DOI: 10.21276/sajp.2016.5.8.7

Pages: 350-358

In this work, a selective and sensible analytical method by reversed phase high performance liquid chromatography was developed and validated. The method was applied in several preformulation assays of a novel benzophenone derivative denominated LFQM117. This compound was selected due to its potential as leishmanicidal drug candidate to topical therapy. Preformulation assays included the LFQM117 physicochemical characterisation as solubility in different vehicles, oil-water partition coefficient (log P) and in vitro skin absorption studies of LFQM117. Forced stress tests were also performed to assess the intrinsic stability of this compound. The results showed that the analytical method developed was suitable to be employed in the preformulation tests carried out in this work. The preformulation studies indicated that LFQM117 showed low water solubility and high lipophilicity (log P = 4.8). And the LFQM117 remained stable under forced stress conditions. The skin absorption studies showed that LFQM117 permeation through the porcine ear skin was significantly increased by addition of oleic acid (absorption enhancer). And this study was the starting point for the development of topical formulations with LFQM117