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目的制备了白介素-2(IL-2)靶向5-氟尿苷棕榈酸酯(5-FURP)脂质体,并进行了体外细胞毒性,初步考察其对IL-2受体高表达的肿瘤细胞的靶向作用。方法采用逆相蒸发法制备5-FURP脂质体,通过交联剂将IL-2连接到脂质体的表面,得IL-2靶向5-FURP脂质体(IL-2-5FURP-L);UV法测定包封率;用考马斯亮蓝结合法测定IL-2与脂质体的结合率;用MTT法测定脂质体对IL-2受体高表达的皮肤T细胞淋巴瘤Hut-102细胞的生长抑制作用。结果 IL-2-5-FURP-L的粒径为180 nm;药物平均包封率为91.3%;IL-2的结合率为56.0%;在pH7.4的释放介质中,脂质体具有缓释作用;MTT实验结果显示,IL-2-5-FURP-L呈剂量依赖性抑制肿瘤细胞的生长,72 h细胞毒性试验表明IL-2-5-FURP-L对Hut-102的杀伤作用(IC50=1.04μg.mL-1)明显优于5-FURP-L(IC50=6.11μg.mL-1)及5-FURP(IC50=7.35μg.mL-1)。结论 IL-2修饰的载药脂质体具有明显的抑瘤作用和主动靶向作用。
Objective To prepare IL-2 targeted 5-fluorouridine palmitate (5-FURP) liposome and to study its cytotoxicity in vitro. To investigate the effect of interleukin-2 (IL-2) Cell targeting. Methods 5-FURP liposomes were prepared by reversed-phase evaporation. The IL-2 was linked to the surface of liposomes by cross-linking agent to obtain IL-2 targeted 5-FURP liposomes (IL-2-5FURP-L ). The encapsulation efficiency was determined by UV method. The binding rate of IL-2 and liposomes was determined by Coomassie brilliant blue binding assay. The effect of liposome on the expression of IL-2 receptor on skin T-cell lymphoma Hut- 102 cell growth inhibitory effect. Results The particle size of IL-2-5-FURP-L was 180 nm. The average entrapment efficiency of drug was 91.3% and the binding rate of IL-2 was 56.0%. In pH7.4 release medium, The results of MTT assay showed that IL-2-5-FURP-L inhibited the growth of tumor cells in a dose-dependent manner. Cytotoxicity assay at 72 h showed that IL-2-5-FURP-L could kill Hut- IC50 = 1.04μg.mL-1) was significantly superior to 5-FURP-L (IC50 = 6.11μg.mL-1) and 5-FURP (IC50 = 7.35μg.mL-1). Conclusion IL-2 modified drug-loaded liposomes have obvious antitumor activity and active targeting.