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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。
OBJECTIVE: To prepare camptothecin / polyethylene glycol-polyglutamic acid benzyl ester (CPT / PEG-PBLG) nanomicelles and study their drug-loading properties and in vitro properties. METHODS: CPT / PEG-PBLG nanomicelles were prepared by membrane dialysis combined with freeze-drying method. The drug release characteristics of CPT / PEG-PBLG were studied in vitro. The cytotoxicity of micelles to HepG-2 cancer cells was also investigated. Results: The PEG-PBLG nanomicelles were able to embed the camptothecin, a hydrophobic drug. The drug loading rate of EG-5 with BLG block was 35% was 11.13%. In vitro release of CPT / PEG- Release and release characteristics of the drug-loaded micelles and their release in alkaline medium were accelerated. The cumulative drug release rate of EG-5 loaded micelles was 60.34% at pH 1.1 and 73.72% at pH 10.0. When the concentration of camptothecin was less than 50 The toxicity of CPT / PEG-PBLG micelles to HepG-2 cancer cells was much lower than that of the camptothecin-positive group (P <0.01) at mg · L-1. CONCLUSION: CPT / PEG-PBLG nanomicelles have simple preparation process, safe and pollution-free, can reduce the cytotoxicity of CPT, and have good clinical value.