Preparation and characterization of novel pseudo ceramide liposomes for the transdermal delivery of baicalein

Abstract

To overcome the disadvantages of natural ceramides, pseudo ceramides (PO3C, 6C, and 9C) were synthesized and used to construct pseudo ceramide liposomes. The liposomes prepared using PO9C were the smallest in size, with a 130 nm particle size when the PO9C:PC content was 2:1. Also, the stability was higher than ordinary ceramide liposomes(CLs). The PC:ceramide ratio of 2:1, in which the particle size of the liposome as well as its stability was optimal, was finally selected to carry baicalein (BAI). Entrapment efficiency of the common CLs was 78.40%, whereas that of the pseudo CLs was over 80%. Notably, liposomes using ω9CL exhibited the highest entrapment efficiency. The morphology of BAI-loaded pseudo CLs were confirmed by TEM. The concentrations of BAI loaded in ordinary CLs present in the stratum corneum, epidermis and dermis, and transdermal permeation were 7.82, 38.59, and 49.46 μg/cm3, respectively. These were closely similar to concentrations of the pseudo CLs, BAI-ω9CL (8.37, 45.04, and 46.31 μg/cm3). In conclusion, it is suggested that the pseudo CLs carrying BAI (BAI-ω9CLs) are as effective as ordinary CLs in delivering the drug to the skin, but have the added advantage of being more stable.