Al-Marabeh S1, Khalil E2, Khanfar M1, Al-Bakri AG2, Alzweiri M1,3.
Pharm Dev Technol. 2016 Jun 27:1-9. [Epub ahead of print]Azelaic acid is a dicarboxylic acid compound used in treatment of acne vulgaris. However, high concentration (ca 20%) is needed to guarantee the drug availability in the skin. The latter increases the incidence of side effects such as local irritation. The prodrug strategy to enhance azelaic acid diffusion through skin was not reported before. Thus, a lipophilic prodrug of azelaic acid (diethyl azelate [DEA]) was synthesized and investigated to improve percutaneous availability of azelaic acid, with a subsequent full physical, chemical, and biological characterization. Read More