Benevenuto Carolina Gomes, Guerra Lucas Offenbecker, Gaspar Lorena Rigo
Faculty of Pharmaceutical Sciences of Ribeirao Preto, University of Sao Paulo, Sao Paulo, Brazil.
Allergisa - Investiga Research Institute, Barao Geraldo, Campinas, Sao Paulo, Brazil.
Eur J Pharm Sci. 2015 Feb 20;68:127-36. doi: 10.1016/j.ejps.2014.12.007. Epub 2014 Dec 19.
This study aimed to assess the phototoxic potential of combined UV-filters and retinyl palmitate (RP) in the presence or not of bemotrizinol (BMTZ), employing photostability and in vitro and in vivo phototoxicity assays. The formulations tested contained octocrylene (OCT), octyl methoxycinnamate (OMC), benzophenone-3 (BZP-3) and RP (photostable) or octocrylene (OCT), octyl methoxycinnamate (OMC), avobenzone (AVO) and RP (less photostable). Both formulations were supplemented with bemotrizinol. Photostability was evaluated by exposing, or not, formulations spread on a glass plate to UVA/UVB irradiation. The resulting products were quantified by HPLC analysis. In vitro phototoxicity of UV-filters and combinations were evaluated using 3T3 viable monolayer fibroblast cultures submitted, or not, to irradiation according to OECD TG 432. In vivo photoallergy and photoxicity were assessed by clinical studies (photopatch test). Photostability assays showed that UV-filter bemotrizinol was a better photostabilizer for RP/benzophenone-3 than for RP/avobenzone. The in vitro phototoxicity of the combination RP/avobenzone was reduced by bemotrizinol. Clinical studies did not indicate phototoxic or photoallergenic potentials in all formulations tested. It is concluded that the 3T3 NRU phototoxicity test may be considered a supplementary assay in formulation developments, since it can detect chemically unstable and potentially phototoxic combinations. However, extrapolation of in vitro positive results to human photopatch tests may be performed only to a limited extent.
本研究旨在通过光稳定性以及体外和体内光毒性试验,评估联合使用紫外线过滤剂和视黄醇棕榈酸酯(RP)在有或没有倍他米松(BMTZ)存在的情况下的光毒性潜力。所测试的配方含有二乙氨羟苯甲酰基苯甲酸己酯(OCT)、甲氧基肉桂酸辛酯(OMC)、二苯甲酮-3(BZP-3)和RP(光稳定型)或二乙氨羟苯甲酰基苯甲酸己酯(OCT)、甲氧基肉桂酸辛酯(OMC)、阿伏苯宗(AVO)和RP(光稳定性较差型)。两种配方均添加了倍他米松。通过将涂在玻璃板上的配方暴露或不暴露于UVA/UVB照射来评估光稳定性。通过HPLC分析对所得产物进行定量。根据经合组织TG 432,使用3T3活单层成纤维细胞培养物评估紫外线过滤剂及其组合的体外光毒性,该培养物接受或不接受照射。通过临床研究(光斑贴试验)评估体内光过敏和光毒性。光稳定性试验表明,紫外线过滤剂倍他米松对RP/二苯甲酮-3的光稳定作用比对RP/阿伏苯宗的光稳定作用更好。倍他米松降低了RP/阿伏苯宗组合的体外光毒性。临床研究未表明所有测试配方具有光毒性或光过敏潜力。结论是,3T3 NRU光毒性试验可被视为配方开发中的补充试验,因为它可以检测化学不稳定且可能具有光毒性的组合。然而,体外阳性结果外推至人体光斑贴试验只能在有限程度上进行。