Prabaharan Mani, Grailer Jamison J, Steeber Douglas A, Gong Shaoqin
Department of Mechanical Engineering, University of Wisconsin-Milwaukee, Milwaukee, WI 53211, USA.
Macromol Biosci. 2009 Aug 11;9(8):744-53. doi: 10.1002/mabi.200800366.
Thermosensitive PNVCL-b-PEG block copolymer coupled with folic acid was prepared as an anti-cancer drug carrier. This polymer self-assembled into stable micelles in aqueous solutions at above 33 degrees C. At 37 degrees C, the release profile of PNVCL-b-PEG-FA micelles showed a slower and more controlled release of the entrapped 5-FU than that at 25 degrees C. The blank and 5-FU-loaded PNVCL-b-PEG-FA micelles did not induce remarkable cytotoxicity against the EA.hy 926 human endothelial cell line; however, 5-FU-loaded PNVCL-b-PEG-FA micelles showed a cytotoxicity effect against 4T1 mouse mammary carcinoma cells due to the availability of loaded anti-cancer drugs delivered to the inside of the cancer cells by the folate-receptor-mediated endocytosis process.
将与叶酸偶联的热敏性聚N-乙烯基己内酰胺-b-聚乙二醇嵌段共聚物制备为抗癌药物载体。该聚合物在33℃以上的水溶液中自组装成稳定的胶束。在37℃时，聚N-乙烯基己内酰胺-b-聚乙二醇-叶酸胶束的释放曲线显示，与25℃时相比，包封的5-氟尿嘧啶释放更缓慢且更可控。空白和负载5-氟尿嘧啶的聚N-乙烯基己内酰胺-b-聚乙二醇-叶酸胶束对EA.hy 926人内皮细胞系未诱导出显著的细胞毒性；然而，负载5-氟尿嘧啶的聚N-乙烯基己内酰胺-b-聚乙二醇-叶酸胶束对4T1小鼠乳腺癌细胞显示出细胞毒性作用，这是由于通过叶酸受体介导的内吞作用将负载的抗癌药物递送至癌细胞内部。
