PEG修飾青蒿素脂質(zhì)納米粒的體外釋放及抗巨噬細(xì)胞攝取特性
發(fā)布時間:2018-06-23 01:56
本文選題:青蒿素 + 脂質(zhì)納米粒; 參考:《天然產(chǎn)物研究與開發(fā)》2015年01期
【摘要】:研究聚乙二醇硬脂酸酯(PEGn-SA)修飾的青蒿素脂質(zhì)納米粒(PEGn-ART-NLC)體外釋放及抗巨噬細(xì)胞(J774)攝取特性。采用高壓乳勻法制備PEGn-SA(n=25、40、55)修飾的PEGn-ART-NLC及未修飾的青蒿素脂質(zhì)納米粒(ART-NLC),進(jìn)行體外釋放試驗、抗吞噬實驗、利用Gouy-Chapmann理論計算固定水化層厚度(FALT),并加以比較。在p H 7.4磷酸鹽緩沖液(PBS)中,藥物的體外釋放度隨PEGn-SA聚合度的改變而改變;加入血漿后,亦有改變。J774細(xì)胞對PEGn-ART-NLC的攝取量隨PEGn-SA聚合度及J774細(xì)胞與制劑孵育時間的改變而改變;加入血漿孵育后,亦有改變。ART-NLC及三種PEGn-ART-NLC的固定水化層厚度分別為0.31、1.76、1.86和2.04 nm。結(jié)果表明該制劑體外具有良好的緩釋特性及抗J774細(xì)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.
【作者單位】: 山西醫(yī)科大學(xué)藥學(xué)院;
【基金】:國家自然基金項目(81373364)
【分類號】:R944
【參考文獻(xiàn)】
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