Centre R&D Pierre Fabre, Innovation et Développement Pharmacologie, Pierre Fabre Dermo-cosmétique, Toulouse, France.
Int J Cosmet Sci. 2021 Aug;43(4):391-404. doi: 10.1111/ics.12705. Epub 2021 May 25.
We investigated the dermal bioavailability and antioxidative properties of a sunscreen formulation containing two antioxidants, oxothiazolidine (OTZ) and δ-tocopheryl glucoside (DTG). OTZ reacts directly with reactive oxygen species to form taurine, while DTG is metabolized in δ-tocopherol to achieve antioxidative activities.
After topical application to a hair follicle-derived reconstructed human epidermis (RHE) model, followed by solar-simulated radiation, kinetics of bioavailability and antioxidative responses were measured over 24 h. Markers for oxidative stress were malondialdehyde (MDA), superoxide dismutase (SOD) and catalase activities.
The two antioxidants had different bioavailability profiles: OTZ was rapidly and extensively absorbed, whereas DTG was slowly absorbed and converted to δ-tocopherol. Compared to OTZ alone, the protection against effects on MDA levels and SOD and catalase activities was higher when DTG was used alone or in combination with OTZ. When used in combination, the degree of protection increased over time and remained constant over 24 h with maximal protection 2 h post-irradiation. DTG slowly penetrated into the skin and was present in the skin at all post-irradiation timepoints, thus allowing a slow but constant supply of δ-tocopherol over at least 24 h. By contrast, the oxidative protection by OTZ was immediate but short-lived due to its rapid penetration through the RHE and into the receptor fluid.
These results indicate a complementary sunlight protective action of OTZ and DTG with an immediate delivery of OTZ just after topical application of the formulation, and a prolonged skin delivery of δ-tocopherol from the slower penetration and metabolism of DTG.
研究含有两种抗氧化剂奥克噻唑啉(OTZ)和 δ-生育酚葡萄糖苷(DTG)的防晒霜配方的皮肤生物利用度和抗氧化性能。OTZ 与活性氧直接反应形成牛磺酸,而 DTG 在 δ-生育酚中代谢以实现抗氧化活性。
在毛发衍生的重建人体表皮(RHE)模型上进行局部应用,然后进行模拟阳光辐射,在 24 小时内测量生物利用度和抗氧化反应的动力学。氧化应激标志物为丙二醛(MDA)、超氧化物歧化酶(SOD)和过氧化氢酶活性。
两种抗氧化剂具有不同的生物利用度曲线:OTZ 被快速广泛吸收,而 DTG 则被缓慢吸收并转化为 δ-生育酚。与单独使用 OTZ 相比,单独使用 DTG 或与 OTZ 联合使用时,对 MDA 水平以及 SOD 和过氧化氢酶活性的保护作用更高。联合使用时,保护程度随时间增加,并在 24 小时内保持恒定,最大保护作用出现在辐射后 2 小时。DTG 缓慢渗透到皮肤中,并在所有辐射后时间点都存在于皮肤中,从而在至少 24 小时内缓慢但持续地供应 δ-生育酚。相比之下,由于 OTZ 快速穿透 RHE 并进入受体液,因此其提供的氧化保护作用是即时的但短暂的。
这些结果表明 OTZ 和 DTG 具有互补的阳光保护作用,OTZ 在配方局部应用后立即提供,而 DTG 缓慢渗透和代谢则提供了持续至少 24 小时的 δ-生育酚的皮肤输送。