包载紫杉醇PLGA纳米粒的制备工艺优化及表征

doi:10.7525/j.issn.1673-5102.2019.04.018

植物研究 ›› 2019, Vol. 39 ›› Issue (4): 627-633.doi: 10.7525/j.issn.1673-5102.2019.04.018

包载紫杉醇PLGA纳米粒的制备工艺优化及表征

王思莹, 赵修华, 赵冬梅

东北林业大学森林植物生态学教育部重点实验室, 哈尔滨 150040

收稿日期:2019-01-07 出版日期:2019-07-05 发布日期:2019-07-03
通讯作者: 赵冬梅 E-mail:156828568@qq.com
作者简介:王思莹(1993-),女,硕士研究生,主要从事药物化学方面的研究。
基金资助:
中央高校基本科研业务费专项资金项目（2572016CA12）

Formulation and Process Optimization of Paclitaxel-loaded PLGA Nanoparticles

WANG Si-Ying, ZHAO Xiu-Hua, ZHAO Dong-Mei

Key Laboratory of Forest Plant Ecology of Ministry of Education, Northeast Forestry University, Harbin 150040

Received:2019-01-07 Online:2019-07-05 Published:2019-07-03
Supported by:
Fundamental Research Funds for the Central Universities(2572016CA12)

摘要/Abstract

摘要： 以生物可降解材料乳酸—羟基乙酸共聚物[poly（lactic-co-glycolic acid），PLGA]为载体材料，采用乳化—溶剂挥发法制备包载紫杉醇（PTX）的PLGA微球（PTX-PLGA NPs）。采用正交实验设计，考察乳化剂质量浓度、PLGA与紫杉醇质量比、油相用量、剪切速度4个因素对粒径和载药率的影响，优化纳米粒最佳制备工艺。研究结果表明：当PLGA与PTX的质量比为4：1，聚乙烯醇PVA用量0.1%，二氯甲烷用量为4 mL，剪切速度为16 000 r·min^-1是纳米粒的最佳制备工艺。最佳工艺条件下的PTX-PLGA NPs多批次重复实验得到PLGA-NPs粒径分布为（207.1±20.5）nm，Zeta电位为（-23.8±2.5）mV，载药量为（14.45±0.04）%。制得的PTX-PLGA NPs均匀圆整、理化性质稳定。冻干粉复溶溶液12 h粒径变化不大，具有良好的药物稳定性，为新型抗肿瘤缓释制剂的研发提供实验基础。

关键词: 紫杉醇, PLGA, 乳化—溶剂挥发法, 工艺优化

Abstract: Paclitaxel-loaded PLGA nanoparticles(PTX-PLGA NPs) was prepared by emulsion solvent evaporation method with the biodegradable materials-poly(lactic-co-glycolic acid)(PLGA) used as carrier materials. The best formulation and preparation conditions were optimized by orthogonal test, investigating the influence of the ratio of paclitaxel and PLGA, the amount of surfactant, the amount of dichloromethane(DCM) and shearing rate on the preparation of nanoparticles. The optimal preparation conditions for PTX-PLGA NPs were as follows:the ratio of paclitaxel and PLGA of 4:1, the amount of surfactant of 0.1%, the amount of dichloromethane of 4 mL and shearing rate of 16 000 r·min^-1. With optimization of the formulation and preparation conditions, the PTX-PLGA NPs are regularly spherical in shape with the mean size of (207.1±20.5) nm, and the ζ-potential of the NPs is about (-23.8±2.5) mV. The encapsulation efficiency was estimated to be 14.45%±0.04%, respectively. The size distribution of PTX-PLGA NPs frozen dry powder was sustained stable character in 12 h. The results indicate that PTX-PLGA NPs were successfully prepared by modified solvent evaporation method, which could provide the experimental basis for the development of a new anti-tumor sustained-release formulation.

Key words: Paclitaxel, poly(lactic-co-glycolic acid), emulsion(O/W) solvent evaporation, process optimization

中图分类号:

Q949.66+1

王思莹, 赵修华, 赵冬梅. 包载紫杉醇PLGA纳米粒的制备工艺优化及表征[J]. 植物研究, 2019, 39(4): 627-633.

WANG Si-Ying, ZHAO Xiu-Hua, ZHAO Dong-Mei. Formulation and Process Optimization of Paclitaxel-loaded PLGA Nanoparticles[J]. Bulletin of Botanical Research, 2019, 39(4): 627-633.

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包载紫杉醇PLGA纳米粒的制备工艺优化及表征

Formulation and Process Optimization of Paclitaxel-loaded PLGA Nanoparticles

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