Department of Pharmaceutical Technology, School of Pharmacy, Ankara University, Tandogan, Ankara, Turkey.
J Pharm Sci. 2010 Apr;99(4):2049-60. doi: 10.1002/jps.21944.
Nonionic surfactant based vesicles (niosomes) are novel drug delivery systems formed from the self-assembly of nonionic amphiphiles in aqueous media. In the present study niosomal formulations of Paclitaxel (PCT), an antineoplastic agent, were prepared using different surfactants (Tween 20, 60, Span 20, 40, 60, Brij 76, 78, 72) by film hydration method. PCT was successfully entrapped in all of the formulations with encapsulation efficiencies ranging between 12.1 +/- 1.36% and 96.6 +/- 0.482%. Z-average sizes of the niosomes were between 229.3 and 588.2 nm. Depending on the addition of the negatively charged dicetyl phosphate to the formulations negative zeta potential values were obtained. High surface charges showed that niosomes can be suspended in water well and this is beneficial for their storage and administration. PCT released from niosomes by a diffusion controlled mechanism. The slow release observed from these formulations might be beneficial for reducing the toxic side effects of PCT. The niosome preparation method was found to be repeatable in terms of size distribution, zeta potential and % drug loading values. The efficiency of niosomes to protect PCT against gastrointestinal enzymes (trypsin, chymotrypsin, and pepsin) was also evaluated for PCT oral delivery. Among all formulations, gastrointestinal stability of PCT was well preserved with Span 40 niosomes.
基于非离子表面活性剂的囊泡(niosomes)是一种新型的药物传递系统,由非离子型两亲分子在水介质中自组装形成。本研究采用薄膜水化法,用不同的表面活性剂(吐温 20、60、司盘 20、40、60、Brij 76、78、72)制备了紫杉醇(PCT)的囊泡制剂,紫杉醇是一种抗肿瘤药物。PCT 成功地包封在所有制剂中,包封效率在 12.1±1.36%和 96.6±0.482%之间。囊泡的 Z-平均粒径在 229.3nm 到 588.2nm 之间。根据向制剂中添加带负电荷的二乙酰基焦磷酸,可以得到负的 Zeta 电位值。高表面电荷表明囊泡可以很好地悬浮在水中,这有利于它们的储存和给药。PCT 通过扩散控制机制从囊泡中释放。这些制剂中观察到的缓慢释放可能有利于降低 PCT 的毒副作用。囊泡制备方法在粒径分布、Zeta 电位和药物载量方面具有可重复性。还评估了囊泡对胃肠道酶(胰蛋白酶、糜蛋白酶和胃蛋白酶)的保护紫杉醇(PCT)的能力,以实现 PCT 的口服传递。在所有制剂中,Span 40 囊泡能很好地保持 PCT 的胃肠道稳定性。