Non-aqueous self-double-emulsifying drug delivery system: A new approach to enhance resveratrol solubility for effective transdermal delivery

• The non-aqueous SDEDDS could improve trans-resveratrol solubility through formulations optimization.
• The SDEDDS could release the oil phase to form fine oil-in-oil-in-water emulsions, with a sustained release of trans-resveratrol.
• trans-Resveratrol from SDEDDS will be higher than the drug permeation from the free form aqueous solution.

trans-Resveratrol, a naturally occurring polyphenol has attracted considerable interest for its beneficial potentials for human health. However, the biological effects of trans-resveratrol appear strongly limited by its low solubility, which is a barrier to the development of therapeutic applications. Herein, we developed a novel formulation, non-aqueous self-double-emulsifying drug delivery systems (SDEDDS) by formulating mixtures of hydrophilic surfactants and oil-in-oil (O/O) emulsions, which could improve trans-resveratrol solubility through formulations optimization. SDEDDS can spontaneously emulsify to oil-in-oil-in-water double emulsions in the mixed aqueous solution, with drugs encapsulated in the internal oil phase of the double emulsions. We employed non-aqueous SDEDDS to improve the skin retention of trans-resveratrol solubility, a polyphenol drug with poor solubility. The optimized trans-resveratrol-SDEDDS was found to be stable up to 3 months under 30 °C and 40 °C. In vitro transdermal studies revealed that trans-resveratrol from SDEDDS will most likely be higher than the drug permeation from the same dose of the free form aqueous solution. These studies demonstrated that non-aqueous SDEDDS might be a promising strategy for topical delivery of poor solubility drug.

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