Prednisolone-α-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system

被引：20

作者：

Bilkova, Eliska ^{[1
]}

Sedlak, Milos ^{[1
]}

Imramovsky, Ales ^{[1
]}

Charova, Petra ^{[2
]}

Knotek, Petr

Benes, Ludvik

机构：

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

[2] Univ Pardubice, Dept Analyt Chem, Fac Chem Technol, Pardubice 53210, Czech Republic

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2011年 / 414卷 / 1-2期

关键词：

pH-sensitivity; Pro-drugs; PEG; Polypseudorotaxane; Prednisolone; RELEASE SYSTEM; AMPHOTERICIN-B; POLYROTAXANE; NECKLACE;

D O I：

10.1016/j.ijpharm.2011.04.060

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The acylation of prednisolone 20-hydrazone with star poly(ethylene glycol) tetracarboxylic acid (M = 20,000) has been used to prepare the corresponding pH-sensitive conjugate. With alpha-cyclodextrin, this conjugate forms a polypseudorotaxane, which was characterised by means of H-1 NMR spectra, powder X-ray diffraction patterns and STM microscopy. The rate of acid-catalysed hydrolysis of the conjugate was studied under in vitro conditions in model media of hydrochloric acid solutions, phosphate and acetate buffers (pH 2-5.8). The acid-catalysed hydrolysis (at pH 2) of the polypseudorotaxane was ca 3.5 times slower than that of the original conjugate. After 1 h in this medium, 86% of the covalently attached prednisolone remained unchanged. The prepared polypseudorotaxane represents a promising peroral transport system of prednisolone with a pH-sensitive linker with delayed acid-catalysed hydrolysis thanks to protection at the molecular level using alpha-cyclodextrin. (C) 2011 Elsevier B.V. All rights reserved.

引用

页码：42 / 47

页数：6

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