Abstract
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.
Copyright 2009 Elsevier B.V. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antifungal Agents / administration & dosage
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Antifungal Agents / chemistry*
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Antifungal Agents / metabolism
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Aspergillus niger / enzymology*
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Buffers
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Cellulases / isolation & purification
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Cellulases / metabolism*
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Chemistry, Pharmaceutical
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Chromatography, Gel
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Chromatography, High Pressure Liquid
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Delayed-Action Preparations
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Drug Carriers*
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Drug Compounding
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Drug Stability
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Half-Life
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Hydrogen-Ion Concentration
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Hydrolysis
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Kinetics
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Magnetic Resonance Spectroscopy
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Nystatin / administration & dosage*
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Nystatin / chemistry
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Nystatin / metabolism
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Polyethylene Glycols / chemistry*
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Propylene Glycols / chemistry*
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Solubility
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Spectrophotometry, Ultraviolet
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Technology, Pharmaceutical / methods
Substances
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Antifungal Agents
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Buffers
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Delayed-Action Preparations
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Drug Carriers
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Propylene Glycols
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Nystatin
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Polyethylene Glycols
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Cellulases
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pentaerythritol