叶酸受体在实体瘤组织细胞表面的过度表达使得叶酸介导的靶向释药系统成为治疗癌症的研究热点;纳米粒子能够逃避网状巨噬细胞（RES）的捕获并加强渗透和滞留效应（EPR）是其应用于药物控释系统的主要原因。以聚乳酸、氨基封端的聚乙二醇和叶酸为原料,采用活性酯的方法合成了聚乳酸-聚乙二醇-叶酸偶合物,并以此为载体,采用溶液挥发自组装的方法制备具有主动靶向性的纳米微粒。采用1 HNMR,对材料结构进行表征;采用荧光探针法对微粒的稳定性进行检测;采用人乳腺癌细胞（MCF-7）和成纤维细胞（CCL-110）对微粒的细胞靶向选择性进行实验。结果表明,在成功合成材料的基础上,制备的纳米粒子具有很好的细胞选择性,和同类材料相比具有较好的稀释稳定性,有望成为叶酸受体介导的靶向药物控释系统的载体材料。
Folate has been employed as a targeting moiety of various anticancer agents to increase their cellular uptake within target cells since folate receptors were vastly overexpressed in several human tumors. In this study, dodecanoled-poly(D, L-lactic acid)-b-poly (ethylene glycol)-folate (Dol-PLA-PEG-FA) was synthesized from dodecanoled-poly(D, L-lactic acid), H2N-PEG-NH2 and folate by active ester method, whereafter, active- targeting nanoparticles were prepared through solution volatilization and self-assembly. 1H NMR was employed to characterize the structure of copolymer, and luminescence spectrometer was characterized the diluting stabili ty of nanoparticles, then model cells breast cancer cells (MCF-7) and fibroblasts cells (CCL-110) were to evalu- ate the targeting- mediated endocytosis pathway. The results showed that the nanoparticles have good diluting stability and targeting selectivity on the basis of successful synthetic materials, and these are potential to be- come the receptor mediated targeted drug release system carrier material.
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