Effect of Cubic Liquid Crystalline Systems on Skin Localization of Oregonin and Hirsutanonol

Abstract

Monoolein-based cubic liquid crystalline systems were formulated for the local delivery of oregonin and hirsutanonol for the treatment of atopic dermatitis. The liquid crystalline phase and its nanodispersion containing drugs were prepared. The skin permeation and deposition properties of the drugs were examined in normal and delipidized rat skin. The proportion of oregonin (%) deposited in normal skin after topical administration of the drugs in the form of aqueous solution, cubic phase or cubic nanodispersions were <TEX>$1.53\;{\pm}\;0.46$</TEX>, <TEX>$3.62\;{\pm}\;0.17$</TEX> and <TEX>$5.13\;{\pm}\;0.73$</TEX>, and those of hirsutanonol were <TEX>$2.46\;{\pm}\;0.02$</TEX>, <TEX>$5.44\;{\pm}\;0.27$</TEX> and <TEX>$17.28\;{\pm}\;2.19$</TEX>, respectively. The greater lipophilicity and thus greater skin affinity of hirsutanonol than oregonin contributed the greater amount of skin deposition. The monoolein-based liquid crystalline phases significantly increased the amount of both drugs permeated and deposited. Approximately 3.2, 2.1 and 3.0 times greater amount of oregonin, and 3.4, 2.1 and 2.2 times greater amount of hirsutanonol were deposited in delipidized skin after administration of each drug in the form of aqueous solution, cubic phase and cubic nanodispersions system, respectively, because of lowered barrier function of the delipidized skin. In this study, the effects of drug property, vehicles type and skin condition on skin deposition and permeation properties of drug were examined and concluded that monoolein-based liquid crystalline systems would be a promising formulation for the local delivery of drugs.