摘要
目的:合成肝靶向药物载体半乳糖基人血清白蛋白,并探讨其生物学特性。方法:以半乳糖和人血清白蛋白为原料,合成半乳糖基人血清白蛋白,利用现代生物质谱技术,分析该药物载体的纯度和糖密度;并用131I标记与模型药物5-氟脲啶偶联后的肝靶向药物载体,进行动物体内靶向性作用的研究。结果:合成的肝靶向药物载体具有较高的纯度,糖密度(即每分子人血清蛋白偶联半乳糖的分子数)达到了51∶1,具有显著的趋肝性,肝脏摄取率达到75.0%。结论:合成的肝靶向药物载体半乳糖基人血清白蛋白是优良的受体介导的肝靶向药物载体。
Objective: To synthesize and characterize a galactosyl-HSA (a human serum albumin, Gal-HSA) that is a specific ligand of asialoglycoprotein receptor on hepatocytes and a hepatic targeting drug carrier. Methods: The galactosyl-HSA was synthesized with galactose and human serum albumin and its purity and galactosyl density were analyzed with MALDI-TOF-MS (Matrix assisted laser adsorption ionization time of flight mass spectrometry); After conjugating with 5-Fu, the Gal-HSA was labeled with 131 I and injected into rabbits and rats to test the biological distribution. Results: The synthesized galactosyl-HSA was pure; the galactosyl/HSA density (the ratio of galactosyl residues to protein) reached to 51∶1 and no HSA remainder was seen in galactosyl-HSA; the galactosyl-HSA had a remarkable positive liver taxis and the uptake rate of galactosyl-HSA by liver was 75.0% in vivo. Conclusion: The synthesized galactosyl-HSA might be a good receptor-mediated hepatic targeting drugs carrier.[
出处
《广东医学院学报》
2005年第3期235-237,共3页
Journal of Guangdong Medical College
基金
广东省科技计划项目(2004B30101004)
湛江市重点攻关招标项目(20030304)资助
