Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka 576 104, India.
Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka 576 104, India.
Colloids Surf B Biointerfaces. 2020 Sep;193:111122. doi: 10.1016/j.colsurfb.2020.111122. Epub 2020 May 12.
Long term exposure of skin to UV rays produces detrimental effects such as premature skin-ageing and skin cancer. Although, zinc oxide (ZnO) and titanium dioxide (TiO) are good sunscreen agents, they do not provide highly efficient UV radiation protection and antioxidant and anti-aging effects. The present study was aimed at developing and characterizing ethosomes loaded with naringin and then to incorporate them into sunscreen creams containing nano-ZnO and -TiO to achieve adequate skin penetration and skin retention so as to scavenge the free radicals by virtue of naringin's antioxidant property. Ethosomes were prepared and optimized with respect to concentrations of ethanol and cholesterol, time of sonication, drug and lipid ratio and amount of drug. The ethosomes were evaluated for size, zeta potential (ZP), polydispersity index (PDI), encapsulation efficiency and surface morphology. Ethosomal sunscreen creams were evaluated for physicochemical tests, spreadability, antioxidant, cytotoxicity and skin permeation studies. Optimized ethosomal formulation exhibited average vesicle size, PDI, ZP and drug encapsulation efficiency of 142.5 ± 5.6 nm, 0.199 ± 0.007, -72.5 ± 2.9 mV and 33.79 ± 1.35%, respectively. Naringin ethosomes showed enhanced retention in the skin (403.44 ± 15.33 μg/cm) compared to naringin suspension (202.81 ± 9.45 μg/cm). The optimized sunscreen cream exhibited SPF of 21.21 ± 0.62 with negligible permeation of naringin across the skin. Ethosomes showed pronounced skin permeation for naringin and optimized cream containing naringin ethosomes along with nano- ZnO and TiO2 showed good skin retention for naringin.
皮肤长期暴露在紫外线下会产生有害影响，如皮肤早衰和皮肤癌。虽然氧化锌（ZnO）和二氧化钛（TiO）是很好的防晒剂，但它们不能提供高效的紫外线辐射防护和抗氧化及抗衰老作用。本研究旨在开发并表征柚皮苷的醇质体，然后将其纳入含有纳米 ZnO 和 TiO 的防晒霜膏中，以实现足够的皮肤渗透和皮肤滞留，从而通过柚皮苷的抗氧化特性清除自由基。从乙醇和胆固醇的浓度、超声时间、药物和脂质的比例以及药物的量等方面对醇质体进行了制备和优化。对醇质体进行了粒径、Zeta 电位（ZP）、多分散指数（PDI）、包封效率和表面形态的评价。对含纳米 ZnO 和 TiO 的柚皮苷醇质体防晒霜膏进行了物理化学性质测试、铺展性、抗氧化、细胞毒性和皮肤渗透研究。优化的醇质体配方的平均囊泡粒径、PDI、ZP 和药物包封效率分别为 142.5±5.6nm、0.199±0.007、-72.5±2.9mV 和 33.79±1.35%。与柚皮苷混悬液（202.81±9.45μg/cm）相比，柚皮苷醇质体显示出更高的皮肤滞留量（403.44±15.33μg/cm）。优化的防晒霜膏显示出 21.21±0.62 的 SPF，柚皮苷几乎没有透过皮肤。醇质体对柚皮苷表现出明显的皮肤渗透作用，含有柚皮苷醇质体和纳米 ZnO、TiO 的优化乳膏对柚皮苷具有良好的皮肤滞留作用。
