Prediction of skin permeation and concentration of rhododendrol applied as finite dose from complex cosmetic vehicles

Abstract

Finite dose experiments represent clinical use wherein depletion of dose, evaporation of excipients, and gradual change in vehicle composition may occur. In the present study, we attempted a mathematical approach for predicting skin permeation and concentration of a cosmetic active, rhododendrol (RD), from complex vehicle-based formulations applied in finite dose. In vitro skin permeation and concentration studies of RD were conducted from formulations containing water and polyols with concentrations ranging from 10 to 100% under infinite and finite dose conditions using vertical Franz diffusion cells. Observed data for skin permeation and the viable epidermis and dermis (VED) concentration of RD were estimated by the differential equations under Fick's second law of diffusion together with water evaporation kinetics and changes in the partition coefficient from vehicles to the stratum corneum. As a result, a goodness-of-fit was observed allowing accurate estimation of skin permeation and VED concentration of RD. This mathematical approach could become a useful tool to estimate the skin permeation and concentration of actives from topical formulation applied in finite dose conditions likened in actual use.

Keywords: Butylene glycol (PubChem CID: 7896); Cosmetic ingredients; Fick’s second law of diffusion; Finite dose; Glycerol (PubChem CID: 753); Residual formulation; Rhododendrol (PubChem CID: 919204); Skin concentration; Skin permeation; Sorbitol (PubChem CID: 5780); Trichloroacetic acid (PubChem CID: 6421).