Water-in-oil microemulsions composed of monoolein enhanced the transdermal delivery of nicotinamide.

Objective Nicotinamide, also known as niacinamide, is a water-soluble vitamin that is used to prevent and treat acne and pellagra. It is often found in water-based skin care cosmetics because of its high water-solubility. Nicotinamide is a small molecule with a molar mass of 122.1 g/mol. However, it has a hydrophilic nature that becomes an obstacle when it penetrates through the skin. The topmost layer of the skin, the stratum corneum, acts as a strong hydrophobic barrier for such hydrophilic molecules. The oil-based formulations are expected to enhance the transdermal delivery efficiency of nicotinamide. Methods We have developed oil-based microemulsion formulations composed of a squalane-vehicle. Monoolein was used as an emulsifier that has a potential to enhance the nicotinamide delivery through the stratum corneum. Results Because the mean size of the emulsions measured by dynamic light scattering was 20.9 ± 0.4 nm, the microemulsion formulation was stable under the long-term storage. Monoolein acted as a skin penetration enhancer, and it effectively enabled the penetration of nicotinamide through human abdominal skin, compared with nicotinamide in a phosphate buffered saline solution. The flux was increased 25-fold. Microscopic imaging revealed that the hydrophilic bioactive compounds penetrated through the intercellular spaces in the epidermis. Conclusion The monoolein-based microemulsion was transparent and stable, suggesting that it is a promising formulation for a transdermal nicotinamide delivery.