Biodistribution and In Vivo Antileishmanial Activity of 1,2-Distigmasterylhemisuccinoyl-sn -Glycero-3-Phosphocholine Liposome-Intercalated Amphotericin B

Antimicrobial Agents and Chemotherapy
Maryam ImanM R Jaafari

Abstract

1,2-Distigmasterylhemisuccinoyl-sn-glycero-3-phosphocholine (DSHemsPC) is a new lipid in which two molecules of stigmasterol (an inexpensive plant sterol) are covalently linked via a succinic acid to glycerophosphocholine. Our previous study revealed that liposome (Lip)-intercalated amphotericin B (AMB) prepared from DSHemsPC (DSHemsPC-AMB-Lip) possesses excellent colloidal properties and in vitro antifungal and antileishmanial activities similar to those of the liposomal AMB preparation AmBisome. The aim of this study was to determine the biodistribution and evaluate the antileishmanial effects of DSHemsPC-AMB-Lip in Leishmania major-infected BALB/c mice. The serum profile and tissue concentrations of AMB were similar in DSHemsPC-AMB-Lip- and AmBisome-treated mice after intravenous (i.v.) injection. Multiple i.v. doses of the micellar formulation of AMB (Fungizone; 1 mg/kg of body weight), DSHemsPC-AMB-Lip (5 mg/kg), and AmBisome (5 mg/kg) were used in L. major-infected BALB/c mouse models of early and established lesions. In a model of the early lesions of cutaneous leishmaniasis (CL), the results indicated that the level of footpad inflammation was significantly (P < 0.001) lower in mice treated with DSHemsPC-AMB-Lip and AmB...Continue Reading

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Citations

Jan 8, 2020·Pharmaceutics·Célia Faustino, Lídia Pinheiro
Dec 22, 2017·Antimicrobial Agents and Chemotherapy·Gert-Jan WijnantSimon L Croft
Jan 9, 2019·Biomedical Microdevices·Alexander K NguyenRoger J Narayan
Aug 23, 2019·Expert Opinion on Drug Delivery·Juliane S LanzaFrédéric Frézard

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