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含有两性霉素B的聚合磷脂囊泡:体外毒性和抗真菌活性评估

Polymerized phospholipid vesicles containing amphotericin B: evaluation of toxic and antifungal activities in vitro.

作者信息

Mehta R, Hsu M J, Juliano R L, Krause H J, Regen S L

出版信息

J Pharm Sci. 1986 Jun;75(6):579-81. doi: 10.1002/jps.2600750611.

Abstract

We have prepared lipid vesicles (liposomes) composed of polymerized bis[12-(methacryloyloxy)dodecanoyl]-L-alpha-phosphatidylcholine (DPL) which contain the antifungal polyene antibiotic amphotericin B (AMB). It was necessary to devise a novel method for incorporating AMB into the liposomes subsequent to polymerization. The polymer liposome AMB was as effective as AMB in "conventional" liposomes in terms of inhibiting fungal growth in vitro. However, in contrast to "conventional" liposomes, the polymerized DPL vesicles did not protect mammalian cells against AMB induced toxicity.

摘要

我们制备了由聚合的双[12-(甲基丙烯酰氧基)十二烷酰基]-L-α-磷脂酰胆碱(DPL)组成的脂质囊泡(脂质体),其包含抗真菌多烯抗生素两性霉素B(AMB)。有必要设计一种在聚合后将AMB掺入脂质体的新方法。就体外抑制真菌生长而言,聚合物脂质体AMB与“常规”脂质体中的AMB一样有效。然而,与“常规”脂质体不同,聚合的DPL囊泡不能保护哺乳动物细胞免受AMB诱导的毒性。

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