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

Salvatore Nicoletti; Karin Seifert; Ian H. Gilbert

doi:10.1016/j.bmc.2010.02.043

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

Salvatore Nicoletti, Karin Seifert, Ian H. Gilbert

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19 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 language	English
Pages (from-to)	2559-2565
Number of pages	7
Journal	Bioorganic & Medicinal Chemistry
Volume	18
Issue number	7
DOIs	https://doi.org/10.1016/j.bmc.2010.02.043
Publication status	Published - 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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10.1016/j.bmc.2010.02.043

http://ukpmc.ac.uk/articles/PMC2862900

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title = "Water-soluble polymer-drug conjugates for combination chemotherapy against visceral leishmaniasis",

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.",

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author = "Salvatore Nicoletti and Karin Seifert and Gilbert, {Ian H.}",

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AU - Nicoletti, Salvatore

AU - Seifert, Karin

AU - Gilbert, Ian H.

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N2 - 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.

AB - 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.

KW - Leishmaniasis

KW - Polymer-drug conjugates

KW - Combination therapy

KW - Amphotericin B

KW - Alendronate

KW - FARNESYL PYROPHOSPHATE SYNTHASE

KW - SODIUM STIBOGLUCONATE

KW - ANTILEISHMANIAL DRUGS

KW - TOXOPLASMA-GONDII

KW - AMPHOTERICIN-B

KW - KALA-AZAR

KW - ALENDRONATE

KW - BISPHOSPHONATES

KW - AMINOSIDINE

KW - DONOVANI

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EP - 2565

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 7

ER -

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

Abstract

Keywords

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