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目的制备半乳糖化白蛋白汉防己甲素纳米粒(Galn-BSA-Tet-NPs),并考察合成半乳糖化白蛋白的最佳条件。方法以乳糖和牛血清白蛋白为原料,采用还原胺化法制备半乳糖化白蛋白(Galn-BSA)。采用苯酚-硫酸比色法测定糖化比率,以糖化比率作为指标考察反应的pH、时间、催化物剂量的多个水平,从中选出最优化组合。并采用去溶剂化法制备半乳糖化白蛋白汉防己甲素纳米粒(Galn-BSA-Tet-NPs)。结果制备半乳糖化白蛋白的最佳条件是磷酸缓冲液的pH值为7.4,反应时间为80h,氰基硼氢化钠的催化量为0.8mmol/L;成功合成了半乳糖化白蛋白汉防己甲素纳米粒(Galn-BSA-Tet-NPs)。结论汉防己甲素可以采用去溶剂化法制备成半乳糖化白蛋白纳米粒,此方法可提高汉防己甲素在水相中的浓度,并靶向肝细胞,从而增强汉防己甲素的抗肝纤维化药效。
Objective To prepare Galn-BSA-Tet-NPs (Gal-BSA-Tet-NPs) and investigate the optimal conditions for the synthesis of galactosylated albumin. Methods GalNA-BSA was prepared by the reductive amination method using lactose and bovine serum albumin as raw materials. The ratio of saccharification was determined by phenol-sulfuric acid colorimetric method. The saccharification ratio was taken as an index to investigate the reaction pH, time and the dosage of catalyst. The optimum combination was selected. Gal-BSA-Tet-NPs were prepared by desolvation method. Results The optimal conditions for the preparation of galactosylated albumin were as follows: the pH value of phosphate buffer was 7.4, the reaction time was 80 h and the catalytic amount of sodium cyanoborohydride was 0.8 mmol / L. Galactosylated albumin A nano-particles (Galn-BSA-Tet-NPs). Conclusion Tetrandrine can be prepared by desalination of galactosylbumin nanoparticles, this method can increase the concentration of tetrandrine in the aqueous phase, and targeting hepatocytes, thereby enhancing the anti-tetrandrine Liver fibrosis efficacy.