In vitro permeation and skin retention of alpha-mangostin proniosome

Abstract

Alpha-mangostin has been identified as a potent anti-melanogenesis compound in vitro on B16F1 melanoma cells. A concentration of 5 µg/mL demonstrated promising anti-melanogenesis effect without compromising the cell viability. However, due to its high lipophilic nature, the cosmeceutical application of a-mangostin in topical formulation is restricted. The current investigation aimed to evaluate the potential of proniosome as a carrier to enhance skin permeation and skin retention of a-mangostin. Alpha-mangostin proniosomal formulations were prepared using coacervation phase separation method. Upon hydration, a-mangostin-loaded niosomes were characterized for size, polydispersity index, entrapment efficiency, zeta potential and morphology. Using different surfactants, preliminary study to evaluate skin concentration suggested that Spans significantly (p < 0.05) enhanced deposition of a-mangostin in the viable epidermis/dermis layer (VED) as compared to Tween 60. Incorporation of soya lecithin in the proniosomal formulation also significantly enhanced the VED concentration of a-mangostin. The in vitro permeation experiments using dermis-split Yucatan Micropig skin revealed that proniosomes composed of Spans, soya lecithin and cholesterol were able to enhance the skin permeation of a-mangostin with a factor range from 1.8 to 8.0-fold as compared to the control suspension. All the proniosomal formulations (except for S20L) had significantly (p < 0.05) enhanced the deposition of a-mangostin in the VED layer with a factor range from 2.5 to 2.9-fold as compared to the control suspension. Proniosome S85L showed the highest permeation profile (8.0-fold) and the highest enhancement of VED concentration of a-mangostin (2.9-fold). Collectively, these results suggested that proniosomes can be utilized as a promising carrier for a highly lipophilic compound like a-mangostin.