Limsuwan Tunyaluk, Boonme Prapaporn, Khongkow Pasarat, Amnuaikit Thanaporn
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Songkhla 90112, Thailand.
Nanotec-PSU Center of Excellence on Drug Delivery System, Songkhla, Thailand.
Biomed Res Int. 2017;2017:8310979. doi: 10.1155/2017/8310979. Epub 2017 Jul 19.
Ethosome formulations containing phenylethyl resorcinol (PR) were developed. The formulation was produced from 0.5% w/v PR, 0.5% w/v cholesterol from lanolin, 3% w/v L--phosphatidylcholine from soybean, 30% v/v absolute ethanol, and water up to 100% v/v. It was characterized by a vesicular size of 389 nm, low polydispersity index of 0.266, zeta potential of -34.19 ± 0.44 mV, high PR entrapment efficiency of 71%, and good stability on storage at 4 and 30°C at 75% RH for 4 months. In vitro studies using pig skin revealed that permeation coefficient of PR from ethosomes was significantly higher than that from liposomes. In vitro retention profiles showed that PR accumulation in pig skin following application of ethosome formulations was 7.4-, 3.3-, and 1.8-fold higher than that achieved using liposomes, 20% propylene glycol solution, and 30% hydroethanolic solution, respectively. An inhibition value of around 80% was measured for antityrosinase activity of PR in pig skin. Consistently, ethosomes exhibited higher tyrosinase inhibition activity and melanin content reduction when compared to other formulations in B16 melanoma cells. Ethosomes did not cause acute dermal irritation in albino rabbits. These findings demonstrate that ethosomes are capable of delivering PR into the skin efficiently and hold promise for topical application of skin lightening products.
研发了含有苯乙基间苯二酚（PR）的醇质体配方。该配方由0.5%（w/v）的PR、0.5%（w/v）来自羊毛脂的胆固醇、3%（w/v）来自大豆的L-磷脂酰胆碱、30%（v/v）无水乙醇以及加至100%（v/v）的水制成。其特征在于囊泡大小为389nm，多分散指数低至0.266，ζ电位为-34.19±0.44mV，PR包封率高达71%，并且在4℃和30℃、75%相对湿度下储存4个月具有良好的稳定性。使用猪皮进行的体外研究表明，PR从醇质体的渗透系数显著高于从脂质体的渗透系数。体外滞留曲线显示，施用醇质体配方后PR在猪皮中的蓄积分别比使用脂质体、20%丙二醇溶液和30%乙醇水溶液时高7.4倍、3.3倍和1.8倍。在猪皮中测得PR的抗酪氨酸酶活性抑制值约为80%。同样，与B16黑色素瘤细胞中的其他配方相比，醇质体表现出更高的酪氨酸酶抑制活性和黑色素含量降低效果。醇质体对白化兔未引起急性皮肤刺激。这些发现表明，醇质体能够有效地将PR递送至皮肤，有望用于美白皮肤产品的局部应用。
