title: Photostability and efficacy studies of topical formulations containing UV-filters combination and vitamins A, C and E.
abstract: It is already known that the photostability of a sunscreen is important for its performance on human skin. On the other hand, there are many formulations besides sunscreens containing combinations of UV-filters and daily use active substances with other claims like hydration and anti-aging effects. Vitamins A, C and E are frequently added in these kinds of products and it is not known if the UV-filters have some influence on the hydration and anti-aging effects of these vitamins on the skin as well as on their stability mainly when photounstable UV-filters like avobenzone and octyl methoxycinnamate are present in the formulation. Thus, the aim of this study was to evaluate the influence of two different UV-filters combinations, a photostable and a photounstable one, on the photostability as well as on the efficacy of a formulation containing vitamin A, C and E derivatives. The formulations that were investigated contained or not (vehicle: formulation 1) a combination of 0.6 % (w/w) vitamin A palmitate (1,700,000 UI/g), 2 % (w/w) vitamin E acetate and 2% (w/w) ascorbyl tetraisopalmitate (formulation 2) supplemented with a photounstable UV filter combination octyl methoxycinnamate (OMC), avobenzone (AVB) and 4-methylbenzilidene camphor (MBC) (formulation 3) or with a photostable UV filter combination OMC, benzophenone-3 (BP-3) and octocrylene (OC) (formulation 4). In the photostability studies, all formulations were spread onto a glass plate and exposed to UVA/UVB irradiation. The filter components and vitamins were quantified by HPLC analysis with detection at 325 and 235 nm and by spectrophotometry. To simulate the effects of these formulations daily use, all of them (formulations 1-4) were applied on the dorsum of hairless mice, which were submitted to a controlled light-dark cycle (and were not irradiated), once a day for 5 days. Transepidermal water loss (TEWL), water content of the stratum corneum and viscoelastic properties of the skin were analyzed by using different non-invasive Biophysics Techniques in order to evaluate hydration and anti-aging effects of these formulations as well as erythema to assess skin irritation. Histopathology, viable epidermal thickness as well as the number of epidermal cell layers were also evaluated. It was observed that both UV filters combinations (photounstable one containing OMC, AVB and MBC and photostable one containing OMC, BP-3 and OC) enhanced vitamin A photostability and F4 was more photostable than F3, in terms of vitamin A. In vivo efficacy studies showed that F2, F3 and F4 enhanced the viable epidermal thickness, the number of epidermal cell layers, TEWL and Uv/Ue parameter, when compared to the vehicle, which can suggest that they enhanced viable epidermis hydration and acted in cell renewal. However formulation 2 (containing only vitamins), which was the most photounstable formulation, provoked an irritation on hairless mouse skin, and consequently it cannot be considered as safe as the other formulations. It can be concluded that both UV filters combinations did not influence the hydration and anti-aging effects of the formulations containing the vitamins under study and reduced the skin irritation observed when the vitamins were present in the formulation. In addition, the photostable UV-filters combination had the highest recovery of vitamin A in the photostability studies. Finally, it could be suggested that the presence of UV-filters can be considered interesting for the reduction of skin irritation and the most suitable formulation was the one containing the combinations of vitamins A, C and E with photostable UV-filters.
authors.affiliation: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Av. do Café s/n, Bairro Monte Alegre, Ribeirão Preto, SP 14 040-903, Brazil.
authors.forename: L R
authors.initials: LR
authors.lastname: Gaspar
authors.forename: P M B G Maia
authors.initials: PM
authors.lastname: Campos
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D001205:Ascorbic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000528:radiation effects*; D004224:Diterpenes; D004355:Drug Stability; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D000084562:Retinyl Esters; D012867:Skin / Q000033:anatomy & histology / Q000737:chemistry / Q000187:drug effects; D013473:Sunscreening Agents / Q000008:administration & dosage / Q000528:radiation effects*; D024505:Tocopherols; D014466:Ultraviolet Rays; D014801:Vitamin A / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000528:radiation effects; D014815:Vitamins / Q000008:administration & dosage / Q000528:radiation effects*; D014867:Water / Q000032:analysis; D024502:alpha-Tocopherol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000528:radiation effects
chemical_list: D004224:Diterpenes; D000084562:Retinyl Esters; D013473:Sunscreening Agents; D014815:Vitamins; D014867:Water; D014801:Vitamin A; C014794:retinol palmitate; D024502:alpha-Tocopherol; D001205:Ascorbic Acid; D024505:Tocopherols