Suh Hee-Won, Lewis Julia, Fong Linda, Ramseier Julie Ying, Carlson Kacie, Peng Zheng-Hong, Yin Emily Sara, Saltzman W Mark, Girardi Michael
Dept. of Biomedical Engineering, Yale School of Engineering & Applied Science 55 Prospect Street, New Haven CT 06520.
Dept. of Dermatology, Yale School of Medicine 333 Cedar Street, New Haven CT 06520.
Bioeng Transl Med. 2018 Jul 6;4(1):129-140. doi: 10.1002/btm2.10092. eCollection 2019 Jan.
Conventional emulsion-based sunscreen formulations are limited by postapplication epicutaneous penetration that increases the risk of allergic dermatitis, cellular damage, and filter photodegradation upon ultraviolet radiation (UVR) exposure. Encapsulation of the UVB filter padimate O within bioadhesive biodegradable nanoparticles (BNPs) composed of poly(d,l-lactic acid)-hyperbranched polyglycerol was previously shown to enhance UVR protection while preventing skin absorption. Herein, we assess the capacity of BNP co-incorporation of avobenzone and octocrylene to provide broad-spectrum UVR protection. The ratio of UV filters within nanoparticles (NPs) was optimized for filter-filter stabilization upon UV irradiation and maximum drug loading. In vitro water-resistance test showed significant particle retention at 85% over 3 hr. In a pilot clinical study, protection against UVR-induced erythema of BNPs was found to be comparable to the FDA standard P2. Thus, sunscreen formulations utilizing BNP incorporation of a combination of organic filters may offer key safety and performance advantages.
传统的乳液型防晒配方存在局限性，涂抹后经皮渗透会增加过敏性皮炎、细胞损伤以及紫外线（UVR）照射下滤光剂光降解的风险。先前研究表明，将UVB滤光剂帕地马酯O封装在由聚（d，l-乳酸）-超支化聚甘油组成的生物粘附性可生物降解纳米颗粒（BNP）中，可增强UVR防护效果，同时防止皮肤吸收。在此，我们评估BNP共载阿伏苯宗和二乙氨羟苯甲酰基苯甲酸己酯以提供广谱UVR防护的能力。对纳米颗粒（NP）中紫外线滤光剂的比例进行了优化，以实现紫外线照射下滤光剂间的稳定以及最大载药量。体外耐水试验表明，3小时内颗粒保留率达85%，具有显著的耐水性。在一项初步临床研究中，发现BNP对UVR诱导红斑的防护效果与美国食品药品监督管理局（FDA）标准P2相当。因此，采用BNP包载有机滤光剂组合的防晒配方可能具有关键的安全性和性能优势。
