Department of Pharmaceutics and Nanotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Int J Nanomedicine. 2020 Nov 11;15:8767-8781. doi: 10.2147/IJN.S261932. eCollection 2020.
Niosomes, bilayer vesicles formed by the self-assembly of nonionic surfactants, are receiving increasing attention as potential oral drug delivery systems but the impact of niosomal formulation parameters on their oral capability has not been studied systematically. The aim of this study was to investigate the impact of surfactant composition and surface charge of niosomes in enhancing oral bioavailability of repaglinide (REG) as a BCS II model drug.
Niosomes (13 formulations) from various nonionic surfactants having HLB in the range of 4-28 (Tweens, Spans, Brijs, Myrj, poloxamer 188, TPGS and Labrasol) were prepared and characterized concerning their loading efficiency, hydrodynamic diameter, zeta potential, drug release profile, and stability. The oral pharmacokinetics of the selected formulations were studied in rats (8 in vivo groups).
The results revealed that type of surfactant markedly affected the in vitro and in vivo potentials of niosomes. The C and AUC values of REG after administration of the selected niosomes as well as the drug suspension (as control) were in the order of Tween 80> TPGS> Myrj 52> Brij 35> Span 60≈Suspension. Adding stearyl amine as a positive charge-inducing agent to the Tween 80-based niosomes, resulted in an additional increase in drug absorption and values of AUC and C were 3.8- and 4.7-fold higher than the drug suspension, respectively.
Cationic Tween 80-based niosomes may represent a promising platform to develop oral delivery systems for BCS II drugs.
非离子型表面活性剂自组装形成的双层囊泡即尼奥斯体，作为潜在的口服药物递送系统受到越来越多的关注，但尼奥斯体制剂参数对其口服能力的影响尚未得到系统研究。本研究旨在探讨不同非离子型表面活性剂（吐温、司盘、布瑞杰、弥赛、泊洛沙姆 188、TPGS 和 Labrasol）组成和表面电荷的尼奥斯体对作为 BCS II 模型药物的瑞格列奈（REG）口服生物利用度的影响。
制备了不同 HLB 值（4-28）的非离子型表面活性剂（吐温、司盘、布瑞杰、弥赛、泊洛沙姆 188、TPGS 和 Labrasol）尼奥斯体（13 种制剂），并对其载药效率、水动力学直径、Zeta 电位、药物释放曲线和稳定性进行了表征。在大鼠中（8 个体内组）研究了选定制剂的口服药代动力学。
结果表明，表面活性剂的类型显著影响尼奥斯体的体外和体内潜力。给予选定的尼奥斯体以及药物混悬剂（作为对照）后，REG 的 C 和 AUC 值的顺序为 Tween 80>TPGS>Myrj 52>Brij 35>Span 60≈混悬剂。向 Tween 80 基尼奥斯体中添加硬脂胺作为正电荷诱导剂，可使药物吸收进一步增加，AUC 和 C 值分别比药物混悬剂高 3.8 倍和 4.7 倍。
阳离子 Tween 80 基尼奥斯体可能代表开发 BCS II 药物口服递送系统的有前途的平台。
