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高密度脂蛋白(HDL)可逆向转运血浆中胆固醇至肝脏代谢,在肝靶向传递系统方面具有较大的开发潜力和、应用价值。载脂蛋白A-Ⅰ(apoA-Ⅰ)是HDL的主要组成部分。以apoA-Ⅰ为载体,水溶性抗肿瘤药盐酸多柔比星为模型药,采用薄膜分散法或硫酸铵梯度法制备重组高密度脂蛋白-盐酸多柔比星纳米粒,并以平均粒径或包封率为指标进行优化。结果表明,优化后的薄膜分散法所得制品平均粒径为(48.3±16.1)nm,包封率为(20.2±4.2)%。优化后的硫酸铵梯度法所得制品平均粒径为(113.8±10.3)nm,包封率为(83.3±8.5)%,且无溶血性。采用5%蔗糖为冻干保护剂制得的冻干,品于-20℃放置8个月,稳定性较好。
High-density lipoprotein (HDL) reversibly transports plasma cholesterol to liver metabolism, and has great potential for development and application in liver-targeted delivery system. Apolipoprotein A-I (apoA-I) is a major component of HDL. ApoA-Ⅰ as a carrier, water-soluble drug-resistant drug doxorubicine as a model drug, the use of thin-film dispersion or ammonium sulfate gradient preparation of recombinant high-density lipoprotein - doxorubicin hydrochloride nanoparticles, and the average particle size Or encapsulation efficiency as an indicator to optimize. The results showed that the average diameter of the product obtained after the optimized film dispersion method was (48.3 ± 16.1) nm, and the entrapment efficiency was (20.2 ± 4.2)%. The average particle diameter of the product obtained by the optimized ammonium sulfate gradient method was (113.8 ± 10.3) nm, and the entrapment efficiency was (83.3 ± 8.5)%, with no hemolysis. Lyophilized with 5% sucrose as lyoprotectants prepared freeze-dried product placed at -20 ℃ for 8 months, the stability is better.