EFFECT OF PEGYLATED TRANSFERSOMES CONTAINING MACROMOLECULAR PROTEIN ON TRANSDERMAL DELIVERY

Abstract

Hydrophilic protein macromolecules are limited to passively penetrate through the skin. The objective of this study was to investigate the effect of various concentrations of PEGylation (1, 5 and 10%) grafted liposomes for delivering macromolecular protein through the skin. PEGylated transfersomes composed of phosphatidylcholine (PC), cholesterol (Chol), DSPE-PEG2000, Tween20 and d-limonene were prepared for loading bovine serum albumin (BSA) as macromolecular protein model. The characterizations of these nanocarriers were evaluated such as size, PDI, zeta potential and %loading capability (%LC). The in vitro permeation study was performed by using Franz diffusion cells through porcine skins.  BSA-FITC content was analyzed using a fluorescence spectrophotometer. For the results, all formulations showed narrow size distributions (PDI<0.3). The sizes and zeta potential of all transfersomes were 43.90±1.75, 44.39±7.20 and 42.98±0.32 nm, and -9.95±0.22, -12.53±1.96, -12.93±1.44 mV, respectively, which increasing the PEGylation decreased the particle size and increased negative charge. %LC of all transfersomes was in the range of 9.70-13.33. The permeation study showed that the skin treated with 5% transfersomes has higher macromolecular protein delivery through skin than other formulations, because higher hydrophilic PEG content might provide higher conformational change on the surface of the transfersomes, leading to increase the skin hydration and then enhance the hydrophilic BSA-FITC penetrated through the skin. In conclusion, the concentration of PEGylation on the liposomes structure significantly affects the physicochemical properties (p < 0.05) leading to improve the skin permeability of hydrophilic protein macromolecules.