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

Vijay Pawar

doi:10.3797/scipharm.1406-19

Abstract

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, triethanolamine, 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.

Highlights

Arthritis is a form of joint disorder involving inflammation, pain, and swelling of one or more joints
Due to the presence of the acidic functional group in biphenylacetic acid (BPA), we prepared some salts of this NSAID with organic and alkali metal bases
The amino group will react with the acidic carboxylic acid group present in the BPA resulting in salt formation

Summary

Introduction

Arthritis is a form of joint disorder involving inflammation, pain, and swelling of one or more joints. For the safe and effective treatment of osteoarthritis (OA), the current new Enhancing Skin Permeation of Biphenylacetic Acid (BPA) Using Salt Formation with Organic and ... For the evaluation of various physicochemical parameters such as aqueous solubility, partition coefficient, and in vitro skin permeability, the HPLC method was developed, calibration curves for BPA (1) were plotted, and the linearity range was calculated.

Results

Conclusion