4.7 Article

Water-soluble polymer-drug conjugates for combination chemotherapy against visceral leishmaniasis

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 7, Pages 2559-2565

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.02.043

Keywords

Leishmaniasis; Polymer-drug conjugates; Combination therapy; Amphotericin B; Alendronate

Funding

  1. Wellcome Trust [074136]

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There is a need for new safe, effective and short-course treatments for leishmaniasis; one strategy is to use combination chemotherapy. Polymer-drug conjugates have shown promise for the delivery of anti-leishmanial agents such as amphotericin B. In this paper, we report on the preparation and biological evaluation of polymer-drug conjugates of N-(2-hydroxypropyl) methacrylamide (HPMA), amphotericin B and alendronic acid. The combinatorial polymer-drug conjugates were effective anti-leishmanial agents in vitro and in vivo, but offered no advantage over the single poly(HPMA)-amphotericin B conjugates. (C) 2010 Elsevier Ltd. All rights reserved.

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