engleski

Assessment of liposomes for (trans)dermal drug delivery ; the skin-PVPA as a novel in vitro model

Present study evaluated the applicability of stratum corneum mimicking PVPA barrier in determining the drug penetration abilities of various types of liposomes: conventional liposomes (CL), deformable liposomes (DL) and propylene glycol liposomes (PGL). The skin-phospholipid vesicle-based permeation assay (PVPA) is a novel in vitro skin barrier model based on the tightly packed phospholipid vesicles mimicking structure and composition of stratum corneum. All of the liposomal formulations exhibited significantly higher permeabilities than the aqueous solution of hydrophilic drug, most probably due to the penetration-enhancing effect of the phospholipids. The highest Papp of DCS was attained with PGL-10-A, followed by DL-A, and the lowest values were obtained by CL-A. These results are consistent with the high elasticity of PGL-10-A and DL-A. The permeation of the hydrophilic drug from the liposomes was affected by their physicochemical properties, which were influenced by the lipid composition and the presence of the edge activator or penetration enhancer. This study demonstrates the potential of the newly developed skin-PVPA for the screening and optimization of liposomes at the early preformulation stage.

Deformable liposomes; Propylene glycol liposomes; Skin models; Dermal drug delivery; Permeabilty

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