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采用一种新设计的末端带有枝状结构寡赖氨酸聚乙二醇高分子磷脂为主要功能性辅料,依照常规薄膜-水合和后续高分子插入两种方法制备了系列外表面带正电荷的高分子脂质体。激光衍射粒径仪研究证明,常规脂质体制备方法和后续高分子插入都可以制备纳米、粒径均匀、外表面携带不同密度正电荷的高分子磷脂脂质体,正电荷密度不同并不影响脂质体的粒径和分布。后续高分子插入过程不影响脂质体的载药工艺,不干扰脂质体的载药量,不引起脂质体的形态和粒径变化,也不诱发脂质体内部包裹的药物早期泄漏。体外细胞学实验证明这种荷正电高分子脂质体局部电荷密度高,对细胞有显著非特异性靶向作用。
Using a newly designed oligo-lysine-terminated polyethylene glycol macromolecule phospholipid with the terminal structure as the main functional adjuvant, two series of methods, ie film-hydration and subsequent polymer insertion, The polymer liposomes. Laser diffraction particle size analyzer studies have shown that conventional liposome preparation methods and follow-up polymer insertion can be prepared nano, uniform particle size, the outer surface of the polymer carrying different density positive phospholipid liposomes, the positive charge density does not affect the different Liposome size and distribution. Subsequent polymer insertion process does not affect the drug loading process of liposomes, does not interfere with the drug loading of liposomes, does not cause changes in the morphology and particle size of liposomes, and does not induce early leakage of drugs encapsulated in liposomes. In vitro cytology experiments show that this charge-positive polymer liposomes have high local charge density and have significant non-specific targeting to cells.