Daniela D'Almeida Peres

Cutaneous biocompatible rutin-loaded gelatin-based nanoparticles increase the SPF of the association of UVA and UVB filters

The encapsulation of natural ingredients, such as rutin, can offer improvements in sun protection effectiveness. This strategy can provide enhanced flavonoid content and produces an improved bioactive compound with new physical and functional characteristics. As an alternative to common synthetic-based sunscreens, rutin-entrapped gelatin nanoparticles (GNPs) were designed and associated with ethylhexyl dimethyl PABA (EHDP), ethylhexyl methoxycinnamate (EHMC) and methoxydibenzoylmethane (BMDBM) in sunscreen formulations. The purpose of this study was to develop rutin-loaded gelatin nanoparticles and characterize their physicochemical, thermal, functional and safety properties. Rutin-loaded gelatin nanoparticles increased antioxidant activity by 74% relative to free-rutin (FR) solution. Also, this new ingredient upgraded the Sun Protection Factor (SPF) by 48%, indicating its potential as a raw material for bioactive sunscreens. The safety profile indicated that GNPs and glutaraldehyde (GTA) decreased HaCaT cell viability in a concentration/time-dependent manner. However, both blank nanoparticles (B-NC) and rutin-loaded nanoparticles (R-NC) had good performance on skin compatibility tests. These results functionally characterized rutin-loaded nanoparticles as a safe SPF enhancer in sunscreens, especially in association with UV filters.

Functional photostability and cutaneous compatibility of bioactive UVA sun care products

Sunscreens are the most-established approach for photoprotection. The strategy of providing antioxidant properties to sun care products by addition of natural and potent anti-free radical compounds has led to the development of bioactive sunscreens, able to neutralize the harmful effects of ultraviolet (UV) radiation. UVA filters, such as benzophenone-3 (BP) and butyl methoxydibenzoylmethane (BMDBM), can exhibit photodegradation which limits the development of broad spectrum sunscreens. Previous research verified that rutin interacts with filters incorporated in sunscreens. In this work, we focused on the development and evaluation of the efficacy of the sunscreens containing either BP or BMDBM with and without rutin. The addition of rutin to the UVA filters afforded antioxidant properties to the formulations and they were considered safe for human use. Additionally, rutin in combination with either BP or BMDBM increased the antioxidant activity about 40 times when compared with the UVA filters alone. Remarkably, the addition of rutin 0.1% (w/w) to BP 6.0% (w/w) raised the SPF from 24.3±1.53 to 33.3±2.89. In conclusion, these findings demonstrated that the addition of rutin into sunscreens can markedly improve the antioxidant properties of the formulation as well as photostabilize some of the UVA filters.

Quality by design (QbD), Process Analytical Technology (PAT), and design of experiment applied to the development of multifunctional sunscreens

Abstract Multifunctional formulations are of great importance to ensure better skin protection from harm caused by ultraviolet radiation (UV). Despite the advantages of Quality by Design and Process Analytical Technology approaches to the development and optimization of new products, we found in the literature only a few studies concerning their applications in cosmetic product industry. Thus, in this research work, we applied the QbD and PAT approaches to the development of multifunctional sunscreens containing bemotrizinol, ethylhexyl triazone, and ferulic acid. In addition, UV transmittance method was applied to assess qualitative and quantitative critical quality attributes of sunscreens using chemometrics analyses. Linear discriminant analysis allowed classifying unknown formulations, which is useful for investigation of counterfeit and adulteration. Simultaneous quantification of ethylhexyl triazone, bemotrizinol, and ferulic acid presented at the formulations was performed using PLS regression. This design allowed us to verify the compounds in isolation and in combination and to prove that the antioxidant action of ferulic acid as well as the sunscreen actions, since the presence of this component increased 90% of antioxidant activity in vitro.

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.

Photostabilization of sunscreens by incorporation of tea as the external phase: Fotoestabilização de protectores solares por incorporação de chás como fase externa

The use of isolated ultraviolet (UV) filters in photoprotective formulations creates products with limited protection against radiation, emphasising the need to develop formulations containing UVA and UVB filter combinations. However, most of the formulations developed to include both filters are unstable as a result of this combination, as well as by exposure to UV radiation. It is, therefore, crucial to include additives that enable photostabilization. Tea is the second most widely consumed beverage in the world and represents a good source of bioactive compounds, particularly polyphenols, which provide antioxidant activity. In the present work formulations containing green tea or black tea, as well as the sunscreens avobenzone (UVA sunscreen) and octilmetoxinamato (UVB sunscreen), were developed and evaluated in order to develop new and effective photostable formulations providing broad spectrum photoprotection. These formulations have been developed with complete replacement of the external phase of the oil in water (O/W) emulsion by these teas. The results showed that both teas presented photostabilizing capacity, particularly for green tea in the storage conditions at room temperature and at 5 °C, and black tea for the samples stored at 40 °C. Key-words: green tea, black tea, photoprotective formulations, photostabilizing capacity, octyl methoxynnamate, avobenzone

Impact of stirring speed, glycerin and sodium chloride concentrations on photoprotective nanoemulsions: Impacto da velocidade de agitação, contração de glicerina e de cloreto de sódio em nanoemulsões fotoprotetoras

New technologies that improve the physical as the sensory properties of sunscreens can help to increase its continued use and impact on health. The use of nanoemulsions in the development of photoprotective vehicles is an advantage, since nanostructured components may have superior properties regarding their performance when compared to conventional products. The advantages of using nanobiotechnology in manufacture of cosmetic and dermatological formulations arise from the protection of compounds from chemical or enzymatic degradation, from the control of their release, and also to the prolonged retention time of cosmetic ingredients in the stratum corneum. Thus, this study aimed to evaluate the impact of stirring speed and of glycerin and sodium chloride concentrations in the development and effectiveness of a nanoemulsion containing ethylhexyl methoxycinnamate and benzophenone-3. The results of statistical analyses regarding the impact of the variables in the process of nanoemulsion development showed that these parameters affect the phase inversion temperature (PIT). However, this did not affect the particle size and the photoprotective efficacy in vitro. Key-words: Nanoemulsion; Photoprotection; Ethylhexyl methoxycinnamate; Benzophenone-3

Stability and efficacy of sunscreens containing inorganic filters and quercetin: Estabilidade e eficácia de fotoprotetores contendo filtros inorgânicos e quercetina

__________________________________________________________________________________ Abstract Exposure to the sun can have health benefits, however, excess exposure can cause skin damage, such as skin cancer. Photoprotection can be used as a preventive method against the harmful effects of the ultraviolet (UV) radiation and Brazilian biodiversity is a fertile field for research in this area. Therefore, the aim of this study was the development of sunscreens containing quercetin (bioactive compound) and inorganic filters (titanium dioxide and zinc oxide) with further characterization of the formulae and evaluation of stability. Formulations containing the bioactive compound, isolated or in association with the inorganic filters, presented: pH values biocompatible with the skin; apparent viscosity between 10550 and 23600 cP; sun protection factor (SPF) between 2.1 and 22.5; and broad spectrum protection, with critical wavelengths above 379 nm. It was found that the association of quercetin with inorganic filters was not adequate due to the negative interactions that occurred between the bioactive compound and the metals, which were only identified during the stability study. However, considering the in vitro estimated efficacy of the isolated flavonoid, its use can still be explored as an alternative substitute to classic UV filters.