Objective To investigate the application of poly (3-hydroxybutyrate-co-3-hydroxyhexanoate) (PHBHHx) as a drug release carrier of hydrophobic rapamycin and its sustained release profile in vitro. Methods The rapamycin-loaded PHBHHx nanoparticles were prepared by a modified emulsification/solvent diffusion method. The diameter of the nanoparticles was measured by a laser light scattering machine. In vitro release study of rapamycin from nanopartilces was performed by the dialysis bag method. HPLC analysis was used for quantification of rapamycin. PC3 cells were treated with rapamycin-loaded PHBHHx nanoparticles and the cell viability was determined by MTT. The level of phospho-p70S6K, one of mTOR substrates, was studied by Western blot analysis. Results The average diameter of rapamycin-loaded PHBHHx nanoparticles was 211.4 nm, with the entrapment efficiency being 92.5%. The entrapped rapamycin could be sustainedly released for at least 7 days. In vitro proliferation of PC3 cell line and the phosphorylation of p70S6K could be inhibited by rapamycin-loaded PHBHHx nanoparticles. Conclusion PHBHHx can be a promising hydrophobic drug delivery carrier.%目的 研究生物可降解高分子材料3-羟基丁酸-3羟基己酸共聚酯(PHBHHx)作为疏水性药物雷帕霉素缓释载体的效果及其体外条件下对疏水性药物的缓释情况.方法 超声乳化分散法制备PHBHHx载药纳米微球,颗粒尺度分析仪对颗粒粒径进行表征,透析袋法进行雷帕霉素体外缓释,高效液相色谱法检测雷帕霉素释放量.用包裹雷帕霉素的PHBHHx纳米颗粒处理体外培养的PC3细胞,MTT法检测细胞活力,Western blot检测mTOR底物p70S6K磷酸化情况.结果 包裹雷帕霉素的PHBHHx纳米颗粒平均粒径为211.4 nm,对雷帕霉素的包封率为92.5％,包裹雷帕霉素的PHBHHx纳米颗粒可以实现雷帕霉素的体外缓释,且能够抑制人前列腺癌细胞系PC3的体外增殖和胞内p70S6K的磷酸化.结论 PHBHHx是一种很有潜力的疏水性药物包封和递送载体材料.
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