Synthesis and characterisation of a new pH-sensitive amphotericin B--poly(ethylene glycol)-b-poly(L-lysine) conjugate
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
17336066
DOI
10.1016/j.bmcl.2007.02.009
PII: S0960-894X(07)00196-5
Knihovny.cz E-resources
- MeSH
- Amphotericin B analogs & derivatives chemical synthesis MeSH
- Antifungal Agents chemical synthesis pharmacology MeSH
- Models, Chemical MeSH
- Chemistry, Pharmaceutical methods MeSH
- Hydrogen-Ion Concentration MeSH
- Molecular Conformation MeSH
- Polyethylene Glycols chemistry MeSH
- Polylysine chemistry MeSH
- Polymers chemistry MeSH
- Drug Design MeSH
- Spectrophotometry, Ultraviolet methods MeSH
- Temperature MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Amphotericin B MeSH
- Antifungal Agents MeSH
- Polyethylene Glycols MeSH
- Polylysine MeSH
- Polymers MeSH
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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