Characterization of Niosomes Prepared With Various Nonionic Surfactants for Paclitaxel Oral Delivery
Characterization of Niosomes Prepared With Various Nonionic Surfactants for Paclitaxel Oral Delivery
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DOI：
10.1002/jps.21944
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发表时间：
2010-04-01
影响因子：
3.8
通讯作者：
Yuksel, Nilufer
中科院分区：
文献类型：
--
作者：
Bayindir, Zerrin Sezgin;Yuksel, Nilufer
基于非离子表面活性剂的囊泡（泡囊）是由非离子两亲物在水介质中自组装形成的新型药物递送系统。本研究采用薄膜水合法，以不同表面活性剂（Tween 20、60，Span 20、40、60，Brij 76、78、72）为原料，制备了紫杉醇（PCT）囊泡制剂。PCT成功包埋在所有制剂中，包封率范围在12.1 +/- 1.36%至96.6 +/-0.482%之间。囊泡的Z-平均尺寸在229.3和588.2nm之间。取决于向制剂中添加带负电荷的磷酸二鲸蜡酯，获得负ζ电位值。高的表面电荷表明囊泡能够很好地悬浮在水中，这有利于囊泡的储存和给药。PCT通过扩散控制机制从囊泡中释放。从这些制剂中观察到的缓慢释放可能有利于减少PCT的毒副作用。发现囊泡制备方法在尺寸分布、ζ电位和%药物负载值方面是可重复的。还评价了囊泡保护PCT免受胃肠道酶（胰蛋白酶、胰凝乳蛋白酶和胃蛋白酶）影响的效率，用于PCT口服递送。在所有制剂中，PCT的胃肠道稳定性用Span 40类脂质体良好地保持。(C)2009 Wiley-Liss，Inc.和美国药学协会药物科学杂志99：2049-2060，2010
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. (C) 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:2049-2060, 2010