两亲性嵌段共聚物普朗尼克的细胞毒性及细胞摄取

目的：考察不同型号、混合普朗尼克对MCF-7及耐药MCF-7的细胞毒性和细胞摄取，筛选出可供后续胶束研究的混合普朗尼克最优配比。方法：选取Pluronic F68、F127、P85、P105、P123，按HLB值分为2组，以一定比例交叉混合，采用CCK-8法和高效液相色谱法，测定普朗尼克、混合普朗尼克对MCF-7及耐药MCF-7的细胞毒性和细胞摄取量。结果：试验结果表明，F68、F127对细胞的毒性较小，而P85、P105、P123对细胞的毒性相对较大；当2种普朗尼克配比使用的质量浓度小于100 μg·mL^-1时，MCF-7及耐药MCF-7 2种细胞的存活率均大于70%。随着混合普朗尼克的浓度增加，细胞毒性均逐渐增强；F68与P85配比使用时，细胞毒性最大，且配比浓度为1：4时的细胞毒性大于1：2。Pluronic P85、P105、P123均可促进肿瘤细胞的药物摄取，Pluronic F68、F127基本不促进药物的摄取。F127-P123较其他混合普朗尼克表现出更强的摄取能力。结论：随着HLB值的降低及浓度的增大，普朗尼克对MCF-7及耐药MCF-7细胞的毒性增加。混合普朗尼克可以促进肿瘤细胞对于化疗药物的摄取。

Cytotoxicity and cellular uptake of amphiphilic block copolymer Pluronic

OBJECTIVE To investigate the cytotoxicity and cell uptake ability of MCF-7 cells and doxorubicin-resistant MCF-7 cells to different models and mixed Pluronic, to find the optimal ratio for subsequent micelles study. METHODS Pluronic F68, F127, P85, P105 and P123 were first selected and divided into two groups according to HLB, then mixed with a certain percentage. The CCK-8 method was used to evaluate the MCF-7 and doxorubicin-resistant MCF-7 cytotoxicity of Pluronic F68, F127, P85, P105 and P123, and HPLC method was used to determine their cell uptake concentrations. RESULTS F68 and F127 showed less cytotoxicity than P85, P105 and P123. When the concentrations of P85 and F127 were less than 100 μg·mL^-1, more than 70% of both cells were survived. The cytotoxicity was increased gradually with the increase of the concentration of mixed pluronic. The P85 and F68 mixture showed the highest cytotoxicity, and the proportion of 1:4 was higher than that of 1:2. Pluronic P85, P105 and P123 promoted the drug uptake ability of tumor cells, Pluronic F68 and F127 basically did not promote drug uptake. F127-P123 showed better uptake ability than other mixed Pluronic. CONCLUSION The cytotoxicity of Pluronic on MCF-7 cells and doxorubicin-resistant MCF-7 cells significantly increases as Pluronic concentration increases and HLB value decreases. Mixed Pluronic can promote tumor cellular uptake of chemotherapeutic drugs.