CAJ | 학술논문

目的：制备整合素受体精氨酸-甘氨酸-天冬氨酸（Arg-Gly-Asp,RGD）和细胞穿膜肽(transcriptional actirator protein, TAT共修饰载紫杉醇（paclitaxel,PTX）脂质体（liposomes，LP（）RGD/TAT-LP-PTX），对其理化性质进行表征，并考察脂质体与肺癌A 549细胞的亲和力以及对A 549细胞增殖的抑制作用。方法采用薄膜分散法制备RGD/TAT-LP-PTX，考察脂质体的粒径，电位以及包封率；通过定量细胞摄取实验考察肺癌A 549细胞对RGD/TAT-LP的摄取效率。构建A 549肿瘤球模型，定性共聚焦实验观察肿瘤细胞和肿瘤球对脂质体的摄取。噻唑蓝实验考察RGD/TAT-LP-PTX对肺癌A 549细胞的增殖抑制作用。结果 RGD/TAT-LP-PTX的粒径在（118.5±11.4）nm，电位为（21.58±2.42）mV，紫杉醇的包封率为86.5%。细胞摄取实验结果显示，RGD/TAT-LP在4 h摄取效率是2 h的1.88倍，差异具有统计学意义（P<0.05）；肺癌A 549细胞在与脂质体共同孵育4 h后对RGD/TAT-LP的摄取效率分别是TAT-LP、RGD-LP和LP的2.1倍、2.8倍和5.1倍，差异具有统计学意义（P<0.01）；MTT实验结果显示，在相同给药浓度下，不同脂质体组间细胞存活率有显著性差异（P<0.01）。结论整合素受体RGD和细胞穿膜肽TAT共修饰载紫杉醇（PTX）脂质体能够有效识别高表达整合素受体的肿瘤细胞，穿透肿瘤细胞膜进入肿瘤细胞，是一种潜在高效的肿瘤靶向给药系统。
목적：제비정합소수체정안산-감안산-천동안산（Arg-Gly-Asp,RGD）화세포천막태(transcriptional actirator protein, TAT공수식재자삼순（paclitaxel,PTX）지질체（liposomes，LP（）RGD/TAT-LP-PTX），대기이화성질진행표정，병고찰지질체여폐암A 549세포적친화력이급대A 549세포증식적억제작용。방법채용박막분산법제비RGD/TAT-LP-PTX，고찰지질체적립경，전위이급포봉솔；통과정량세포섭취실험고찰폐암A 549세포대RGD/TAT-LP적섭취효솔。구건A 549종류구모형，정성공취초실험관찰종류세포화종류구대지질체적섭취。새서람실험고찰RGD/TAT-LP-PTX대폐암A 549세포적증식억제작용。결과 RGD/TAT-LP-PTX적립경재（118.5±11.4）nm，전위위（21.58±2.42）mV，자삼순적포봉솔위86.5%。세포섭취실험결과현시，RGD/TAT-LP재4 h섭취효솔시2 h적1.88배，차이구유통계학의의（P<0.05）；폐암A 549세포재여지질체공동부육4 h후대RGD/TAT-LP적섭취효솔분별시TAT-LP、RGD-LP화LP적2.1배、2.8배화5.1배，차이구유통계학의의（P<0.01）；MTT실험결과현시，재상동급약농도하，불동지질체조간세포존활솔유현저성차이（P<0.01）。결론정합소수체RGD화세포천막태TAT공수식재자삼순（PTX）지질체능구유효식별고표체정합소수체적종류세포，천투종류세포막진입종류세포，시일충잠재고효적종류파향급약계통。
Objective To prepare RGD and TAT co-modified paclitaxel loaded liposome(RGD/TAT-LP-PTX)for A 549 cells targeting.Method The co-modified liposome was prepared by film-ultrasonic method. The appearance,particle size,Zeta potential were evaluated. The cellular uptake by A 549 cells in vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD/TAT-LP-PTX was evaluated by MTT assay. Results The particle diameter of the co-modified liposome was (118.5±11.4) nm with the Zeta potential of (21.58±2.42 )mV. The entrapment efficiency of PTX was 86.5%. The result demonstrated that the co-modified liposome uptaken by A 549 were 2.1, 2.8 times higher than that of TAT-LP and RGD-LP, respectively. The RGD/TAT-LP-PTX shows the highest anti-proliferation efficiency. Conclusion The co-modified liposome might serve as a promising tumor delivery system of antitumor drugs.