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The aim of the study was to investigate a system using liposomes and cell penetrating peptides (CPP) for optimal transdermal delivery of macromolecules. CPP-conjugated liposomes resulted higher cellular uptake efficiency compared to typical liposomes, showing higher fluorescent intensity. In confocal laser scanning microscope studies, for Rhodamine B, having a relatively small molecular weight, absorption into the cell was successful, and showed the highest rate of cellular uptake with CPP-conjugated liposomes. Dextran-RITC, a macromolecule with a relatively bigger molecular weight, showed similar results to Rhodamine B. In terms of skin permeation, CPP-conjugated liposomes containing Rhodamine B showed noticeable skin absorption after 4 and 18 hours, and the permeation range was wider and thicker than that with typical liposomes. For Dextran-RITC with typical DOPE liposome, it was hardly permeable through the skin, but for that with CPP-conjugated liposomes, the skin permeations after 4 and 18 hours were remarkable. The improved cellular uptake and skin permeation of the CPP-conjugated liposomes are due to the cationic arginine-rich peptide. In vivo studies also proved that the CPP-conjugated liposomes are superior in depigmentation and anti-wrinkle studies than typical liposomes. These results demonstrate that the CPP-conjugated liposomes could also be effective for transdermal drug delivery of antioxidant and anti-aging therapeutics.
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