Ex vivo penetration analysis and anti-inflammatory efficacy of the association of ferulic acid and UV filters.

BACKGROUND: Unprotected chronic exposure to ultraviolet (UV) radiation generates many harmful effects to human skin and sunscreens are essential to health, however, traditional products do not provide enough protection against cutaneous oxidative stress, a process amplified by UV radiation. Therefore, the development of multifunctional photoprotective formulations seems to be a more efficacious approach, since these enable the absorption/reflection of UV radiation and maintain the cutaneous homeostasis. OBJECTIVES: In the present study, ferulic acid (FA), a well-known antioxidant, has been combined with two UV filters, bemotrizinol and ethylhexyl triazone, and the safety and efficacy of this formulation has been assessed combining ex vivo and in vivo methods. METHODS: Skin permeation assays were performed by applying the formulation in the volar forearm of participants, after which consecutive samples of the stratum corneum were collected by tape stripping, and the quantification of FA, bemotrizinol and ethylhexyl triazone was performed by high-performance liquid chromatography (HPLC). Also, the FA anti-inflammatory action in combination with the UV filters was probed through a method employing Laser Doppler flowmetry to measure the vasodilatory response to methyl nicotinate topical application. RESULTS: Skin permeation assay was able to characterize the penetration depth of each substance. It should also be noted that a specific HPLC analytical method was developed in this study to enable the rapid simultaneous quantification of the three substances. Results from Laser Doppler flowmetry showed that the FA was able to mitigate the vasodilatory response. CONCLUSIONS: FA proved to be a valuable resource in a multifunction sunscreen, not only providing an increase in the SPF of sunscreens, previously published, but also decreasing the extent of inflammation.

Butyrospermum parkii butter increased the photostability and in vivo SPF of a molded sunscreen system.

BACKGROUND: Ultraviolet (UV) radiation exposure is related to skin and lip tumors. Therefore, the development of photoprotective lipstick formulations is of utmost importance. AIMS: Considering the biological properties of Shea butter (Butyrospermum parkii), we assessed its potential as an adjuvant in a molded lipstick sunscreen system by in vivo tests and photostability. PATIENTS/METHODS: Shea butter was used in a photoprotective lipstick formulation at two different concentrations (10.0% and 15.0% w/w) associated with ethylhexyl methoxycinnamate (EHM) and titanium dioxide. Skin compatibility was assessed in vivo. The in vivo SPF value was determined according to the current recognized method. Additionally, the photostability of EHM was determined by high-performance liquid chromatography. RESULTS: By the cutaneous compatibility, the product presented no interference with skin barrier and no adverse reactions, thus proving its safety. The in vivo SPF assay showed that the highest concentration of Shea butter increased the in vivo SPF value of the sample by 35%, demonstrating it to be a booster in photoprotective lipstick formulations. Also, Shea butter was proved to enhance the photostability of EHM, a commonly used UVB filter available in several countries. CONCLUSION: Shea butter increased the photostability and in vivo SPF of a molded lipstick sunscreen.

Another Reason for Using Caffeine in Dermocosmetics: Sunscreen Adjuvant.

The excessive exposure to ultraviolet (UV) radiation is the main cause of skin cancer, the most commonly diagnosed cancer in the world. In this context, the development of innovative and more effective sunscreens, with bioactive compounds like caffeine, displaying antioxidant and anticancer potential, is required. This research work assessed in vitro and in vivo the efficacy and safety of topical sunscreen formulations containing caffeine as an adjuvant of the UV filters. Sunscreens were prepared with 2.5% w/w caffeine or in the absence of this compound. In order to evaluate the safety of these formulations, stratum corneum hydration, skin barrier and colorimetry were assessed in vivo in healthy subjects before and after skin treatment with the samples. The efficacy of the sunscreens was assessed in vitro, using PMMA plates and a spectrophotometer equipped with an integrating sphere; and in vivo by the determination of the sun protection factor (SPF). None of the formulations caused erythema or impaired the skin barrier function. The in vitro functional characterization showed higher SPF values for the caffeine formulation. The in vivo studies also confirmed the higher SPF value of the formulation combining caffeine with the filters, compared to the caffeine-free sample. This improvement contributed to an increase of, approximately, 25% in the in vivo anti-UVB protection. In conclusion, caffeine was well tolerated by the skin and increased the photoprotective activity, being a new alternative adjuvant in sunscreens formulation.

SPF enhancement provided by rutin in a multifunctional sunscreen.

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.

Active ingredients, mechanisms of action and efficacy tests of antipollution cosmetic and personal care products

Urban population around the globe is direct exposed to the pollution caused by several sources (vehicles, industries, smokes etc.) and primary pollutants are divided in particulate matter and toxic gases. Current researches in populous countries indicated that exposure to pollution could affect sebum composition, stratum corneum quality and signs of skin aging. Hair and scalp are also affected by the excessive exposure to pollutants, resulting in a dull, dry and lifeless appearance. Cosmetics have been evolved conceptual and scientifically to achieve substantial effectiveness against pollution damaging on the cutaneous tissue, involving the development of innovative multipurpose active ingredients and efficacy tests, skilled to prove the protection and benefits of such personal care products. In this review, we highlighted the skin and hair/scalp damages provoked by the main environmental pollutants and the active substances used in antipollution cosmetics/personal care products with the respective mechanisms of action. Likewise, in vitro and in vivo efficacy tests were discussed concerning the antipollution claim substantiating

Anti-inflammatory therapies in TRAMP mice: delay in PCa progression.

The aim of this study was to characterize the structural and molecular biology as well as evaluate the immediate and late responses of prostatic cancer in the transgenic adenocarcinoma of the mouse prostate (TRAMP) model after treatment with goniothalamin (GTN) and celecoxib. The treated mice received GTN (150 mg/kg, gavage) or celecoxib (10 mg/kg, gavage) from 8 to 12 weeks of age. They were killed at different ages: the immediate-response groups at 12 weeks and the late-response groups at 22 weeks. The ventral prostate was collected for light microscopy, immunohistochemistry, western blotting, TUNEL, and ELISA. Morphological analyses indicated that GTN treatment delayed the progression of prostatic adenocarcinoma, leading to a significant decrease of prostatic lesion frequency in both experimental period responses to this treatment, mainly high-grade prostatic intraepithelial neoplasia and well-differentiated adenocarcinoma. Also, the celecoxib treatment showed a particular decrease in the proliferative processes (PCNA) in both the experimental periods. Despite celecoxib diminishing the COX2 and IGFR1 levels, GTN presented higher action spectrum considering the decrease of a greater molecular number involved in the proliferative and inflammatory processes in prostatic cancer. Goniothalamin attenuated the pro-inflammatory response in TRAMP prostatic microenvironment, delaying prostate cancer (PCa) progression. Celecoxib treatment was efficient in the regulation of COX2 in the TRAMP mice, mainly in the advanced disease grade. Finally, we concluded that inflammatory process control in early grades of PCa was crucial for the downregulation of the signaling pathways involved in the proliferative processes in advanced cancer grades.

Ethanol intake-induced apoptosis in glial cells and axonal disorders in the cerebellar white matter of UChA rats (voluntary ethanol consumers).

Ethanol intake may cause alterations in cellular metabolism altering motricity, learning and cognition. The cerebellum is one of the most susceptible organs to ethanol-related disorders during development, and is associated with oxidative stress-induced apoptosis being crucial for pathogenic consequences. The UChA variety is a special strain of Wistar rat genetically selected and represents a rare model for the studies related to genetic, biochemical, physiological, nutritional, and pharmacological effects of ethanol. We evaluated the structure and apoptosis in the cerebellar white matter of UChA rats. There were two groups of 09 rats: a control group that did not consume ethanol, and an experimental group of UChA rats that consumed ethanol at 10% (v/v) (<2 g ethanol/kg body weight/day). At 120 days old, rats were anaesthetized followed by decapitation, and their cerebella were collected and fixed. Cerebellar sections were subjected to immunohistochemistry for Caspase-3 and XIAP and transmission electron microscopy (TEM). The UChA group showed more glial cells immunoreactive for caspase-3 and less for XIAP than control group. Alcohol consumption affected myelin integrity. Severe ultrastructural damages in UChA group were observed such as disruption of the myelin sheath, disorganization and deformation of its components, and an increase in the interaxonal spaces. In conclusion, our data demonstrated that ethanol induced apoptosis in the glial cells and promoted an intense change in the myelin sheath of UChA rats, which may cause functional disorders.