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目的:制备叶酸修饰去甲斑蝥素隐形泡囊新型给药系统,并进行表征及体外药效学评价。方法:采用改良注入法制得新型给药系统,考察其形态、粒径、包封率和体外释放特性等理化性质对其进行表征,并通过它对叶酸受体过度表达Hela细胞的体外细胞摄取试验及生长抑制试验,进行体外药效学评价。结果:研制的隐形泡囊新型给药系统的平均粒径为100.87 nm,包封率为52.3%,体外释放显著缓慢于游离药物,且在模拟正常细胞pH 7.4环境下的释放t1/2是在模拟肿瘤细胞pH 5.0的1.98倍。细胞摄取试验说明叶酸泡囊能提高肿瘤细胞对药物的摄取(P<0.01)。细胞毒性试验证实,叶酸泡囊抑制肿瘤细胞生长的作用显著(P<0.01),但游离叶酸可减轻叶酸泡囊对肿瘤细胞的杀伤作用。结论:本研究采用简单易行的方法制得的叶酸修饰去甲斑蝥素隐形泡囊,体外具有pH敏感性、隐形性、叶酸受体靶向性,是一种具有良好开发前景的主动靶向抗肿瘤新型给药系统。
OBJECTIVE: To prepare a novel delivery system for folic acid-modified norcantharidin invisible vesicles and to characterize and evaluate pharmacodynamics in vitro. Methods: A new drug delivery system was prepared by modified injection method. The morphological, particle size, entrapment efficiency and in vitro release characteristics of the drug delivery system were characterized. The in vitro cell uptake assay of folic acid receptor overexpression Hela cells And growth inhibition test, in vitro pharmacodynamic evaluation. Results: The average particle size of the new drug delivery system was 100.87 nm with entrapment efficiency of 52.3%. The in vitro release was significantly slower than that of free drug and the release t1 / 2 in simulated normal cells at pH 7.4 was 1.98 times the simulated tumor cell pH 5.0. Cell uptake test showed that folate follicles can improve tumor cell uptake of drugs (P <0.01). Cytotoxicity test confirmed that folic acid vesicles inhibited the growth of tumor cells significantly (P <0.01), but folic acid free folate can reduce the cytotoxicity of folic acid vesicles on tumor cells. CONCLUSION: In this study, folic acid-modified norcantharidin invisible vesicles prepared by a simple and easy method, with pH sensitivity, invisibility, folate receptor targeting in vitro, is an active target with good development prospects Anti-tumor new drug delivery system.