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Evaluation of physicochemical properties, skin permeation and accumulation profiles of ketorolac fatty ester prodrugs

Title
Evaluation of physicochemical properties, skin permeation and accumulation profiles of ketorolac fatty ester prodrugs
Author
최한곤
Keywords
ketorolac fatty ester prodrug; skin permeation; skin accumulation
Issue Date
2007-11
Publisher
PHARMACEUTICAL SOC JAPAN
Citation
BIOLOGICAL & PHARMACEUTICAL BULLETIN, v. 30, No. 11, Page. 2211-2216
Abstract
The purpose of this study was to evaluate the physicochemical properties, skin permeation and accumulation profiles of model lipophilic ketorolac fatty ester (esters) prodrugs. Ketorolac linoleate (C18:2), oleate (C18:1) and stearate (C18:0) were evaluated for their solubility, capacity factor, enzymatic hydrolysis, chemical stability, and skin permeation and accumulation profiles using the combination of common permeation enhancing techniques such as the use of supersaturated solution of permeants in the enhancer vehicle, lipophilic receptor solution, enhancer pretreatment of skins, removal of stratum corneum and delipidization of skins etc. Esters were highly lipophilic, chemically stable for the duration of observation, enzymatically unstable in hairless mouse skin/liver homogenates and plasma, and impermeable into the receptor solution. Absence of skin permeation, relative enzymatic stability during permeation and chemical stability of these esters could delineate preliminary possibilities for designing safer topical agents without systemic absorption.
URI
https://www.jstage.jst.go.jp/article/bpb/30/11/30_11_2211/_article/-char/ja/http://repository.hanyang.ac.kr/handle/20.500.11754/107328
ISSN
0918-6158
DOI
10.1248/bpb.30.2211
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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