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

Salvatore Nicoletti, Karin Seifert, Ian H. Gilbert

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    16 Citations (Scopus)

    Abstract

    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.

    Original languageEnglish
    Pages (from-to)2559-2565
    Number of pages7
    JournalBioorganic & Medicinal Chemistry
    Volume18
    Issue number7
    DOIs
    Publication statusPublished - Apr 2010

    Keywords

    • Leishmaniasis
    • Polymer-drug conjugates
    • Combination therapy
    • Amphotericin B
    • Alendronate
    • FARNESYL PYROPHOSPHATE SYNTHASE
    • SODIUM STIBOGLUCONATE
    • ANTILEISHMANIAL DRUGS
    • TOXOPLASMA-GONDII
    • AMPHOTERICIN-B
    • KALA-AZAR
    • ALENDRONATE
    • BISPHOSPHONATES
    • AMINOSIDINE
    • DONOVANI

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