穿膜肽介导紫杉醇脂质体对肿瘤的治疗作用

摘要

目的：制备和表征 F3修饰紫杉醇脂质体，并进行细胞学和体内抗肿瘤评价。方法采用薄膜分散法制备脂质体，人肺腺癌细胞 A549进行摄取评价；小鼠肝癌细胞 H22荷瘤小鼠进行体内抗肿瘤活性评价。结果 F3修饰脂质体粒径为90 nm；该修饰后脂质体被细胞摄取能力明显增强，进而提高了药物的抗肿瘤活性，给药16天后，F3— Lipo 组瘤体增长仅为11倍，相比于生理盐水组26倍，Taxol 18倍，未修饰脂质体14倍，有更好的抗肿瘤效果。结论 F3穿膜肽可以明显提高载体入胞能力，进而改善药物治疗作用。%Objective To prepare and exosyndrome F3 modified paclitaxel liposome and evaluate the cellular uptake and antitumor activities. Methods The liposomes were prepared by film — dispersed method;The studies of cellular uptake and antitumor activities were performed in A549 cells and H22 — bearing mice,respectively. Results The F3 modified lipo-somes with a diameter size of around 90 nm were uptaken by cells and thus had better antitumor activities. Conclusion F3 penetrating peptides could enhance the cellular uptake and thus improve the therapeutic outcome of drugs.