陈 涛 王汝涛 王 昭 卢婷利 赵 雯. 非特异靶向荷正电高分子磷脂脂质体的构建和体外评价J. 药学学报, 2010,45(3): 359-364.
引用本文: 陈 涛 王汝涛 王 昭 卢婷利 赵 雯. 非特异靶向荷正电高分子磷脂脂质体的构建和体外评价J. 药学学报, 2010,45(3): 359-364.
CHEN Chao, Wang-Ru-Chao, Wang- Zhao, Lei-Ting-Li, Diao- Wen. Construction and evaluation of non-specific targeting cationic polymer lipid liposomesJ. 药学学报, 2010,45(3): 359-364.
Citation: CHEN Chao, Wang-Ru-Chao, Wang- Zhao, Lei-Ting-Li, Diao- Wen. Construction and evaluation of non-specific targeting cationic polymer lipid liposomesJ. 药学学报, 2010,45(3): 359-364.

非特异靶向荷正电高分子磷脂脂质体的构建和体外评价

Construction and evaluation of non-specific targeting cationic polymer lipid liposomes

  • 摘要:

    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。

     

    Abstract:

    A new class of dendrimer polylysine poly(ethylene glycol)-lipid was designed and synthesized.  The cationic polymer liposomes were prepared by the lipid film-extrusion and post-insertion two methods with these dendrimer polylysine poly(ethylene glycol)-lipid and other lipids.  The structural properties of obtained cationic polymer liposomes were studied by laser light scattering and fluorescence spectrometer.  It was    demonstrated that the nano sized liposomes with different density of surface cationic charges can be prepared by either lipid film-extrusion or post-insertion methods, but post-insertion process did not affect drug loading, did not influence drug loading capacity and did not induce liposomal morphology and particle size.  The density of positive charge does not affect the size and distribution of different liposomes size and distribution.  It was the better choice for manufacture because post-insertion method did not cause early release of drug and size changes.  Cell binding experiments show that cationic polymer liposomes, especially dendrimer polymer liposomes had higher local charge density, and therefore have dramatic non specific cell targeting ability.

     

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