【摘要】 目的:制备喜树碱/聚乙二醇-聚谷氨酸苄酯(CPT/PEG-PBLG)纳米胶束并考察其载药特性及体外性能。方法:采用膜透析结合冷冻干燥法制备CPT/PEG-PBLG纳米胶束,通过体外试验研究其释药特性,并考察胶束对HepG-2癌细胞的细胞毒性。结果:PEG-PBLG纳米胶束能包埋疏水性药物喜树碱,BLG嵌段摩尔比为35%的EG-5载药率达11.13%;CPT/PEG-PBLG纳米胶束的体外释放具有突释与缓释特性并在碱性介质中释放速度加快,EG-5载药胶束在pH 1.1累计释药率60.34%,而在pH 10.0时则为73.72%;当喜树碱质量浓度≤50 mg·L-1时,CPT/PEG-PBLG胶束对HepG-2癌细胞的毒性远低于相应浓度的喜树碱阳性组(P<0.01)。结论:CPT/PEG-PBLG纳米胶束制备工艺简单,安全无污染,可降低喜树碱的细胞毒性,具有较好的临床应用价值。更多还原

【Abstract】 Objective: To prepare camptothecin-loaded core-shell type nano-micelles( polyethylene glycol-poly benzyl-L-glutamate,PEG-PBLG) and investigate its drug-loaded characteristics and in vitro properties. Method: Camptothecin-loaded( CPT) nano-micelles with PEG-PBLG was prepared by dialysis and freeze-drying method,in vitro release characteristics of CPT / PEG-PBLG nano-micelles was measured by UV, and its cytotoxicity for HepG-2 cell was investigated. Result: Camptothecin could be entrapped in PEG-PBLG nanomicelles,drug loading content of EG-5 was 11. 13%,whose molar ratio of BLG block was 35%; CPT / PEGPBLG nano-micelles had in vitro burst and sustained release profile,it could accelerate release speed in alkaline medium,cumulative release rate of EG-5 micelles was 60. 34% at pH 1. 1,but it was 73. 72% at pH 10. 0;When the concentration of camptothecin ≤50 mg·L- 1,CPT/PEG-PBLG nano-micelles displayed much less cell cytotoxicity than the same concentration of camptothecin positive group( P < 0. 01). Conclusion: Preparation technology of CPT / PEG-PBLG nano-micelles was simple and safe without pollution for environment, it would reduce cytotoxicity of camptothecin for clinic treatment value of tumor.更多还原