叶酸偶联白蛋白纳米粒的制备工艺研究

采用去溶剂化法制备普通白蛋白纳米粒 ,利用叶酸活性酯在微碱性条件下与白蛋白纳米粒表面的氨基反应 ,制得叶酸偶联白蛋白纳米粒。采用葡聚糖凝胶柱色谱法及紫外分光光度法验证偶联是否成功 ,并测定叶酸偶联的程度。通过葡聚糖凝胶柱色谱法可以清楚地看到叶酸偶联白蛋白纳米粒与未反应的叶酸活性酯完全分离 ,叶酸偶联白蛋白纳米粒与叶酸白蛋白机械混合物的胰蛋白酶水解液在 35 8nm处的紫外吸收图谱基本一致 ,说明叶酸已经成功地偶联于白蛋白纳米粒的表面。纳米粒形态圆整 ,平均粒径为 6 6 nm。叶酸偶联白蛋白纳米粒制备成功 ,作为叶酸受体表达丰富的多种肿瘤细胞的主动靶向给药的潜在途径 ,值得进一步的关注和研究

Study on the Preparation of Folate-conjugated Albumin Nanoparticles

Bovine serum albumin nanoparticles(BSANP)were prepared by desolvation method. The activated folic acid (N hydroxysuccinimide ester of folic acid) was conjuated to the surface of BSANP via the amino groups. Then the folate conjugated BSANPs (folate BSANP) were purified with Sephadex G 50 column and completely separated from unreacted folic acid. After chymotryptic hydrolysis, the extent of folate conjugation on the BSANP was determined by quantitative ultraviolet(UV) spectrophotometric analysis. It was found that the spectrum of trypsin digest of folate conjugate BSANP is basically identical with that of folate, thus indicating folate is successfully expressed on the surface of BSANP. The folate BSANP was averagely 66 nm in diameter and was spherical in shape. Folate conjugated BSANP was achieved, which represents a potential new drug carrier for tumor cell selective targeting.