羟基喜树碱两亲性嵌段共聚物纳米粒的制备及性质

Preparation and Characterization of Hydroxycamptothecin Nanoparticles of Amphiphilic Block Copolymer

目的:制备羟基喜树碱(hydroxycamptothec in,HCPT)的两亲性嵌段共聚物纳米粒并进行初步的性质考察。方法:本文合成了聚乙二醇-聚己内酯嵌段共聚物(polyethyleneglycol-polycaprolatone,PEG-PCL),用1H-NMR对其结构进行了表征,并以此为载体材料,采用溶剂扩散法制备了羟基喜树两亲性嵌段共聚物纳米粒(HCPT-PEG-PCL-NPs),并对其进行初步的质量评价及稳定性考察。结果:制备的HCPT-PEG-PCL-NPs平均粒径为164.5 nm,多分散系数为0.14,载药量为5.49%,包封率为83.2%,ξ电位为-26.1 mV;冻干粉剂的稳定性较好,但高温环境不利于保存。结论:本文制备的纳米粒大大增加了HCPT的水溶性,是一种值得研究开发的HCPT的新剂型。

Objective ： To prepare hydroxycamptothecin nanoparticles of amphiphilic block copolymer and study its characterization initially. Methods： Polyethyleneglycol-polycaprolactone（PEG-PCL） was synthesized and its structure was characterized by 1^H-NMR. The HCPT-PEG-PCL-NPs were prepared by solvent-diffusion method using PEG-PCL block eopolymer as a matrix and HCPT as an antitumor agent. Then the obtained NPs were evaluated and the physical stabilities of both suspl and freeze drying powder were investigated. Results： The mean particle size of the prepared NPs was 164. 5 nm, polydispersity index （PI） was 0. 14, drug loading （DL） was 5.49% , entrapment efficiency （EE） was 83.2% , ξ potential was - 26.1 mV. The physical stability of freeze drying powder was better and hot environment seemed to be bad for the stability. Conclusion： The HCPT-PEG-PCL-NPs increase the solubility of HCPT in water and are valuable for the development of the novel dosage form of HCPT.