肝细胞靶向甘草酸表面修饰白蛋白纳米粒的制备工艺

目的研究能主动靶向于肝实质细胞的甘草酸表面修饰白蛋白纳米粒的制备工艺。方法去溶剂化法制备普通纳米粒，以高碘酸盐氧化法制备甘草酸-白蛋白纳米粒偶联物。用2,4,6-三硝基苯磺酸显色法与凝胶柱色谱法验证是否偶联成功，HPLC法测定修饰纳米粒表面甘草酸密度。结果修饰纳米粒表面活性氨基数量较对照组减少19.6%；偶联于纳米粒表面的甘草酸密度为9.2%。纳米粒形态圆整，平均粒径为73 nm，在25 ℃和37 ℃条件下放置10 d后，性质稳定。结论甘草酸表面修饰白蛋白纳米粒制备成功，为进一步研究其对肝细胞的靶向性奠定了实验基础。

Preparation of bovine serum albumin nanoparticles surface-modified with glycyrrhizin

AIM: To study the preparation of bovine serum albumin nanoparticles surface-modified with glycyrrhizin(BSA-NP-GL) targeting to hepatocytes. METHODS: The bovine serum albumin nanoparticles (BSA-NP) were prepared by desolvation process. Glycyrrhizin (GL) was oxidized by sodium periodate to be conjugated to surface reactive amino groups (SRAG) of the BSA-NP. The SRAG were quantified by spectrophotometric method using 2, 4, 6-trinitrobenzenesulfonic acid(TNBS). Glycyrrhetinic acid(GA) hydrolyzed from GL, which was on the surface of BSA-NP-GL was assayed by HPLC after isolation by sephadex G-50. Both methods were used to verify the conjugation achieved. HPLC was used to determine surface density of GL on BSA-NP-GL. RESULTS: The amount of SRAG of the BSA-NP-GL decreased by 19.6% compared with normal BSA-NP. The amount of GL molecule was 9.2% of the total determined SRAG of BSA-NP. The mean diameter of the BSA-NP-GL was 73 nm with round shape. The stability of BSA-NP-GL was constant when it was stored at 25 degrees C and 37 degrees C during 10 days. CONCLUSION: BSA-NP-GL was successfully prepared, which is considered to establish an experimental foundation for further research on its ability for targeting to hepatocytes.