Cationic Nanoliposomes Efficiently Delivering Phenylethyl Resorcinol Produce Enhanced Skin Lightening Effect

Phenylethyl resorcinol-loaded cationic nanoliposomes (PR-CLPs) were prepared and characterized. Moreover, their transdermal properties, cellular uptake, and inhibition of tyrosinase activity and melanin production in B16F10 cells were studied. The mean particle size, polydispersity index (PDI) and zeta potential of the PR-CLPs were [Formula: see text][Formula: see text]nm, [Formula: see text][Formula: see text]mV [Formula: see text][Formula: see text]mV, respectively. The drug loading efficiency (DLE) and entrapment efficiency (EE) of PR in the PR-CLPs were [Formula: see text]% and [Formula: see text]%, respectively. Sustained release of PR from the PR-CLPs was observed in vitro release experiments. The results of the in vitro transdermal experiments showed that PR-CLPs significantly improved both the retention of PR in the skin and its transdermal permeability ([Formula: see text]) in comparison with PR solution or traditional phenylethyl resorcinol nanoliposomes (PR-LPs). The uptake and accumulation of FITC-CLPs in B16F10 cells was significantly enhanced as compared with that of FITC-LPs. Furthermore, at a PR concentration of 20 or 30[Formula: see text][Formula: see text]g/mL, PR-CLPs displayed a high tyrosinase inhibitory activity and caused a noticeable reduction in the melanin content in B16F10 cells. Taken together, these results indicate that PR-CLPs can efficiently deliver phenylethyl resorcinol to produce an enhanced skin lightening effect.