Targeted antifungal delivery system: beta-glucosidase sensitive nystatin-star poly(ethylene glycol) conjugate
Language English Country Netherlands Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
19874880
DOI
10.1016/j.ijpharm.2009.10.034
PII: S0378-5173(09)00760-1
Knihovny.cz E-resources
- MeSH
- Antifungal Agents administration & dosage chemistry metabolism MeSH
- Aspergillus niger enzymology MeSH
- Cellulases isolation & purification metabolism MeSH
- Chemistry, Pharmaceutical MeSH
- Technology, Pharmaceutical methods MeSH
- Chromatography, Gel MeSH
- Hydrolysis MeSH
- Kinetics MeSH
- Hydrogen-Ion Concentration MeSH
- Delayed-Action Preparations MeSH
- Magnetic Resonance Spectroscopy MeSH
- Drug Carriers * MeSH
- Nystatin administration & dosage chemistry metabolism MeSH
- Half-Life MeSH
- Polyethylene Glycols chemistry MeSH
- Drug Compounding MeSH
- Propylene Glycols chemistry MeSH
- Buffers MeSH
- Solubility MeSH
- Spectrophotometry, Ultraviolet MeSH
- Drug Stability MeSH
- Chromatography, High Pressure Liquid MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Antifungal Agents MeSH
- Cellulases MeSH
- Delayed-Action Preparations MeSH
- Drug Carriers * MeSH
- Nystatin MeSH
- pentaerythritol MeSH Browser
- Polyethylene Glycols MeSH
- Propylene Glycols MeSH
- Buffers MeSH
A new targeted intravenous conjugate of nystatin with pentaerythritol poly(ethylene glycol)ether has been prepared and characterised (NY(4)-sPEG, M=25 160). The conjugate contains a beta-d-glucopyranoside molecular switch sensitive to beta-glucosidases (E.C.3.2.1.21), which are specifically present in the enzyme outfit of fungal pathogens. The investigated conjugate is stable under in vitro conditions for 24h (solution of phosphate buffer pH=7.4). Spectrophotometrically controlled releasing of nystatin in model medium containing beta-glucosidase ((Aspergillus niger) 2mg/mL, 66.6 units/g; pH 7.4, 2 x 10(-2)M), reported decomposition half-life of conjugate tau(1/2)=(88+/-2)s. This implies that releasing of nystatin is controlled only enzymatically.
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