TPGS修饰多烯紫杉醇前体囊泡口服递药系统的构建及表征

Development and characterization of TPGS modified proniosomes of docetaxel

该研究旨在建立一种新型的载多烯紫杉醇的TPGS修饰前体囊泡口服递药系统(Doce-TPGS-PN),并对其水化后的物理化学特性和体外释放进行考察。首先,以制得前囊泡水化后的粒径、包封率和突释量为指标,考察脂质材料的种类、TPGS修饰方法、TPGS加入量及表面活性剂和胆固醇的比例对前囊泡水化后性质的影响,筛选最优处方和制备工艺。其次,对最优处方制得DTX-TPGS-PN的形态、粒径、表面电荷、包封率及体外释放行为进行考察。结果表明,Doce-TPGS-PN系统水化后,粒径为(93±6.5)nm,Zeta电位为(-83.95±3.69)m V,包封率(97.31±0.60)%,在PBS中的释放分为前0.5 h的速释相和之后的缓释相。实验证明,该研究成功构建了Doce-TPGS-PN这一新型口服给药系统,且其具有良好性质。

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.