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糖基化脂质体作为熊果酸的药物传递系统,用于治疗细菌感染。

Glucosylated liposomes as drug delivery systems of usnic acid to address bacterial infections.

机构信息

Dipartimento di Chimica, Università degli Studi di Roma "Sapienza", P.le Aldo Moro 5, 00185 Roma, Italy.

Dipartimento di Scienze Fisiche e Chimiche, Università degli Studi dell'Aquila, Via Vetoio 10, 67100 Coppito (Aq), Italy.

出版信息

Colloids Surf B Biointerfaces. 2019 Sep 1;181:632-638. doi: 10.1016/j.colsurfb.2019.05.056. Epub 2019 Jun 4.

Abstract

Because of the increased incidence of infections caused by resistant pathogens, due to the intensive use of antibiotics, there is an urgent need to develop new therapeutic strategies against bacteria, possibly based on non conventional drugs. (+)-Usnic acid is a natural compound that exerts a potent antibacterial activity, however its clinical application is hampered by its scarce solubility in water. Usnic acid was included, by both passive and active loading techniques, in liposomes containing structurally related glucosylated amphiphiles. Liposome formulations were characterized from the physicochemical point of view and their activity against biofilm associated Staphylococcus epidermidis was also evaluated. The inclusion of usnic acid in glucosylated cationic liposomes promotes its penetration in biofilm matrix with a consequent increase of its antimicrobial activity. The effect of both cationic charge and sugar residue seems to be synergistic.

摘要

由于耐药病原体引起的感染发病率增加,由于抗生素的大量使用,因此迫切需要开发针对细菌的新治疗策略,可能基于非传统药物。(+)-地衣酸是一种具有强大抗菌活性的天然化合物,但由于其在水中的溶解度低,其临床应用受到限制。通过被动和主动加载技术,地衣酸被包含在含有结构相关的糖基化两亲物的脂质体中。从物理化学的角度对脂质体配方进行了表征,并评估了它们对与生物膜相关的表皮葡萄球菌的活性。地衣酸被包含在糖基化阳离子脂质体中促进其穿透生物膜基质,从而增加其抗菌活性。阳离子电荷和糖残基的作用似乎是协同的。

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