Cristiano Maria Chiara, Froiio Francesca, Spaccapelo Roberta, Mancuso Antonia, Nisticò Steven P, Udongo Betty P, Fresta Massimo, Paolino Donatella
Department of Experimental and Clinical Medicine, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", viale Europa, 88100 Catanzaro, Italy.
Department of Experimental Medicine, University of Perugia, Piazzale Lucio Severi n. 1, 06132 Perugia, Italy.
Pharmaceutics. 2019 Dec 19;12(1):6. doi: 10.3390/pharmaceutics12010006.
Sulforaphane is a multi-action drug and its anticancer activity is the reason for the continuous growth of attention being paid to this drug. Sulforaphane shows an in vitro antiproliferative activity against melanoma and other skin cancer diseases. Unfortunately, this natural compound cannot be applied in free form on the skin due to its poor percutaneous permeation determined by its physico-chemical characteristics. The aim of this investigation was to evaluate ethosomes and transfersomes as ultradeformable vesicular carriers for the percutaneous delivery of sulforaphane to be used for the treatment of skin cancer diseases. The physico-chemical features of the ultradeformable vesicles were evaluated. Namely, ethosomes and transfersomes had mean sizes <400 nm and a polydispersity index close to 0. The stability studies demonstrated that the most suitable ultradeformable vesicles to be used as topical carriers of sulforaphane were ethosomes made up of ethanol 40% () and phospholipon 90G 2% (). In particular, in vitro studies of percutaneous permeation through human stratum corneum and epidermis membranes showed an increase of the percutaneous permeation of sulforaphane. The antiproliferative activity of sulforaphane-loaded ethosomes was tested on SK-MEL 28 and improved anticancer activity was observed in comparison with the free drug.
萝卜硫素是一种具有多种作用的药物，其抗癌活性是该药物受到持续关注的原因。萝卜硫素对黑色素瘤和其他皮肤癌疾病表现出体外抗增殖活性。不幸的是，由于其物理化学特性决定的经皮渗透性较差，这种天然化合物不能以游离形式应用于皮肤。本研究的目的是评估乙醇脂质体和传递体作为超可变形囊泡载体用于经皮递送萝卜硫素以治疗皮肤癌疾病。评估了超可变形囊泡的物理化学特征。具体而言，乙醇脂质体和传递体的平均尺寸<400 nm，多分散指数接近0。稳定性研究表明，用作萝卜硫素局部载体的最合适的超可变形囊泡是由40%（体积分数）乙醇和2%磷脂90G组成的乙醇脂质体。特别是，通过人角质层和表皮膜的体外经皮渗透研究表明，萝卜硫素的经皮渗透率有所提高。在SK-MEL 28细胞上测试了负载萝卜硫素的乙醇脂质体的抗增殖活性，与游离药物相比，观察到抗癌活性有所提高。
