【摘要】 合成了下缘十二烷基修饰的磺化杯[8]芳烃(SC8A-12C),用于提高维生素A(Va)在水相中的溶解性和稳定性,并促进Va的经皮渗透.脂溶性Va在水中几乎不溶, SC8A-12C能将Va的溶解度提高至1.1 mg/mL,将Va在水溶液中的半衰期从5 h延长到35 h.体外透皮测试表明, SC8A-12C提高Va的透皮量达16.9倍. SC8A-12C还能增溶苯乙基间苯二酚、水杨酸、槲皮素及壬二酸等多种护肤成分,并将水杨酸的透皮量提高3.8倍.SC8A-12C从增溶、增稳和透皮性3个方面提升了Va的功效,有望开发出无油配方的纯水剂Va类护肤品.鉴于SC8A-12C对多种护肤成分的增溶作用,有望助力于多功效护肤品的发展.更多还原

【Abstract】 The sulfonated calix[8]arene modified with dodecyl at the lower-rim(SC8A-12C) was synthesized to improve the solubility and stability of vitamin A(Va) in aqueous solution, and promote the percutaneous permeability of Va. Lipophilic Va is almost insoluble in water, SC8A-12C could improve solubility of Va to 1.1 mg/mL and prolong the half-life of Va in aqueous solution from 5 h to 35 h. In vitro transdermal test showed that SC8A-12C increased the transdermal amount of Va by 16.9 times. SC8A-12C also increased the solubility of various skin-care ingredients, such as phenoethylresorcinol, salicylic acid, quercetin and azelaic acid, and increased the transdermal amount of salicylic acid by 3.8 times. SC8A-12C improved the efficacy of Va through improving solubility, stability and skin permeability, and was expected to develop oil-free skin-care products of Va. In view of the SC8A-12C improving solubility of a variety of skin-care ingredients, it is expected to contribute to the development of multi-functional skin-care products.更多还原