叶酸偶联白蛋白纳米粒肿瘤细胞靶向性研究

Study on the Tumor Cell Targetability of Folate-conjugated Albumin Nanoparticles

目的 研究能通过叶酸受体介导靶向肿瘤细胞的叶酸偶联白蛋白纳米粒。方法 利用叶酸活性酯在碱性条件下与白蛋白纳米粒表面上的氨基反应 ,制得叶酸偶联的白蛋白纳米粒。以荧光定量法确定浓度、时间、游离叶酸对肿瘤细胞摄取叶酸偶联白蛋白纳米粒的影响程度。结果 成功制备了叶酸偶联白蛋白纳米粒。叶酸偶联白蛋白纳米粒的肿瘤细胞摄取量随纳米粒浓度增大、培养时间延长而增加 ,肿瘤细胞对叶酸偶联白蛋白纳米粒的摄取可被过量的外源性游离叶酸所抑制。结论 叶酸偶联白蛋白纳米粒能通过细胞膜上的叶酸受体介导内吞入胞 。

Objective To study folate-conjugated albumin nanoparticles targeting to tumor cells via folate receptor-mediated endocytosis. Methods The activated folic acid (N-hydroxysuccinimide ester of folic acid) was conjuated to the surface of bovine serum albumin nanoparticles (BSANP) via the amino groups. The extent of the influence that concentration, incubation time and free folate exerted on the uptake of Folate-BSANP by ovarian cancer cells (SKOV3) was determined using fluorescence spectrophotometer. Results Folate-conjugated BSANP (Folate-BSANP) was successfully achieved. Uptake of Folate-BSANP by cancer cells was gradually increased with the extension of incubation time or the increase of Folate-BSANP concentration, and the uptake could be competitively inhibited by excess free folate. Conclusion Folate-BSANP could be delivered into tumor cells via folate receptor-mediated endocytosis and significantly targeted to tumor cells with rich folate receptors.