Huang Pao Hsien, Hu Stephen Chu Sung, Yen Feng Lin, Tseng Chih Hua
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 807, Taiwan.
Department of Dermatology, College of Medicine, Kaohsiung Medical University, Kaohsiung City 807, Taiwan.
Pharmaceutics. 2019 Aug 8;11(8):399. doi: 10.3390/pharmaceutics11080399.
As is known, many antioxidants from plant extracts have been used as additives in skincare products to prevent skin damage following overexposure to environmental pollutants. 7,3',4'-trihydroxyisoflavone (734THIF), an isoflavone compound, possesses various biological activities, including antioxidant, antityrosinase, photodamage protection, and anticancer effects. Unfortunately, 734THIF has poor water solubility, which limits its skin penetration and absorption, and subsequently influences its biological activity. The aim of the present study was to investigate the mechanisms for the improvement in water solubility and skin penetration of 2-hydroxypropyl-β-cyclodextrin (HPBCD) inclusion complex with 734THIF (5-7HP). We also determined its photostability, antipollutant activity in HaCaT keratinocytes, and moisturizing effect in human subjects. Our results showed that 734THIF was embedded into the lipophilic inner cavity of HPBCD and its water solubility and skin penetration were thereby improved through amorphous transformation, surface area enhancement, and hydrogen bonding formation between 734THIF and HPBCD. In addition, 5-7HP inhibited PM-induced ROS generation and then downregulated ROS-mediated COX-2 and MMP9 production and AQP-3 consumption by inhibiting the phosphorylation of MAPKs. Consequently, we suggest that 5-7HP is a safe and photostable topical ingredient to enhance the skin penetration of 734THIF and skin hydration, and therefore 5-7HP may be used as an antipollutant additive in skin care products.
众所周知，许多植物提取物中的抗氧化剂已被用作护肤品中的添加剂，以防止过度暴露于环境污染物后对皮肤造成损伤。7,3',4'-三羟基异黄酮（734THIF）是一种异黄酮化合物，具有多种生物活性，包括抗氧化、抗酪氨酸酶、光损伤保护和抗癌作用。不幸的是，734THIF的水溶性较差，这限制了其皮肤渗透和吸收，进而影响其生物活性。本研究的目的是探讨2-羟丙基-β-环糊精（HPBCD）与734THIF的包合物（5-7HP）改善水溶性和皮肤渗透性的机制。我们还测定了其光稳定性、对HaCaT角质形成细胞的抗污染活性以及对人体受试者的保湿效果。我们的结果表明，734THIF嵌入到HPBCD的亲脂性内腔中，通过无定形转变、表面积增加以及734THIF与HPBCD之间形成氢键，从而改善了其水溶性和皮肤渗透性。此外，5-7HP通过抑制丝裂原活化蛋白激酶（MAPKs）的磷酸化，抑制了颗粒物（PM）诱导的活性氧（ROS）生成，进而下调了ROS介导的环氧化酶-2（COX-2）和基质金属蛋白酶9（MMP9）的产生以及水通道蛋白3（AQP-3）的消耗。因此，我们认为5-7HP是一种安全且光稳定的局部用成分，可增强734THIF的皮肤渗透性和皮肤水合作用，因此5-7HP可作为护肤品中的抗污染添加剂。
