohsen, Amira Mohamed;AbouSamra, Mona Mahmoud;ElShebiney, Shaimaa Ahmed
本研究旨在研究格列美脲（GLM）囊泡的效力，旨在提高其口服生物利用度和降血糖功效。采用薄膜水化法制备了含非离子表面活性剂的囊泡，并对其进行了表征。使用透析技术进行体外释放研究。在四氧嘧啶诱导的糖尿病大鼠上进行体内药效学研究以及药代动力学评价。GLM囊泡具有较高的包封率（E. E. %）至98.70%，粒度直径范围为186.8 +/-18.69至797.7 +/-12.45nm，具有带负电荷的ζ电位（ZP）。与游离药物相比，不同的GLM囊泡制剂显示出延迟的体外释放。体内研究显示，与游离药物和市售产品相比，GLM囊泡在降低血糖水平（BGL）和在更长时间内维持GLM的治疗水平方面具有优势。载药囊泡的平均血浆AUC（0- 48 hr）与市售产品的AUC（0- 48 hr）无显著差异。与游离药物相比，负载GLM的囊泡的相对生物利用度提高了7倍。这些发现加强了囊泡用于增强口服生物利用度和通过口服给药延长GLM递送的潜在用途。
This study was designed to investigate the potency of niosomes, for glimepiride (GLM) encapsulation, aiming at enhancing its oral bioavailability and hypoglycemic efficacy. Niosomes containing nonionic surfactants (NIS) were prepared by thin film hydration technique and characterized. In-vitro release study was performed using a dialysis technique. In-vivo pharmacodynamic studies, as well as pharmacokinetic evaluation were performed on alloxan-induced diabetic rats. GLM niosomes exhibited high-entrapment efficiency percentages (E.E. %) up to 98.70% and a particle size diameter ranging from 186.8 +/- 18.69 to 797.7 +/- 12.45nm, with negatively charged zeta potential (ZP). Different GLM niosomal formulation showed retarded in vitro release, compared to free drug. In-vivo studies revealed the superiority of GLM niosomes in lowering blood glucose level (BGL) and in maintaining a therapeutic level of GLM for a longer period of time, as compared to free drug and market product. There was no significant difference between mean plasma AUC(0-48hr) of GLM-loaded niosomes and that of market product. GLM-loaded niosomes exhibited seven-fold enhancement in relative bioavailability in comparison with free drug. These findings reinforce the potential use of niosomes for enhancing the oral bioavailability and prolonged delivery of GLM via oral administration.