OBJECTIVE  To study the dermal delivery effect and mechanism of hydrophilic molecules with high molecular weight by cerosomes, and provide foundation for the development of efficient dermal delivery system containing ganoderma lucidum fermentative liquid (GLFL).

  METHODS  Using water-soluble macromolecule fluorescein isothiocyanate-dextran(FD) as fluorescent probe, the impact of ceramide on the dermal delivery effect of liposomes was investigated by Franz diffusion cell method and rat isolated skin, and the intradermal drug distribution was observed by fluorescence microscope. Cerasomes containing GLFL were prepared by thin-film dispersion method. The morphology, particle size, encapsulation efficiency and stability of the prepared cerasomes were measured. Attenuated total reflectance-Fourier transform infrared spectroscopy (FTIR-ATR) was applied to study the mechanism of dermal penetration enhancement mechanism.

  RESULTS  The results of in vitro dermal delivery experiments showed that the 12-hour intradermal retention of liposomes with the ratio of ceramide to soybean phospholipid of 1 ∶ 6 was the highest, which was 2.87 times and 1.78 times of the drug solution and conventional liposomes without ceramide, respectively. Fluorescence microscopy results showed that cerosomes could promote more drugs to penetrate deeper into the skin. The prepared cerasomes were spherical in shape and uniform in size with the average particle size of (259.3±16.7)nm, and the encapsulation efficiency of protein and peptide components was (43.03±0.90)%. ATR-FTIR results showed that cerosomes could change the skin hydration capacity and the main characteristic peak displacement and peak area of stratum corneum lipids and keratins.

  CONCLUSION  Cerasomes may enhance the stratum corneum hydration, change the structure of the skin stratum corneum, and reduce the barrier function, thereby significantly improve the dermal delivery of water-soluble polar substances with high molecular weight.