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Vesicular carriers containing phenylethyl resorcinol for topical delivery system; liposomes, transfersomes and invasomes

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Asian Journal of Pharmaceutical Sciences 2018年第5期13卷 472-484页

作者： Thanaporn Amnuaikit Tunyaluk Limsuwan Pasarat Khongkow prapaporna boonme Department of Pharmaceutical Technology Faculty of Pharmaceutical Sciences Prince of Songkla University Institute of Biomedical Engineering Faculty of Medicine Prince of Songkla University Nanotec-PSU Center of Excellence on Drug Delivery System

Topical administration of phenylethyl resorcinol(PR) has attracted much attention as skin lightening agent with potent anti-tyrosinase activity. Two novel types of elastic carriers were developed to overcome the limitation of PR as topical delivery by increasing the solubility, stability and decreasing skin irritation compared to conventional liposomes. In addition, it also promotes skin penetration of PR to reach deep skin layer at the target site. The lead formulations were obtained from the invasomes containing 1%(w/v) d-limonene mixed with 10%(v/v) absolute ethanol as the skin enhancer, and transfersomes containing 15%(w/w) sodium deoxycholate(SDC) as edge activator. All formulations gave a vesicle size 50%, and good stability on storage at 30 °C at 75% RH for 4 months. Transfersomes have a lower degree of deformability(6.63%) than invasomes(25.26%). In contrast, the liposomes as rigid vesicles do not show a deformable property. This characteristic affects the skin permeation, and thus, transfersomes with high elastic property provided a significantly higher cumulative amount, steady state flux( J ss) and permeability coefficient( K p) compared to other formulations. However, in vitro PR accumulation in full-thickness newborn pig skin demonstrated that the application of elastic carrier formulations gave significantly higher accumulation than liposomes, and gave anti-tyrosinase activity up to 80%. These results are straightforwardly related to the results of cellular level study. Transfersomes and invasomes showed higher tyrosinase inhibition activity and melanin content reduction when compared to liposomes in B16 melanoma cells. In addition, acute irritation test in rabbits confirmed that these formulations are safe for skin application. Therefore, elastic vesicle carriers have theefficiency to deliver PR into the deep skin in both quantity and effectiveness which are better than conventional liposomes and appropriate for

关键词： Phenylethyl resorcinol Transfersomes Invasomes Tyrosinase inhibition

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