PEG修饰青蒿素脂质纳米粒的体外释放及抗巨噬细胞摄取特性

发布时间：2018-06-23 01:56

本文选题：青蒿素 + 脂质纳米粒　；参考：《天然产物研究与开发》2015年01期

【摘要】：研究聚乙二醇硬脂酸酯(PEGn-SA)修饰的青蒿素脂质纳米粒(PEGn-ART-NLC)体外释放及抗巨噬细胞(J774)摄取特性。采用高压乳匀法制备PEGn-SA(n=25、40、55)修饰的PEGn-ART-NLC及未修饰的青蒿素脂质纳米粒(ART-NLC),进行体外释放试验、抗吞噬实验、利用Gouy-Chapmann理论计算固定水化层厚度(FALT),并加以比较。在p H 7.4磷酸盐缓冲液(PBS)中,药物的体外释放度随PEGn-SA聚合度的改变而改变;加入血浆后,亦有改变。J774细胞对PEGn-ART-NLC的摄取量随PEGn-SA聚合度及J774细胞与制剂孵育时间的改变而改变;加入血浆孵育后,亦有改变。ART-NLC及三种PEGn-ART-NLC的固定水化层厚度分别为0.31、1.76、1.86和2.04 nm。结果表明该制剂体外具有良好的缓释特性及抗J774细胞吞噬性。
[Abstract]:To study the release of polyethylene glycol stearate (PEGn-SA) modified artemisinin lipid nanoparticles (PEGn-ART-NLC) and its anti-macrophage (J774) uptake in vitro. PEGn-SA modified PEGn-ART-NLC and unmodified artemisinin lipid nanoparticles (ART-NLC) were prepared by high pressure emulsion method. The in vitro release test and anti-phagocytosis test were carried out. The fixed hydration layer thickness (Fart) was calculated by Gouy-Chapmann theory and compared. In pH 7.4 phosphate buffer (PBS), the drug release in vitro changed with the change of PEGn-SA polymerization degree, and the uptake of PEGn-ART-NLC by J774 cells changed with the change of PEGn-SA polymerization degree and incubation time of J774 cells with preparation. After plasma incubation, the fixed hydration layer thickness of .ART-NLC and three kinds of PEGn-ART-NLC were 0.31 ~ 1.76 ~ 1.86 and 2.04 nm, respectively. The results showed that the preparation had good sustained release properties and anti-phagocytosis of J774 cells in vitro.
【作者单位】：山西医科大学药学院;
【基金】：国家自然基金项目(81373364)
【分类号】：R944

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