Nanocarriers with strong tumor cell targeting ability have been expected to overcome limitations of cancer chemotherapy. Herein, cell membrane mimetic micelles were prepared from a random copolymer (PMNCF) containing cell membrane phosphorylcholine zwitterion, cholesterol, and tumor cell targeting folic acid (FA) at the side chain ends. Surface orientation of the FA ligand was optimized during PMNCF micelle preparation by controlling solvent solubility for FA. The out-oriented ligands on the micelles were immobilized by the strongly associated hydration layer around the closely packed phosphorylcholine zwitterions. The doxorubicin (DOX) loaded PMNCF micelles were demonstrated to reduce normal cell toxicity to less than 20%. More significantly, HeLa and MCF-7 tumor cell killing efficacy of the optimized formulation was enhanced to 160% compared with that of free DOX. The excellent performances of the drug loaded PMNCF micelles on both tumor cell killing and normal cell toxicity reducing efficacies reveal great potential for developing advanced drug delivery system.

中文翻译：

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叶酸配体的方向进行优化的细胞膜模拟胶束形成过程中增强的肿瘤细胞靶向。

预期具有强肿瘤细胞靶向能力的纳米载体将克服癌症化学疗法的局限性。本文中，由无规共聚物（PMNCF）制备细胞膜模拟胶束，所述无规共聚物在侧链末端包含细胞膜磷酸胆碱两性离子，胆固醇和靶向肿瘤细胞的叶酸（FA）。通过控制FA的溶剂溶解度，可以在PMNCF胶束制备过程中优化FA配体的表面取向。胶束上的外向配体被紧密结合的磷酸胆碱两性离子周围的强缔合水合层固定。载有阿霉素（DOX）的PMNCF胶束可将正常细胞毒性降至20％以下。更重要的是 与游离DOX相比，优化制剂的HeLa和MCF-7肿瘤细胞杀伤效力提高至160％。载药PMNCF胶束在肿瘤细胞杀伤和降低正常细胞毒性方面均具有出色的性能，显示了开发先进药物输送系统的巨大潜力。