Document Detail

Prednisolone-α-cyclodextrin-star PEG polypseudorotaxanes with controlled drug delivery properties.
MedLine Citation:
PMID:  20859603     Owner:  NLM     Status:  MEDLINE    
The reaction of α-amino-ω-methoxypoly(ethylene glycol) [M = 5000] or star α-amino-poly(ethylene glycol) [M = 20 000] with hemiesters of prednisolone dicarboxylic acids (succinic, glutaric, adipic, phthalic acid) has been used to prepare the corresponding conjugates. The rate of esterase catalyzed hydrolysis of the conjugates is controlled by the molecular mass of poly(ethylene glycol) and the length of the linker between prednisolone and poly(ethylene glycol) (τ(1/2)∼ 5-0.5 h). The enzymatic hydrolysis proceeds most rapidly at conjugates with linkers derived from adipic and phthalic acids. The synthesized conjugates form polypseudorotaxanes with α-cyclodextrin which were characterized by 2D NOESY NMR spectra, powder X-ray diffraction patterns and in one case also by STM microscopy. In the case of the polypseudorotaxane having the linker derived from adipic acid, the enzymatic release proceeds ca. five times slower in comparison with the rate of prednisolone release from the corresponding conjugate. The rate of prednisolone release from the carrier can be controlled by three factors: character of the linker between the polymeric carrier and prednisolone, the molecular mass of poly(ethylene glycol) and complex formation with α-cyclodextrin. The synthesized polypseudorotaxanes represent new promising transport systems intended for targeted release of prednisolone in transplanted liver.
Eliška Bílková; Miloš Sedlák; Bohuslav Dvořák; Karel Ventura; Petr Knotek; Ludvík Beneš
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-09-22
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  8     ISSN:  1477-0539     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-11-10     Completed Date:  2011-02-01     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  5423-30     Citation Subset:  IM    
Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentská 573, 532 10 Pardubice, Czech Republic.
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MeSH Terms
Cyclodextrins / chemistry*
Microscopy, Scanning Tunneling
Molecular Structure
Poloxamer / chemistry*
Polyethylene Glycols / chemistry*
Prednisolone / chemistry*
Rotaxanes / chemistry*
alpha-Cyclodextrins / chemistry*
Reg. No./Substance:
0/Cyclodextrins; 0/Polyethylene Glycols; 0/Rotaxanes; 0/alpha-Cyclodextrins; 0/pseudopolyrotaxane; 10016-20-3/alpha-cyclodextrin; 106392-12-5/Poloxamer; 50-24-8/Prednisolone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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