| Literature DB >> 17257788 |
Lucia Montenegro1, Claudia Carbone, Claudio Maniscalco, Daniela Lambusta, Giovanni Nicolosi, Cinzia A Ventura, Giovanni Puglisi.
Abstract
Quercetin-3-O-acyl esters (I-VI) were synthesized and their usefulness as quercetin topical prodrugs was evaluated. Quercetin esters were assayed to determine their water stability and solubility, their susceptibility to undergoing enzymatic hydrolysis and their permeation through excised human skin. Quercetin ethyl (I) and hexyl (IV) esters proved poorly stable in aqueous media and they were not assayed further. Among the derivatives tested, quercetin propyl (II) and butyl (III) esters were more water-soluble than the parent drug. Esters II, III and V were readily hydrolyzed by human plasma and esters II and III penetrated excised human skin better than quercetin from aqueous saturated solutions. On the basis of the results obtained, esters II and III could be regarded as promising quercetin topical prodrugs.Entities:
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Year: 2006 PMID： 17257788 DOI： 10.1016/j.ijpharm.2006.12.003
Source DB: PubMed Journal: Int J Pharm ISSN： 0378-5173 Impact factor: 5.875