Montenegro Lucia, Turnaturi Rita, Parenti Carmela, Pasquinucci Lorella
Department of Drug Sciences, Pharmaceutical Technology Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
Rita Turnaturi Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
Pharmaceutics. 2018 Feb 27;10(1):27. doi: 10.3390/pharmaceutics10010027.
The evaluation of UV-filter in vitro percutaneous absorption allows the estimation of the systemic exposure dose (SED) and the margin of safety (MoS) of sunscreen products. As both the vehicle and pattern of application may affect sunscreen safety and efficacy, we evaluated in vitro release and skin permeation of two widely used UV-filters, octylmethoxycinnamate (OMC) and butylmethoxydibenzoylmethane (BMBM) from topical formulations with different features (oil in water (O/W) emulsions with different viscosity, water in oil (W/O) emulsion, oils with different lipophilicity). To mimic in-use conditions, we carried out experiments repeating sunscreen application on the skin surface for three consecutive days. BMBM release from all these vehicles was very low, thus leading to poor skin permeation. The vehicle composition significantly affected OMC release and skin permeation, and slight increases of OMC permeation were observed after repeated applications. From skin permeation data, SED and MoS values of BMBM and OMC were calculated for all the investigated formulations after a single application and repeated applications. While MoS values of BMBM were always well beyond the accepted safety limit, the safety of sunscreen formulations containing OMC may depend on the vehicle composition and the application pattern.
对紫外线过滤剂体外经皮吸收的评估有助于估算防晒产品的全身暴露剂量（SED）和安全边际（MoS）。由于载体和涂抹方式都可能影响防晒产品的安全性和有效性，我们评估了两种广泛使用的紫外线过滤剂，即桂皮酸盐（OMC）和丁基甲氧基二苯甲酰甲烷（BMBM），从具有不同特性的局部制剂（不同粘度的水包油（O/W）乳液、油包水（W/O）乳液、不同亲脂性的油）中的体外释放和皮肤渗透情况。为模拟实际使用条件，我们进行了连续三天在皮肤表面重复涂抹防晒霜的实验。所有这些载体中BMBM的释放都非常低，因此皮肤渗透较差。载体组成显著影响OMC的释放和皮肤渗透，并且在重复涂抹后观察到OMC渗透略有增加。根据皮肤渗透数据，计算了单次涂抹和重复涂抹后所有研究制剂中BMBM和OMC的SED和MoS值。虽然BMBM的MoS值始终远远超过公认的安全限值，但含有OMC的防晒制剂的安全性可能取决于载体组成和涂抹方式。
