| 19874880 |
Bilkova E, Imramovsky A, Buchta V, Sedlak M: Targeted antifungal delivery system: beta-glucosidase sensitive nystatin-star poly (ethylene glycol) conjugate. Int J Pharm. 2010 Feb 15;386(1-2):1-5. Epub 2009 Oct 27.
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. |
32(0,1,1,2) |