Targeted antifungal delivery system: β-Glucosidase sensitive nystatin-star poly(ethylene glycol) conjugate

被引：19

作者：

Bilkova, Eliska ^{[1
]}

Imramovsky, Ales ^{[1
]}

Buchta, Vladimir ^{[2
,3
]}

Sedlak, Milos ^{[1
]}

机构：

[1] Univ Pardubice, Fac Chem Technol, Dept Organ Chem & Technol, Pardubice 53210, Czech Republic

[2] Charles Univ Prague, Sch Med, Dept Clin Microbiol, Hradec Kralove 50005, Czech Republic

[3] Teaching Hosp, Hradec Kralove 50005, Czech Republic

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2010年 / 386卷 / 1-2期

关键词：

Nystatin; Star poly(ethylene glycol); Drug polymer conjugates; beta-Glucosidase sensitivity; Controlled release in vitro; AMPHOTERICIN-B; ANTIBIOTICS;

D O I：

10.1016/j.ijpharm.2009.10.034

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A new targeted intravenous conjugate of nystatin with pentaerythritol poly(ethylene glycol)ether has been prepared and characterised (NY4-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) 2 mg/ml., 66.6 units/g; pH 7.4,2 x 10(-2) M), reported decomposition half-life of conjugate T-1/2 = (88 +/- 2) s. This implies that releasing of nystatin is controlled only enzymatically. (C) 2009 Elsevier B.V. All rights reserved.

引用

页码：1 / 5

页数：5