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[多西他赛的TPGS修饰前体脂质体的研制与表征]

[Development and characterization of TPGS modified proniosomes of docetaxel].

作者信息

Liu He-long, Hu Kai-li, Feng Jian-fang

出版信息

Zhongguo Zhong Yao Za Zhi. 2015 Oct;40(19):3775-9.

Abstract

A novel oral delivery system that TPGS modified docetaxel proniosomes, DTX-TPGS-PN, was developed and the characterization after hydration was observed. Firstly, Doce-TPGS-PN was optimized by investing the factors, including the type of surfactant, methods of adding TPGS, content of TPGS and the molar ratio of span40/cholesterol, which may affecting the particle size, encapsulation efficiency and instantaneous release of drug in the formulation. Then, the morphology, particle size, Zeta potential, encapsulation efficiency and in vitro release of the formulation were evaluated. The result showed that hydrated nanoparticles of DTX-TPGS-PNs were (93 ± 6.5) nm in size,(-83.95 ± 3.69) mV in zeta potential, (97.31 ± 0.60)% in encapsulation efficiency, exhibiting spherical morphology and biphasic release process that a low burst effect within the first 0.5 hour and a relative-sustained release for the next several hours in PBS. These results indicate the oral delivery system of DTX-TPGS-PN was successfully built with good properties.

摘要

开发了一种新型口服给药系统,即TPGS修饰的多西他赛前体脂质体(DTX-TPGS-PN),并观察了其水化后的特性。首先,通过研究包括表面活性剂类型、添加TPGS的方法、TPGS含量以及司盘40/胆固醇的摩尔比等可能影响制剂中粒径、包封率和药物瞬时释放的因素,对多西他赛-TPGS-PN进行了优化。然后,对该制剂的形态、粒径、Zeta电位、包封率和体外释放进行了评估。结果表明,DTX-TPGS-PN的水化纳米粒粒径为(93±6.5)nm,Zeta电位为(-83.95±3.69)mV,包封率为(97.31±0.60)%,呈现球形形态和双相释放过程,即在PBS中最初0.5小时内有较低的突释效应,随后数小时有相对持续的释放。这些结果表明成功构建了具有良好性能的DTX-TPGS-PN口服给药系统。

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