Clinical, Cosmetic and Investigational Dermatology (Dec 2015)
Phosphatidylcholine liposomes as carriers to improve topical ascorbic acid treatment of skin disorders
Abstract
Gabriel Serrano,1,* Patricia Almudéver,2,* Juan-Manuel Serrano,1 Javier Milara,2–5 Ana Torrens,1 Inmaculada Expósito,1 Julio Cortijo2–51Sesderma Laboratorios, 2Department of Pharmacology, Faculty of Medicine, University of Valencia, 3Clinical Research Unit, University General Hospital Consortium, 4CIBERES, Health Institute Carlos III, 5Research Foundation of the University General Hospital of Valencia, Valencia, Spain*These authors contributed equally to this workAbstract: Liposomes have been intensively investigated as carriers for different applications in dermatology and cosmetics. Ascorbic acid has potent antioxidant and anti-inflammatory properties preventing photodamage of keratinocytes; however, due to its instability and low skin penetration, an appropriate carrier is mandatory to obtain desirable efficacy. The present work investigates the ability of a specific ascorbate phosphatidylcholine (PC) liposome to overcome the barrier of the stratum corneum and deliver the active agent into the dermis to prevent photodamage. Abdominal skin from ten patients was used. Penetration of PC liposomes was tested ex vivo in whole skin, epidermis, and dermis by means of fluorescein and sodium ascorbate. Histology and Franz diffusion cells were used to monitor the percutaneous absorption. Ultraviolet (UV)-high performance liquid chromatography was used to analyze diffusion of sodium ascorbate through the different skin layers, while spectrofluorimetry and fluorescent microscopy were used for fluorescein monitoring. UVA/UVB irradiation of whole skin was applied to analyze the antioxidant capacity by Trolox assay and anti-inflammatory effects by tumor necrosis factor alpha and interleukin 1 beta enzyme-linked immunoassay. PC liposomal formulation improved skin penetration of fluorescein and ascorbate. Fluorescein PC liposomes showed better diffusion through epidermis than dermis while ascorbate liposomes showed better diffusion through the dermis than the epidermis. Ascorbate PC liposomes showed preventive antioxidant and anti-inflammatory properties on whole human skin irradiated with UVA/UVB. In summary, ascorbate PC liposomes penetrate through the epidermis and allow nonstable hydrophilic active ingredients reach epidermis and dermis preventing skin photodamage.Keywords: skin absorption, liposomes, phosphatidylcholine, sodium ascorbate, fluorescein
