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Sci. Pharm. 2015, 83(1), 191-205; doi:10.3797/scipharm.1406-19 (registering DOI)

Enhancing Skin Permeation of Biphenylacetic Acid (BPA) Using Salt Formation with Organic and Alkali Metal Bases

Pharmacy Department, Faculty of Technology & Engineering, The M. S. University of Baroda, Vadodara-390001, India
Author to whom correspondence should be addressed.
Received: 30 June 2014 / Accepted: 26 September 2014 / Published: 26 September 2014
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In the present study, a series of organic and alkali metal salts of biphenylacetic acid (BPA) have been prepared and evaluated in vitro for percutaneous drug delivery. The physicochemical properties of BPA salts were determined using solubility measurements, DSC, and IR. The DSC thermogram and FTIR spectra confirmed the salt formation with organic and alkali metal bases. Among the series, salts with organic amines (ethanolamine, diethanolamine, triethanol-amine, and diethylamine) had lowered melting points while the alkali metal salt (sodium) had a higher melting point than BPA. The in vitro study showed that salt formation improves the physicochemical properties of BPA, leading to improved permeability through the skin. Amongst all the prepared salts, ethanolamine salt (1b) showed 7.2- and 5.4-fold higher skin permeation than the parent drug at pH 7.4 and 5.0, respectively, using rat skin.
Keywords: BPA; Lipophilicity; NSAID; Salt; Skin permeation BPA; Lipophilicity; NSAID; Salt; Skin permeation
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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PAWAR, V.; NAIK, P.; GIRIDHAR, R.; YADAV, M.R. Enhancing Skin Permeation of Biphenylacetic Acid (BPA) Using Salt Formation with Organic and Alkali Metal Bases. Sci. Pharm. 2015, 83, 191-205.

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