| Synthesis and characterisation of a new pH-sensitive amphotericin B--poly(ethylene glycol)-b-poly(L-lysine) conjugate. | |
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MedLine Citation:
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PMID: 17336066 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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 LD(50) value determined in vivo (mouse) is 45 mg/kg. |
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Authors:
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Milos Sedlák; Martin Pravda; Lenka Kubicová; Petra Mikulcíková; Karel Ventura |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2007-02-07 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 17 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2007 May |
Date Detail:
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Created Date: 2007-04-06 Completed Date: 2007-07-24 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 2554-7 Citation Subset: IM |
Affiliation:
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Department of Organic Chemistry, University of Pardubice, Pardubice, Czech Republic. milos.sedlak@upce.cz |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Amphotericin B
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analogs & derivatives*,
chemical synthesis* Antifungal Agents / chemical synthesis*, pharmacology Chemistry, Pharmaceutical / methods* Drug Design Hydrogen-Ion Concentration Models, Chemical Molecular Conformation Polyethylene Glycols / chemistry* Polylysine / chemistry* Polymers / chemistry Spectrophotometry, Ultraviolet / methods Temperature |
| Chemical | |
Reg. No./Substance:
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0/Antifungal Agents; 0/Polyethylene Glycols; 0/Polymers; 1397-89-3/Amphotericin B; 25104-18-1/Polylysine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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