Evaluation of physicochemical properties, skin permeation and accumulation profiles of salicylic acid amide prodrugs as sunscreen agent

Title
Evaluation of physicochemical properties, skin permeation and accumulation profiles of salicylic acid amide prodrugs as sunscreen agent
Author(s)
용철순엄의동[엄의동]성준호[성준호]이동원[이동원]김정선[김정선]진은미[진은미]김대덕[김대덕]김동욱[김동욱]김종오박명관[박명관]이동훈[이동훈]최한곤[최한곤]
Keywords
IN-VITRO; PERCUTANEOUS-ABSORPTION; TRANSDERMAL DELIVERY; SYSTEMIC ABSORPTION; TOPICAL DELIVERY; BARRIER FUNCTION; ESTER PRODRUGS; PENETRATION; PERMEABILITY; ENHANCERS
Issue Date
201110
Publisher
ELSEVIER SCIENCE BV
Citation
INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.419, no.1-2, pp.154 - 160
Abstract
Various amide prodrugs of salicylic acid were synthesised, and their physicochemical properties including lipophilicity, chemical stability and enzymatic hydrolysis were investigated. In vivo skin permeation and accumulation profiles were also evaluated using a combination of common permeation enhancing techniques such as the use of a supersaturated solution of permeants in an enhancer vehicle, a lipophilic receptor solution, removal of the stratum corneum and delipidisation of skin. Their capacity factor values were proportional to the degree of carbon-carbon saturation in the side chain. All these amides were highly stable in acetonitrile and glycerine. Amide prodrugs were converted to salicylic acid both in hairless mouse liver and skin homogenates. N-dodecyl salicylamide (C12SM) showed the lowest permeation of salicylic acid in skin compared to the other prodrugs, probably due to its low aqueous solubility. It had a high affinity for the stratum corneum and its accumulation was restricted to only the uppermost layer of skin. Thus, this amide prodrug could be a safer topical sunscreen agent with minimum potential for systemic absorption. (C) 2011 Elsevier B.V. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/24406http://dx.doi.org/10.1016/j.ijpharm.2011.07.043
ISSN
0378-5173
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약학대학 > 약학부 > Articles
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