title: In vitro photosafety and efficacy screening of apigenin, chrysin and beta-carotene for UVA and VIS protection.
abstract: Currently most of sunscreens provide effective protection in the full UV range but lack VIS protection. The addition of effective antioxidants to sunscreens might afford suitable UV-VIS protection. Apigenin (API), chrysin (CRI) and beta-carotene (BTC) have shown potential for UV-VIS protection. This paper reports a photosafety and efficacy screening of such antioxidants through evaluation of the photostability, photoreactivity and phototoxicity as well as UVA/UVB ratio and critical wavelength. The assessment of the photostability, photoreactivity and phototoxicity of API, CRI and BTC, isolated and combined (CMB) was performed by HPLC, ROS assay and 3T3 NRU phototoxicity test, respectively. The phototoxicity test was also performed for CMB plus bemotrizinol (BMZ). The in vitro evaluation of the UVA protection was assessed by the determination of the UVA/UVB ratio and the critical wavelength. The antioxidants API, CRI, BTC and CMB were stable under UVA/VIS and VIS light. However weak photoreactivity after UVA/VIS irradiation was observed for API, CRI and CMB in the ROS assay. In the 3T3 NRU phototoxicity test, phototoxic potential was observed for CRI, BTC, CMB and CMB+BMZ after UVA/VIS exposure, and for BTC and CMB after VIS exposure. BMZ reduced the phototoxic potential of CMB in the VIS range. In the in vitro evaluation of UVA protection API, CRI, BTC, CMB and CMB+BMZ presented ultra UVA protection (UVA/UVB ratio>0.9) and exhibited critical wavelength close to or above 370nm. In conclusion, the use of API, CRI, BTC and their CMB aiming skin photoprotection could be considered safer in the VIS range. Furthermore, API presented the best performance in the photosafety screening among the studied antioxidants, since it was photostable and non-phototoxic in UVA/VIS and photostable, non-photoreactive and non-phototoxic in VIS range.
authors.affiliation: Departamento de Ciências Farmacêuticas, Universidade de São Paulo, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Ribeirão Preto, SP, Brazil.
authors.forename: Juliana Vescovi
authors.initials: JV
authors.lastname: Freitas
authors.affiliation: Departamento de Ciências Farmacêuticas, Universidade de São Paulo, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Ribeirão Preto, SP, Brazil. Electronic address: lorena@fcfrp.usp.br.
authors.forename: Lorena Rigo
authors.initials: LR
authors.lastname: Gaspar
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000009:adverse effects / Q000494:pharmacology; D047310:Apigenin / Q000009:adverse effects / Q000494:pharmacology*; D002460:Cell Line; D017484:Dermatitis, Phototoxic / Q000209:etiology; D004355:Drug Stability; D005347:Fibroblasts / Q000187:drug effects; D005419:Flavonoids / Q000009:adverse effects / Q000494:pharmacology*; D008027:Light / Q000009:adverse effects; D051379:Mice; D008807:Mice, Inbred BALB C; D009499:Neutral Red / Q000009:adverse effects / Q000494:pharmacology; D012867:Skin / Q000528:radiation effects; D013473:Sunscreening Agents / Q000009:adverse effects / Q000494:pharmacology*; D014466:Ultraviolet Rays / Q000009:adverse effects; D019207:beta Carotene / Q000009:adverse effects / Q000494:pharmacology*
chemical_list: D000975:Antioxidants; D005419:Flavonoids; D013473:Sunscreening Agents; D019207:beta Carotene; D009499:Neutral Red; C043561:chrysin; D047310:Apigenin
keywords: Antioxidants; Photoprotection; Photoreactivity; Photostability; Phototoxicity