Aim: The development and characterization of nanostructured flavanone formulations (FF) of 1 extracted from Eysenhardtia platycarpa and 1a, 1b, 1c and 1d derivatives by structural modification of 1 as anti-inflammatory candidates for topical treatment of local inflammation. Materials & methods: The FF were physicochemical characterized and the behavior release, skin permeation and, in vivo anti-inflammatory efficacy in the rat model were studied. Results: The FF revealed sustained drug release and showed slow drug penetration in human skin. The FF reduced inflammation in comparison with the standard formulation. Conclusion: The FF could be effective systems for the delivery and controlled release of flavanones on the skin, and the chemical modification of lead molecule 1 improved the efficacy.
Keywords: ex vivo permeation; in vitro release; in vivo anti-inflammation; nanostructured formulations; natural and derivatives flavanones.