Trotta Valentina, Goios Filipa, Monteiro Helena, Almeida Isabel F, Scalia Santo
Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara , Ferrara , Italy and.
Drug Dev Ind Pharm. 2014 Sep;40(9):1233-9. doi: 10.3109/03639045.2013.814062. Epub 2013 Jul 9.
Essential requirements for the efficacy of sunscreen agents are optimal UV absorption, high photostability and resistance against water removal.
Aim of this study was to investigate the effect of encapsulation in lipid microparticles (LMs) on the overall performance of the two most commonly used sunscreen agents, octyl methoxycinnamate (OMC) and butyl methoxydibenzoylmethane (BMDBM).
LMs loaded with OMC and BMDBM were prepared by melt emulsification and characterized by optical microscopy, UV filter content and release studies. The LMs incorporating OMC and BMDBM or the nonencapsulated sunscreen agents were introduced into a model cream (oil-in-water emulsion).
No significant differences were observed between the sun protection factor (SPF) of the formulations containing the free (SPF, 9.4 ± 1.9) or microencapsulated (SPF, 9.6 ± 1.3) UV filters. Irradiation of the creams with a solar simulator demonstrated that the photodecomposition of OMC and BMDBM was significantly decreased by encapsulation in LMs from 55.7 ± 5.3% to 46.1 ± 5.1% and 36.3 ± 3.9% to 20.1 ± 4.7%, respectively. However, in vitro water-resistance studies showed that entrapment in the LMs significantly enhanced the sunscreen agent removal caused by watering (the losses for OMC and BMDBM were 45.1 ± 6.3% and 49.2 ± 8.4%, respectively), as compared to the formulation with the nonencapsulated sunscreen agents (the losses for OMC and BMDBM were 26.7 ± 6.1% and 28.0 ± 6.7%, respectively).
Incorporation in LMs can have controversial effects on UV filter efficacy. In particular, the water-resistance properties of sun-care formulations containing sunscreens loaded in LMs should be verified to assure that the photoprotective activity is maintained during usage.
防晒剂发挥功效的基本要求是具有最佳的紫外线吸收能力、高光稳定性和抗脱水能力。
本研究旨在探讨脂质微粒(LMs)包封对两种最常用防晒剂桂皮酸盐(OMC)和丁基甲氧基二苯甲酰甲烷(BMDBM)整体性能的影响。
通过熔融乳化法制备了负载OMC和BMDBM的LMs,并通过光学显微镜、紫外线过滤剂含量和释放研究对其进行了表征。将含有OMC和BMDBM的LMs或未包封的防晒剂引入模型乳膏(水包油乳液)中。
含有游离(防晒系数,9.4±1.9)或微包封(防晒系数,9.6±1.3)紫外线过滤剂的配方之间的防晒系数(SPF)未观察到显著差异。用太阳模拟器照射乳膏表明,通过包封在LMs中,OMC和BMDBM的光分解分别从55.7±5.3%显著降低到46.1±5.1%和36.3±3.9%降低到20.1±4.7%。然而,体外耐水研究表明,与含有未包封防晒剂的配方(OMC和BMDBM的损失分别为26.7±6.1%和28.0±6.7%)相比,包封在LMs中显著增强了浇水引起的防晒剂去除(OMC和BMDBM的损失分别为45.1±6.3%和49.2±8.4%)。
包封在LMs中对紫外线过滤剂的功效可能有争议性影响。特别是,应验证含有LMs负载防晒剂的防晒配方的耐水性能,以确保在使用过程中保持光保护活性。