Investigation of skin penetration enhancing mechanism of limonenecontaining liposome entrapped hydrophilic compound
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Abstract
Introduction: Penetration enhancer-containing liposome vesicles have been reported as a carriers for transdermal delivery of entrapped drug. The aim of this study was to investigate the
penetration enhancing mechanism of limonene-containing liposomes (LI) on the transdermal delivery of hydrophilic compound. Methods: NaFI was used as a model hydrophilic compound for loading into liposome vesicles. The physicochemical characteristics of liposome formulations were evaluated. The in vitro skin penetration study was performed by using Franz diffusion cells. Transmission electron microscopy (TEM) was used to observe the penetrated vesicles in the receiver medium. Fourier transform infrared spectroscopy (FTIR) was used to determine the modification of intercellular lipid organization of stratum corneum. Results: The physicochemical properties of LI showed smaller vesicle size (40.59 nm), higher entrapment efficiency, and higher membrane fluidity than liposomes without limonene. The skin penetration of NaFI-entrapped in LI was higher than non NaFI-entrapped in LI, NaFI-entrapped in liposomes without limonene, and NaFI solution, respectively. TEM image showed LI vesicles penetrated through skin into the receiver compartment. FTIR result of LI treated stratum corneum also exhibited high fluidity of intercellular lipid organization of stratum corneum barrier. Conclusion: The skin penetration enhancement of limonene-containing liposomes might result from LI as transdermal carriers to deliver the entrapped drug through skin. Moreover, limonene (as a penetration enhancer) provided the main modification in the stratum corneum barrier, leading to increase of skin penetration of hydrophilic compound.
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