Synthesis and characterisation of a new pH-sensitive amphotericin B -: poly(ethylene glycol)-b-poly(L-lysine) conjugate

被引：26

作者：

Sedlak, Milos

Pravda, Martin

Kubicova, Lenka

Mikulcikova, Petra

Ventura, Karel

机构：

[1] Univ Pardubice, Dept Organ Chem, Pardubice 53210, Czech Republic

[2] Univ Pardubice, Dept Analyt Chem, Pardubice 53210, Czech Republic

[3] Charles Univ Prague, Fac Pharm, Dept Inorgan & Organ Chem, Hradec Kralove 50005, Czech Republic

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 09期

关键词：

drug delivery; amphotericin B; pH-sensitive conjugate;

D O I：

10.1016/j.bmcl.2007.02.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This paper reports on the synthesis, characterisation, and efficiency of a new intravenous conjugate of amphotericin B (AMB). Twelve molecules of AMB were attached to block copolymer poly(ethylene glycol)-b-poly(L-lysine) via pH-sensitive imine linkages. In vitro drug release studies demonstrated the conjugate (M-w = 26,700) to be relatively stable in human plasma and in phosphate buffer (pH 7.4, 37 degrees C). Controlled release of AMB was observed in acidic phosphate buffer (pH 5.5, 37 degrees C) with the half-life of 2 min. The LD50 value determined in vivo (mouse) is 45 mg/kg (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2554 / 2557

页数：4

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