Fernanda Daud Sarruf

Broad spectrum bioactive sunscreens

The development of sunscreens containing reduced concentration of chemical UV filters, even though, possessing broad spectrum effectiveness with the use of natural raw materials that improve and infer UV absorption is of great interest. Due to the structural similarities between polyphenolic compounds and organic UV filters, they might exert photoprotection activity. The objective of the present research work was to develop bioactive sunscreen delivery systems containing rutin, Passiflora incarnata L. and Plantago lanceolata extracts associated or not with organic and inorganic UV filters. UV transmission of the sunscreen delivery system films was performed by using diffuse transmittance measurements coupling to an integrating sphere. In vitro photoprotection efficacy was evaluated according to the following parameters: estimated sun protection factor (SPF); Boots Star Rating category; UVA/UVB ratio; and critical wavelength (lambda(c)). Sunscreen delivery systems obtained SPF values ranging from 0.972+/-0.004 to 28.064+/-2.429 and bioactive compounds interacted with the UV filters positive and negatively. This behavior may be attributed to: the composition of the delivery system; the presence of inorganic UV filter and quantitative composition of the organic UV filters; and the phytochemical composition of the P. incarnata L. and P. lanceolata extracts. Among all associations of bioactive compounds and UV filters, we found that the broad spectrum sunscreen was accomplished when 1.68% (w/w) P. incarnata L. dry extract was in the presence of 7.0% (w/w) ethylhexyl methoxycinnamate, 2.0% (w/w) benzophenone-3 and 2.0% (w/w) TiO(2). It was demonstrated that this association generated estimated SPF of 20.072+/-0.906 and it has improved the protective defense against UVA radiation accompanying augmentation of the UVA/UVB ratio from 0.49 to 0.52 and lambda(c) from 364 to 368.6nm.

Estabilidade e estudo de penetração cutânea in vitro da rutina veiculada em uma emulsão cosmética através de um modelo de biomembrana alternativo

Rutin is employed as antioxidant and to prevent the capillary fragility and, when incorporated in cosmetic emulsions, it must target the action site. In vitro cutaneous penetration studies through human skin is the ideal situation, however, there are difficulties to obtain and to maintain this tissue viability. Among the membrane models, shed snake skin presents itself as pure stratum corneum, providing barrier function similar to human and it is obtained without the animal sacrifice. The objectives of this research were the development and stability evaluation of a cosmetic emulsion containing rutin and propylene glycol (penetration enhancer) and the evaluation of rutin in vitro cutaneous penetration and retention from the emulsion, employing an alternative model biomembrane. Emulsion was developed with rutin and propylene glycol, both at 5.0% w/w. Active substance presented on the formulation was quantified by a validated spectrophotometric method at 361.0 nm. Rutin cutaneous penetration and retention was performed in vertical diffusion cells with shed snake skin of Crotalus durissus, as alternative model biomembrane, and distilled water and ethanol 99.5% (1:1), as receptor fluid. The experiment was conducted for six hours, at 37.0 ± 0.5 oC with constant stirring of 300 rpm. Spectrophotometry at 410.0 nm, previously validated, determined the active substance after cutaneous penetration/retention. Emulsion did not promote rutin cutaneous penetration through C. durissus skin, retaining 0.931 ± 0.0391 mg rutin/mg shed snake skin. The referred formulation was chemically stable for 30 days after stored at 25.0 ± 2.0 oC, 5.0 ± 0.5 oC and 45.0 ± 0.5 oC. In conclusion, it has not been verified the active cutaneous penetration through the model biomembrane, but only its retention on the Crotalus durissus stratum corneum, condition considered stable for 30 days.

Influence of Urea, Isopropanol, and Propylene Glycol on Rutin In Vitro Release from Cosmetic Semisolid Systems Estimated by Factorial Design

Rutin, one of the major flavonoids found in an assortment of plants, was reported to act as a sun protection factor booster with high anti-UVA defense, antioxidant, antiaging, and anticellulite, by improvement of the cutaneous microcirculation. This research work aimed at evaluating the rutin in vitro release from semisolid systems, in vertical diffusion cells, containing urea, isopropanol and propylene glycol, associated or not, according to the factorial design with two levels with center point. Urea (alone and in association with isopropanol and propylene glycol) and isopropanol (alone and in association with propylene glycol) influenced significant and negatively rutin liberation in diverse parameters: flux (μg/cm2.h); apparent permeability coefficient (cm/h); rutin amount released (μg/cm2); and liberation enhancement factor. In accordance with the results, the presence of propylene glycol 5.0% (wt/wt) presented statistically favorable to promote rutin release from this semisolid system with flux = 105.12 ± 8.59 μg/cm2.h; apparent permeability coefficient = 7.01 ± 0.572 cm/h; rutin amount released = 648.80 ± 53.01 μg/cm2; and liberation enhancement factor = 1.21 ± 0.07.

Prospective ultramorphological characterization of human hair by optical coherence tomography.

Background/purpose: The continuous advancement in cosmetic science has led to an increasing demand for the development of non‐invasive, reliable scientific techniques directed toward claim substantiation, which is of utmost relevance, to obtain data regarding the efficacy and safety of cosmetic products.

Safety and efficacy evaluation of gelatin-based nanoparticles associated with UV filters.

The safety and efficacy assessment of nanomaterials is a major concern of industry and academia. These materials, due to their nanoscale size, can have chemical, physical, and biological properties that differ from those of their larger counterparts. The encapsulation of natural ingredients can provide marked improvements in sun protection efficacy. This strategy promotes solubility enhancement of flavonoids and yields an improved active ingredient with innovative physical, physicochemical and functional characteristics. Rutin, a flavonoid, has chemical and functional stability in topical vehicles exerting a synergistic effect in association with ultraviolet (UV) filters. However, the solubility of rutin is a limiting factor. Additionally, this bioactive compound does not have tendency to permeate across the stratum corneum. As an alternative to common synthetic based sunscreens, rutin-entrapped gelatin nanoparticles were designed. The present study investigated the pre-clinical safety of gelatin nanoparticles (GNPs) using an in vitro method and also assessed the clinical safety and efficacy of the association of GNPs with three commonly used chemical UV filters (ethylhexyl dimethyl PABA, ethylhexyl methoxycinnamate and methoxydibenzoylmethane). The non-irritant and adequate safety profile under sun-exposed skin conditions of the nanomaterials and the emulsions qualified the products for clinical efficacy assays. The in vivo results indicated that the GNPs increased the antioxidant protection of the emulsions developed. However, the presence of rutin in the nanosized material did not enhance performance on the SPF test. In conclusion, these findings characterized the nanomaterials as an innovative platform for multifunctional bioactive sunscreens.

Influence of particle size on appearance and in vitro efficacy of sunscreens

A nanotecnologia se aplica a diversos setores da ciencia. Na area de cosmeticos, os investimentos tem reforcado a ideia de que nanoprodutos oferecem inumeros beneficios para os consumidores. A exposicao excessiva a luz solar pode causar efeitos indesejaveis, logo, a adicao de filtros UV em produtos cosmeticos e frequentemente usada como prevencao. O p-metoxicinamato de octila e a benzofenona-3 sao filtros UV amplamente utilizados em formulacoes de proteccao solar, que absorvem radiacoes UVB e UVA, respectivamente. Neste estudo, desenvolveram-se formulacoes de protetores solares na forma de nano e macroemulsao, mas compostos pelas mesmas materias-primas. A nanoemulsao foi obtida pelo metodo da temperatura de inversao de fases (PIT). As propriedades fisicas e funcionais foram avaliadas por analise visual, distribuicao de tamanho de particulas e por espectrofotometria de reflectância difusa. A nanoemulsao obtida apresentou brilho azulado, menor consistencia aparente quando comparada `a macroemulsao, estabilidade superior a 48 horas (22,0 ± 2,0 ° C) e distribuicao de tamanhos de particula bimodal, com media (media) de tamanhos ao redor de 10 nm (61%) e 4,5 µm (39%) . A macroemulsao apresentou aspecto leitoso, maior consistencia aaprente do que nanoemulsao, instabilidade apos 48 horas (22,0 ± 2,0 oC) e distribuicao de tamanhos de particula bimodal, com media (media) de tamanhos ao redor de 202 nm (9%) e 10,4 µm (91%). O perfil de eficacia das formulacoes fotoprotetoras permaneceu aparentemente similar, com base em resultados obtidos por ensaios de FPS in vitro, relacao UVA/UVB e comprimento de onda critico.

Comparative study of the stability of free and modified papain incorporated in topical formulations

A papaina e uma enzima utilizada em formulacoes topicas como agente proteolitico debridante no tratamento de lesoes abertas de grande extensao e queimaduras. E, tambem, empregada na pele integra como agente promotor da permeacao cutânea de principios ativos, peeling quimico e como agente depilatorio progressivo. A estabilidade de formulacoes contendo enzimas nao e facilmente alcancada. No presente trabalho realizou-se a modificacao da enzima com polietilenoglicol, visando maior estabilidade das formulacoes. A realizacao do Teste Estabilidade Normal comparativo entre as formulacoes contendo as formas da enzima nao modificada e modificada demonstrou que a ultima apresentou um perfil de estabilidade diferenciado, nas diferentes condicoes (5,0 ± 1,0 °C; 22,0 ± 2,0 °C; 40,0 ± 2,0 °C). A condicao de 5,0 ± 1,0 °C foi a mais adequada para a formulacao contendo papaina nao modificada enquanto a 22,0 ± 2,0 °C foi indicada para aquela contendo a forma modificada. Estes resultados confirmaram o aumento da estabilidade da papaina modificada comparada com a livre e seu potencial de aplicacao em formulacoes de uso topico.

Ferulic acid photoprotective properties in association with UV filters: multifunctional sunscreen with improved SPF and UVA-PF

Ultraviolet (UV) radiation stimulates several injurious biological effects on cutaneous tissue, causing, for instance, photocarcinogenesis. Sunscreens are topical products designed to protect the skin against these harmful effects and their use must be encouraged. The addition of antioxidants, as ferulic acid (FA), a phenolic compound from the class of the hydroxycinnamic acids, in sunscreens could improve their sun protection factor (SPF) and prevent inflammatory reactions. Here, the clinical safety and efficacy of an association of ethylhexyl triazone and bis-ethylhexyloxyphenol methoxyphenyl triazine (UV filters) with ferulic acid were assessed. Samples had good skin biocompatibility and presented satisfactory safety profile, even in a sun-exposed condition. A synergic effect between the natural polyphenol and the UV filters was evidenced, as well as, FA increased in vivo SPF in 37% and the UVA protection factor (UVA-PF) in 26%. The in vivo data indicated that FA reinforced the broad-spectrum characteristic of the photoprotective formulations. Additionally, according to the results from the ex vivo antioxidant test, it is plausible to recommend adjustments on the ex vivo protocol to explicitly determine the positive effects of topical antioxidant ingredients applied over the skin. These results provided a new perspective for the development of multifunctional bioactive sunscreens using FA as a new platform.

SPF enhancement provided by rutin in a multifunctional sunscreen

ABSTRACT Unprotected chronic exposure to solar radiation can contribute to premature skin cancer and sunscreens are a key factor to avoid those detrimental effects. Currently, there is a growing interest in the photoprotector and antioxidant potential of bioactive substances, such as rutin, that could increase the sun protection factor (SPF) value and, also, donate multifunctional characteristics to sunscreens. Recent in vitro findings indicated that rutin, when incorporated into sunscreens, can provide antioxidant activity and SPF improvement. However, clinical studies are fundamental to determine this activity, due to the lack of repeatability of in vitro methodology and low correlation with the in vivo data. We aimed at evaluating the clinical safety and in vivo SPF of rutin by comparing sunscreen formulations containing 0.1% (w/w) rutin, 3.0% (w/w) butyl methoxydibenzoylmethane and 8.0% (w/w) octyl dimethyl PABA (2‐ethylhexyl 4‐(dimethylamino)benzoato) with a similar bioactive‐free preparation. Additionally, skin hydration, in vitro SPF and in vitro antioxidant activity of rutin, in association with the ultraviolet (UV) filters, were investigated. The safety profile of the formulations under sun‐exposed skin conditions qualified the formulas for clinical efficacy assays. 2,2‐Diphenyl‐1‐picrylhydrazyl (DPPH) test confirmed the antioxidant properties of rutin, revealing around 40% increase in radical scavenging potential when the bioactive compound was present. Rutin in combination with the UV filters robustly elevated the clinical SPF around 70%, when compared with the bioactive‐free formulation. To date, this is the first report in the specialized literature of an in vivo SPF measurement of a rutin‐containing photoprotective preparation, supporting the claim that rutin is an effective and safe bioactive compound to be used in multifunctional sunscreens.

Spectroscopic and thermal characterization of alternative model biomembranes from shed skins of Bothrops jararaca and Spilotis pullatus

Recently, there has been an interest in the use of shed snake skin as alternative model biomembrane for human stratum corneum. This research work presented as objective the qualitative characterization of alternative model biomembranes from Bothrops jararaca and Spilotis pullatus by FT-Raman, PAS-FTIR and DSC. The employed biophysical techniques permitted the characterization of the biomembranes from shed snake skin of B. jararaca and S. pullatus by the identification of vibrational frequencies and endothermic transitions that are similar to those of the human stratum corneum.