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含有香豆素-类蛋白共轭物的光敏脂质体。

Light-sensitive liposomes containing coumarin-proteinoid conjugate.

作者信息

Seo Hee Jin, Kim Jin-Chul

机构信息

Division of Biotechnology and Bioengineering and Institute of Bioscience and Biotechnology, Kangwon National University, 192-1, Hyoja 2-dong, Chuncheon-si, Kangwon-do 200-701, Korea.

出版信息

J Nanosci Nanotechnol. 2012 May;12(5):4044-50. doi: 10.1166/jnn.2012.5856.

DOI:10.1166/jnn.2012.5856
PMID:22852345
Abstract

Photo-sensitive liposomes were prepared by modifying the surface with coumarin derivative-proteinoid conjugate. Epoxypropoxy coumarin (EPC) was conjugated to proteinoid composed of Asp, Ser and Leu (PASL) using the reaction mixture of which EPC/PASL ratio was 8/1 (w/w). The molar ratio of Asp residue/Ser residue/Leu residue/EPC residue of the resulting conjugate was calculated to be 71.1:18.6/6.3/4.0 on 1H NMR spectrum. Egg phosphatidylcholine (egg PC) liposomes bearing PASL-EPC conjugate was prepared by hydrating egg PC dry film with a buffer solution containing the conjugate. Egg PC/PASL-EPC conjugate ratios (w/w) in the preparation were 100:1 to 100:20, and the specific loadings of EPC residue in the liposomes were 0.0002 mg/mg to 0.0018 mg/mg. The release from the liposomes prepared using the egg PC/PASL-EPC conjugate ratios of 100:5 began to markedly increase 30 min after the irradiation of lambda = 254 nm and the release degree in 180 min was about 30%. Without the UV irradiation, no appreciable release was observed.

摘要

通过用香豆素衍生物-类蛋白共轭物修饰表面来制备光敏脂质体。使用环氧丙氧基香豆素(EPC)与天冬氨酸、丝氨酸和亮氨酸组成的类蛋白(PASL)的反应混合物,以EPC/PASL比例为8/1(w/w)将EPC与PASL共轭。根据1H NMR光谱计算,所得共轭物中天冬氨酸残基/丝氨酸残基/亮氨酸残基/EPC残基的摩尔比为71.1:18.6/6.3/4.0。通过用含有共轭物的缓冲溶液水合卵磷脂酰胆碱(卵PC)干膜来制备带有PASL-EPC共轭物的卵PC脂质体。制备中卵PC/PASL-EPC共轭物的比例(w/w)为100:1至100:20,脂质体中EPC残基的比负载量为0.0002 mg/mg至0.0018 mg/mg。使用卵PC/PASL-EPC共轭物比例为100:5制备的脂质体在λ = 254 nm照射30分钟后释放开始显著增加,180分钟时的释放度约为30%。在没有紫外线照射的情况下,未观察到明显的释放。

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