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目的优选薄膜-超声法制备三种姜黄素类化合物与表没食子儿茶素没食子酸酯(epigallocatechin gallate,EGCG)复方脂质体,建立脂质体有效成分的含量测定方法,并对其抗肿瘤活性进行初步评价。方法以包埋率和载药量为指标,考察姜黄素类化合物与EGCG复合物、硬脂酸、卵磷脂以及吐温-80(1.0%)用量对包埋率和载药量的影响,并通过正交试验优化处方及制备工艺;通过MTT法测定不同浓度下脂质体对A549和CT-26肿瘤细胞的抑制作用。结果当姜黄素类化合物与EGCG复合物35 mg,硬脂酸120 mg,卵磷脂60 mg,吐温-80(1.0%)10 ml时,所得脂质体平均粒径为85.2 nm,多分散度(polydispersity index,PDI)0.152,Zeta电位为-45.3 m V,包埋率达到93.74%,载药量为13.26%。结论优选出的工艺稳定可行;三种复方脂质体联合给药对A549和CT-26肿瘤细胞有更强的抑制作用,体现了很好的抗肿瘤协同作用。
OBJECTIVE To prepare three kinds of curcumin and epigallocatechin gallate (EGCG) liposomes by membrane-ultrasonic method and establish the method for determination of the effective components of liposomes. The antitumor activity Make a preliminary assessment. Methods The embedding rate and drug loading were taken as indexes to investigate the effect of curcuminoids and EGCG complex, stearic acid, lecithin and Tween-80 (1.0%) on embedding rate and drug loading The orthogonal test was used to optimize the formulation and preparation process. The inhibitory effects of liposomes on A549 and CT-26 tumor cells were determined by MTT assay. Results When the curcuminoids and EGCG complex were 35 mg, 120 mg stearic acid, 60 mg lecithin and 10 ml Tween-80 (1.0%), the average diameter of liposomes was 85.2 nm. The polydispersity (polydispersity index, PDI) of 0.152, Zeta potential of -45.3 mV, embedding rate of 93.74% and drug loading of 13.26%. Conclusion The optimized process is stable and feasible. The combination of three liposomes has stronger inhibitory effect on A549 and CT-26 tumor cells, which shows good antitumor synergism.