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在本研究中,我们制备了iRGD,CRGDK/RGPD/EC)修饰、含溶血磷脂的温敏脂质体(LTSL)载体系统用以递送共轭亚油酸-紫杉醇(CLA-PTX),简称iRGD-LTSL-CLA-PTX.在B16-F10黑色素瘤细胞上评估了iRGD-LTSL-CLA-PTX的体外细胞摄取和体外细胞毒性.在荷B16-F10黑色素瘤的C57BL/6小鼠上评价了iRGD-LTSL-CLA-PTX的体内抗肿瘤作用.细胞摄取实验结果表明,与SSL-CLA-PTX组相比,在42℃分别孵育2、4和6h,iRGD-LTSL-CLA-PTX给药组中CLA-PTX的细胞摄取分别增加2.05、3.31和4.83倍.体内抗肿瘤效果表明,与CLA-PTX溶液、LTSL-CLA-PTX、LTSL-CLA-PTX(加热条件)和iRGD-LTSL-CLA-PTX相比,iRGD-LTSL-CLA-PTX(加热条件)可显着抑制B16-F10肿瘤的生长(P＜0.01).iRGD-LTSL-CLA-PTX对B16-F10黑素瘤的体外和体内抗肿瘤作用得到证实,这是iRGD和LTSL共同作用的结果.“,”In the present study,we prepared the iRGD-modified lysolipid-containing thermosensitive liposomes (LTSL) containing conjugated linoleic acid-paclitaxel (CLA-PTX),also known as iRGD-LTSL-CLA-PTX.The in vitro cellular uptake and in vitro cytotoxicity of iRGD-LTSL-CLA-PTX were evaluated in B 16-F10 melanoma cells.The in vivo anti-tumor effect of iRGD-LTSL-CLA-PTX was investigated using B 16-F10 tumor-bearing C57BL/6 mice.The results of the cellular uptake experiment indicated that the increased cellular uptake of CLA-PTX in the iRGD-LTSL-CLA-PTX-treated groups was 2.05-,3.31-or 4.83-fold compared with that in the SSL-CLA-PTX group after a 2-,4-or 6-h incubation at 42 ℃,respectively.The in vivo antitumor results showed that iRGD-LTSL-CLA-PTX/hent significantly inhibited the growth of B 1 6-F10 tumors compared with the CLA-PTX solution (LTSL-CLA-PTX,LTSL-CLA-PTX/heat and iRGD-LTSL-CLA-PTX) (P＜0.01).In conclusion,the antitumor effect of iRGD-LTSL-CLA-PTX was confirmed on B16-F10 melanoma in vitro and in vivo,which was induced by both the effect of iRGD and LTSL.