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

Research output: Contribution to journal › Article › peer-review

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

Access to Document

10.1016/j.bmc.2010.02.043

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

Embargoed Document

Elsevier Sponsored Document
337 KB
Embargo ends: 31/12/99

Cite this

@article{b909964d33aa4a00a1a986cb337d57a8,

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.",

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",

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

year = "2010",

month = apr,

doi = "10.1016/j.bmc.2010.02.043",

language = "English",

volume = "18",

pages = "2559--2565",

journal = "Bioorganic \& Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier",

number = "7",

}

TY - JOUR

T1 - Water-soluble polymer-drug conjugates for combination chemotherapy against visceral leishmaniasis

AU - Nicoletti, Salvatore

AU - Seifert, Karin

AU - Gilbert, Ian H.

PY - 2010/4

Y1 - 2010/4

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

U2 - 10.1016/j.bmc.2010.02.043

DO - 10.1016/j.bmc.2010.02.043

M3 - Article

C2 - 20338769

SN - 0968-0896

VL - 18

SP - 2559

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

Access to Document

Embargoed Document

Fingerprint

Cite this