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目的制备冬凌草甲素/胆固醇甲酰-壳聚糖共聚物(ORI/CF-CS)纳米胶束并研究其体外抗肿瘤活性。方法采用酰胺化反应合成胆固醇甲酰-壳聚糖共聚物(CF-CS);以CF-CS为载体材料制备ORI/CF-CS纳米胶束,并测定其载药量、包封率、形态、粒径和ξ电位;MTT法测定其对宫颈癌Hela肿瘤细胞的细胞毒作用。结果 ORI/CF-CS纳米胶束载药量为9.16%,包封率为48.83%,粒径控制在68.10～113.8 nm内,ξ电位为-34.97～-29.19 mV,体外释药缓慢;ORI/CF-CS纳米胶束对Hela肿瘤细胞的细胞毒作用优于冬凌草甲素溶液,且IC50值比冬凌草甲素溶液低约3倍。结论 CF-CS是冬凌草甲素的优良载体,且可提高其抗Hela肿瘤细胞的活性。
OBJECTIVE To prepare oridonin / cholesterol formyl-chitosan copolymer (ORI / CF-CS) nanomicelles and study the antitumor activity in vitro. Methods Cholesterol formyl-chitosan copolymer (CF-CS) was synthesized by amidation reaction. ORI / CF-CS nanomicelles were prepared by CF-CS as carrier. The drug loading, entrapment efficiency, , Particle size and zeta potential. MTT assay was used to determine the cytotoxic effect on Hela tumor cells. Results The drug loading of ORI / CF-CS nanomicelles was 9.16%, encapsulation efficiency was 48.83%, particle size was controlled within 68.10 ~ 113.8 nm, zeta potential was -34.97 ~ -29.19 mV, The cytotoxic effect of CF-CS nanomicelles on Hela tumor cells was better than that of oridonin solution, and the IC50 value was about 3 times lower than that of oridonin solution. Conclusion CF-CS is an excellent carrier of oridonin, and can improve its anti-Hela tumor cell activity.