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Influence of physicochemical properties on the in vitro skin permeation of the enantiomers, racemate, and eutectics of ibuprofen for enhanced transdermal drug delivery

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dc.contributor.author Capomacchia, Anthony C.
dc.contributor.author Yuan, Xudong
dc.date.accessioned 2017-10-17T10:53:20Z
dc.date.available 2017-10-17T10:53:20Z
dc.date.copyright 2013 en_US
dc.identifier.issn 1520-6017 en_US
dc.identifier.uri http://hdl.handle.net/10725/6329
dc.description.abstract Physicochemical properties of chiral ibuprofen are significant to formulation scientists because its enantiomers and eutectics possess lower melting points than its racemate. The influence of these properties on transdermal formulation development, especially the relative effect of lowered melting point, on skin permeation must be carefully assessed to provide the most efficacious formulation. Thermodynamic properties and crystalline structures of the enantiomers, eutectics, and racemate of chiral ibuprofen were investigated by differential scanning calorimetry and X-ray powder diffraction. The effect of melting point lowering on membrane permeation rates was mathematically modeled. Model was validated by in vitro skin permeation experiments using different preparations of racemic ibuprofen, enantiomer, and eutectic. Both enantiomer and eutectic formed a two-phase liquid system containing an emulsifiable aqueous phase and an oily phase in the presence of aqueous isopropyl alcohol (aIPA). The eutectic emulsion had the highest permeation rate, a 2.21-fold increase in flux compared with saturated aIPA solutions of the racemate with a 2.03-fold increase in flux. Results from the two-phase liquid system supported those from the mathematical models, albeit somewhat lower, and confirmed their use in predicting maximum flux utilizing thermodynamic data. Study data also supported the idea that eutectic formation, for ibuprofen and probably other chiral drugs, may be one of the best ways to develop topical formulations for improved percutaneous absorption to avoid the use of permeation enhancers or synthetically modifying chemical structure. en_US
dc.language.iso en en_US
dc.title Influence of physicochemical properties on the in vitro skin permeation of the enantiomers, racemate, and eutectics of ibuprofen for enhanced transdermal drug delivery en_US
dc.type Article en_US
dc.description.version Published en_US
dc.author.school SOP en_US
dc.author.idnumber 201408778 en_US
dc.author.department Pharmaceutical Sciences Department en_US
dc.description.embargo N/A en_US
dc.relation.journal Journal of Pharmaceutical Sciences en_US
dc.journal.volume 102 en_US
dc.journal.issue 6 en_US
dc.article.pages 1957-1969 en_US
dc.identifier.doi http://dx.doi.org/10.1002/jps.23548 en_US
dc.identifier.ctation Yuan, X., & Capomacchia, A. C. (2013). Influence of physicochemical properties on the in vitro skin permeation of the enantiomers, racemate, and eutectics of ibuprofen for enhanced transdermal drug delivery. Journal of pharmaceutical sciences, 102(6), 1957-1969. en_US
dc.author.email anthony.capomacchia@lau.edu.lb en_US
dc.identifier.tou http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php en_US
dc.identifier.url http://onlinelibrary.wiley.com/doi/10.1002/jps.23548/full en_US
dc.author.affiliation Lebanese American University en_US


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