Impact of ferulic acid and resveratrol on the effectiveness and safety of sunscreen

Abstract The combination of avobenzone (AVO) and octyl ρ-methoxycinnamate (OMC) is widely used to ensure broad-spectrum photo-protection because they absorb UVA and UVB, respectively. However, they are thermally and photo unstable because they degrade and undergo photo- tautomerization and trans-cis isomerization, thus reducing their photo-protection efficacy during UV exposure. This study aimed to evaluate the potential use of the antioxidants ferulic acid and resveratrol as stabilizing substances in AVO and OMC mixtures in solution or emulsion. The effects of both antioxidants on the thermal/photo-stability and suppression of the filter singlet state, besides skin permeation, were evaluated. Both antioxidants contributed to preserving OMC and AVO during the thermal stability test, which relates to the maintenance of photo-protection even after storing the formulations at high temperatures. Nevertheless, although resveratrol retained part of the OMC trans isomer and suppressed the AVO singlet state when exposed to UV, no contribution to photo-protection stability was observed, contrary to expectations. Regarding the permeation assay, the addition of both antioxidants was accompanied by a reduction of AVO permeation, while resveratrol increased OMC permeation. Thus, the chemical and physicochemical properties of these antioxidants impacted their efficacy and safety profiles; therefore, further studies are required to establish the real cost-benefit ratio for their use in sunscreens.

A randomized controlled pilot study of a proprietary combination versus sunscreen in melasma maintenance

Background: Melasma is the commonest cause of facial hypermelanosis in skin type IV-VI. First-line treatment includes a triple combination containing topical corticosteroid and hydroquinone which have side effects on prolonged use. Chemical peels are a second-line management option with the laser being used in refractory cases, but the worsening of hyperpigmentation in darker skin types can occur following laser therapy. Sunscreen is a must to prevent relapses. Aims and Objectives: (i) To compare the effects of treatment with a proprietary combination (phenyl ethyl resorcinol, nonapeptide-1, aminoethyl phosphinic acid, antioxidants and sunscreen) versus sunscreen alone in limiting or reducing, melasma and preventing recurrence as a maintenance regimen after the initial use of triple combination,(ii) to evaluate the safety of the formulation studied, and (iii) to study the improvement of the quality of life of the patients after using the study formulation versus placebo. Methods: It was a prospective double-blinded parallel-group randomized controlled pilot study. A total of 46 subjects were recruited by consecutive sampling methods and randomized to 23 each in case and control groups. The study period was eight months with three phases. Phase 1 constituted the application of triple combination for eight weeks by both groups followed by phase 2 with the case group applying proprietary medicine and the control group applying sunscreen. Phase 3 was a follow-up period to see the sustenance of results in both groups as well as any evidence of relapses. Sunscreen was applied in all three phases. Results: Case group in the study showed improvement in the melasma severity score and mean melanin index as measured by mexameter but it did not attain statistical significance as compared to the control group. The melasma area and severity index score showed a consistent reduction in the case group, whereas it increased in the control group from baseline. Limitations: Small sample size and a short follow-up period of our study were major limitations. Conclusion: The proprietary combination, which has sunscreen as one of its constituents, is more effective in maintaining remission after triple combination without any added inconvenience of application of two separate preparations as compared to sunscreen alone

Effectiveness of sunscreens and factors influencing sun protection: a review

Abstract The effectiveness of sun protection depends directly on the photo-protective product employed, the way it is used and the amount applied. Many studies report that sunscreens are often applied incorrectly, at amounts much lower than those recommended for the sun protection factor (SPF) specified on the label. When not used properly, the effectiveness of the product against sun exposure damage is reduced. Currently, sunscreens are available in a variety of different formulations and types, such as stick (bar), aerosol, cream, lotion, oil, tanning formulations and makeup. However, developing an effective stable photo-protective formula that can be correctly applied regardless of type poses a challenge, as effectiveness is dependent on several factors. Factors influencing effectiveness include sun exposure conditions (direct or indirect), level of protection (SPF), amount of product applied, maximum exposure period before reapplication, product type (spray, lotion, etc.), layer thickness required, coverage, and ability to spread and permeate into the skin. Studies comparing the effectiveness of different forms of sunscreens, the amount of product applied by consumers and SPF and UVA protection determined by validated methodologies, are lacking. Therefore, the objective of this study was to review the available literature on the topic and discuss the effectiveness of sunscreen formulations and factors influencing sun protection. This review was carried out on the scientific databases MEDLINE, PubMed and Scielo. Of the many publications retrieved, thirty-nine articles most relevant for this review were selected.

A study on 2-(2'-hydroxyphenyl) benzoxazoles derivatives as potential organic UV filters, Part I

Abstract Damage resulting from the incidence of ultraviolet (UV) radiation on the skin is common nowadays, with UVB (290-320 nm) and UVA (320-400 nm) radiation responsible for photoaging, sunburn and carcinogenesis. For this reason, sunscreens represent products of growing interest to prevent such damage. However, there are few organic filters marketed worldwide with photostability and effectiveness at wavelengths greater than 340 nm (long UVA), which justifies the exploration for new compounds. In this work, we determined the photostability and sun protection factor (SPF) of three 2-(2'-hydroxyphenyl)benzoxazole derivative dyes in order to develop new organic UV filters. UV-vis spectrophotometry has high level of reproducibility when compared with in vivo human clinical methods. Solubility determinations were performed in different solvents. The compounds absorbed UVA and UVB radiation, with maximum absorption wavelengths ranging from 336 to 374 nm. Photostability was evaluated using a solar simulator (3 J.m2.s-1 UVA radiation) for a maximum of 3 h. The 2-(amino-2'-hydroxyphenyl) benzoxazoles showed higher photostability than the acetylated derivative under the evaluated conditions. The three benzoxazoles presented SPF values of around 40 and preliminary results indicate that they show suitable properties to act as good chemical filters in photoprotective formulations.

Evaluation of cell biomarkers as in vitro photoprotective assays for sunscreen formulations

Objectives: The aim of this study was to evaluate cellular indicators, which change with exposure to ultraviolet (UV) radiation and can be used as parameters for measuring sunscreens efficiency. Methods: Commercial strains of L929 and HaCaT cells (skin dermis and epidermis, respectively), from the cell bank of Rio de Janeiro, were exposed to different doses of UVA (350 nm) and UVB (309 nm) radiation. The evaluation of the photoprotective potential of sunscreens was analyzed with cell viability, lipid peroxidation and ROS generation tests. Samples of sunscreen with SPF values ranging from 15 to 60 were applied to a quartz plate superimposed on the top of a microplate containing the cell culture, and then the system was irradiated. Results: The viability and lipid peroxidation of the two cell lines remained unchanged after exposure to UVA radiation. When exposed to UVB radiation, the reduction in viability and the increase in lipid peroxides were dose-dependent, that is, they varied from 3.15% to 95.4%, and from 1.2 to 42.7 nM MDA/pg protein, respectively, both for the L929 strain. The dose of 0.5 J/cm2 reduced by 41.4%±1.67 the number of viable cells, and the dose of 30 J/cm2 promoted the oxidation of 42.7 nM of MDA/pg protein. These doses were selected to evaluate the photoprotective effectiveness of commercial sunscreens. Sunscreens exposed to UVB rays could prevent the loss of cell viability (viability remained around 100% for higher SPF) and the formation of lipid peroxides (30 to 80% reduction of peroxide levels). None of the two cell strains, submitted to UVB radiation, formed amounts of intracellular ROS in a dose-dependent manner. Under exposure to UVA radiation, only the HaCaT cell line produced the largest amounts of ROS in a dose-dependent manner. After treating these cells with photoprotective formulations (20 J/cm2), the researchers observed a reduction in the amount of ROS formed. Conclusions: The parameters of cell viability and lipid peroxidation were promising to evaluate the photoprotective capacity of sunscreens against UVB radiation. The generation of ROS expressed in the HaCaT strain can discriminate the photoprotective potential of formulations against UVA radiation, as sunscreens reduced the formation of ROS. These results suggest that in vitro tests that evaluate the damage caused to cells can predict cellular indicators of the photoprotective effectiveness of sunscreens and contribute to minimize these tests in the initial phase of product research and development.

Knowledge, attitude, practice and perception on sunscreen and skin cancer among doctors and pharmacists

@#Introduction: Excessive ultraviolet light (UV) can cause premature skin aging and potentially skin cancer. Currently there is a lack of awareness among health care professionals and the public on sun protection. The objectives of this study were to determine knowledge on sunscreen and skin cancer among health care professionals, to evaluate the knowledge, attitude, practice and perception of doctors and pharmacists toward the usage of sunscreen as protection against UV radiation. Materials And Methods: This is a cross-sectional study conducted among doctors and pharmacists in Hospital Sultanah Nora Ismail, Batu Pahat, Johor, Malaysia. Questionnaires were used in this study. Results: A total of 384 participants completed the questionnaires. The participants consisted of 323 doctors (84.1%) and 61 pharmacists (15.9%). The age group of the participants ranged between 25 till 55 years old. Ninety doctors (27.9%) and thirty-one pharmacists (51.0%) reported used sunscreen daily (p<0.001). This finding showed that there was a deficit in the practice of sun protection. Pharmacists scored a higher knowledge score of median 12 (IQR=3.0) while the doctors scored 11 (IQR=2.0). This study showed a significant association between ethnicity and skin cancer knowledge (p<0.05). Conclusion: This study demonstrated a lack of knowledge of sunscreen and skin cancer prevention among health care practitioners. This finding supports better medical education program on this topic.

Determination of lanthanum in whole blood by microwave digestion-inductively coupled plasma optical emission spectrometry / 药学实践杂志

Objective To evaluate the transdermal safety of lanthanum (La) in sunscreen and jellyfish sting protective lotion, establish a microwave digestion-inductively coupled plasma opticalemission spectroscopy (ICP-OES) method for determination of lanthanum (La) in rat’s whole blood. Methods The whole blood samples were digested by microwave and analyzed by inductively coupled plasma emission spectrometer (ICP-OES). Using 333.749 nm as the analysis line, the content of La in rat whole blood was determined. Results The correlation linearity of the standard curve of this method was good (r>0.9994), the detection limit of the method was 0.0025 μg/ml, the limit of quantification was 0.0077 μg/ml, the precision was less than 3%, and the recovery rate was between 94.9% and 102.0%. Conclusion The ICP-OES method based on microwave digestion is stable and reliable, and can provide an important basis for the study of the transdermal safety of lanthanum.

Comparison of the photoprotective effect between hydrolyzed and aglycones flavonoids as sunscreen: A systematic review

Currently, there is growing evidence of the role of polyphenols as protection agents against ultraviolet radiation(UVR), both in plant and animal cells, especially flavonoids, which are considered beneficial compounds that increasephotoprotection of sunscreen formulations. The objective of this systematic review is to analyze if there is an increase inphotoprotection of the hydrolyzed forms of polyphenols, specifically of flavonoids, such as quercetin and kaempferol,with respect to their corresponding glycosides, which are present in polar extracts of aerial parts of plants. Followingthe PRISMA guidelines, the systematic review was carried out in three electronic databases (Science Direct, Pubmed,and Embase) to identify the main articles that evaluated the effect of polyphenols against UVR protection. From atotal of 1,230 research articles found, 21 met the inclusion parameters, of which 13 studies evaluated extracts isolatedfrom different plants, and one study evaluated an agroindustrial residue. In all the cases, the main constituents werecharacterized as flavonoid compounds, including some of the compounds of interest of this revision. The effect ofthe pure compounds rutin and quercetin, as photoprotection enhancers, was evaluated in seven articles. Although aconclusive answer to the objective question of this systematic review could not be obtained, all the studies confirmedthe biological activity of the polyphenols as photoprotector.

Antiproliferative and photoprotective activities of the extracts and compounds from Calea fruticosa

In this paper, we complement our previous study on the antiproliferative activity of Calea fruticosa (Asteraceae) by isolating the compounds apigenin-4',7-dimethyl ether (1), budlein A (2), quercetin (3), and cichoriin (4) from the plant's aerial parts. The antiproliferative activity of these compounds was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method against human tumor cell lines. Compound 3 displayed moderate antiproliferative activity in three cell lines (HCT-116, PC-3, and SF-295, with cell growth inhibition values of 72.97, 74.55, and 68.94%) and high antiproliferative activity (90.86%) in the HL-60 cell line. The in vitro sun protection factor (SPF) of the extracts and compound 4, with and without sunscreen, was determined by a spectrophotometric method. The ethanol extract exhibited the highest SPF (9.67) at a concentration of 0.100 mg/mL, while compound 4, isolated from this extract, showed a SPF of 13.79 at the same concentration. A relative increased efficacy of SPF was observed for the extracts and compound 4 when sunscreen was also used. Compound 4 has not been reported previously from any species within the genus Calea. Compounds 1-4 were obtained from this species for the first time.

Does using a high sun protection factor sunscreen on face, along with physical photoprotection advice, in patients with melasma, change serum vitamin D concentration in Indian conditions? A pragmatic pretest-posttest study

Background: Use of sunscreens on the face is becoming popular, and patients with melasma are prescribed sunscreen for use on the face. Results of a few Western studies on the effect of sunscreen use on serum vitamin D concentration are not applicable to Indian conditions. Aims: To examine the effect of use of a high sun protection factor (SPF 50+, PA++++) sunscreen on face in patients with melasma on serum concentration of 25-hydroxyvitamin D. Methods: Forty-five Indian patients (Fitzpatrick skin types III and IV) with melasma were advised to use a sunscreen with SPF 50 + for 3 months, 43 (33 female, 10 male; age 32.9 ± 8 years) completed the study. Patients staying outdoor for <4 hours applied sunscreen once daily after bath. Patients staying outdoors for >4 hours reapplied sunscreen 4 hours after first application. Patients were provided a container to measure the amount of sunscreen for use, which was approximately equal to recommended thickness. Compliance was tested by weighing the used tubes and tubes in use during monthly visits. Serum concentration of 25-hydroxyvitamin D was tested before and after the study period. Results: Amount of sunscreen advised (100.5 ± 29.2 ml) and the actual amount used (96.6 ± 27.9 ml) were similar (P = 0.53, t-test). The difference between serum concentrations of 25-hydroxyvitamin D at the baseline (19.20 ± 9.06 ng/ml) and at 3 months (18.91 ± 8.39 ng/ml) was not significant (P = 0.87, paired t-test, 95% confidence interval of difference −3.33 to 3.92). No correlation was found between the amount of sunscreen used and the percentage change in serum 25-hydroxyvitamin D concentration at 3 months (rho = 0.099, P = 0.528, Spearman's rank correlation). Limitations: Longer duration of application and a larger sample size may detect minor differences in vitamin D concentration. Conclusion: Using a high SPF sunscreen on the face, along with physical photoprotection advice, in patients with melasma for 3 months does not influence serum 25-hydroxyvitamin D concentration in Indian conditions.

Photoprotection / photostabilizer potential in a quercetin sunscreens: determination of physical-chemical, safety and efficacy properties / Potencial fotoprotetor / fotoestabilizador de filtros solares associados à quercetina: ensaios físico-químicos e pré-clínicos

Ultraviolet radiation (UV) is related to the development of skin cancer and photoaging, also produces free radicals or reactive oxygen species (ROS) that cause premature aging. Therefore, sunscreens with extended UV protection capacity have been studied associated with antioxidant compounds. Different components can be incorporated with the purpose of improving, the photoprotection efficiency, as well as other cosmetic attributes, creating a multifunctional product. Among the compounds, there are some to be used from natural origin that are excellent, because it reduces the side effects and toxicity. Flavonoids are good examples of natural agents, because have demonstrated photoprotective antioxidant action in food and it is also promising for topical use. The aim of this work is to develop photoprotective formulations with quercetin, evaluating potential photoprotective and antioxidant of each formulation through tests already established and described in the literature, with emphasis on in vitro testing of potential photoprotective, antioxidant and security (het-cam); ex vivo antioxidant potential (tape-stripping). The results show us the photoprotective and antioxidant capacity of quercetin and the ideal concentration for this potential, thereby contributing to the synthesis of new molecules and development of new products, concerning stable, safe and effective exposure to solar UV radiation, preventing new incidences of skin cancer and reduction of photoaging

A radiação ultravioleta (UV) está relacionada ao desenvolvimento de câncer de pele e fotoenvelhecimento, também produz radicais livres ou espécies reativas de oxigênio (EROs) que causam o envelhecimento precoce. Portanto, protetores solares com capacidade de proteção UV amplo espectro foram estudados associados a compostos antioxidantes. Diferentes componentes podem ser incorporados com o objetivo de melhorar a eficiência da fotoproteção, assim como outros atributos cosméticos criando um produto multifuncional. Entre os compostos a serem utilizados, de origem natural são excelentes, pois reduzem os efeitos colaterais e a toxicidade. Os flavonóides são bons exemplos de agentes naturais, porque demonstraram ação antioxidante fotoprotetora nos alimentos e também são promissores para uso tópico. O objetivo deste trabalho é desenvolver formulações fotoprotetoras com quercetina, avaliando potenciais fotoprotetores e antioxidantes de cada formulação através de testes já estabelecidos e descritos na literatura com ênfase em ensaios in vitro de potenciais fotoprotetores, antioxidantes e de segurança (het-cam); potencial antioxidante ex vivo (tape-stripping). Os resultados nos mostram a capacidade fotoprotetora e antioxidante da quercetina e a concentração ideal para este potencial, contribuindo para a síntese de novas moléculas e desenvolvimento de novos produtos estáveis, seguros e eficazes em relação à exposição à radiação solar UV, prevenindo novas incidências de câncer de pele e redução do fotoenvelhecimento

Development and characterization of photoprotective formulations containing keratin particles

This work deals with development and evaluation of MFQ protective formulation, which contains two organic filters, namely: octyl-p-methoxycinnamate (OMC) and benzophenone-3 (BP-3); a photostabilizing agent called ethylhexylmethoxycrylene (EHMCR) and keratin particles. The MFQ formulation was evaluated in order to measure its pH, spin-spin lattice relaxation time (T2H), occlusivity factor, formulation efficacy, photostability and skin permeation, as well as keratin particle properties. Keratin particle size increased when incorporated to formulation, however, it did not affect pH. The MFQ formulation was found to be photostable and photoprotective, as evidenced by sunlight photostability test, sun protection factor (SPF), UVA/UVB ratio and critical wavelength. Interaction between keratin particles and active substances (OMC, BP-3 and EHMCR) was evidenced by T2H measurements. Evidences suggest that keratin reduces the permeation of both UV filters employed along this study, therefore, it can be stated that keratin has a promising potential for use in sunscreen formulations.

In vitro spf determination of embilica officinalis and nelumbu nucifera seed oils

Medicinal plants are natural gift to human lives to promote disease free healthy life. The phytochemicals present in leaf, fruits and vegetables could reduce various risks of diseases owing to prevent the oxidative damage produced by free radicals. The plant seed also contain many active molecules responsible for various medicinal properties. N.nucifera, E,officinalis, M. oleifera, T.chebula, T.bellerica and flax seed oils are tested for SPF determination by in vitro method. The seed oils had shown very good SPF values. E.officinalis seed showed 25.77 as Sun Protection Factor (SPF) value and N.nucifera seed Cotyledon had 21.45 SPF values which was quite high when comparing other seed oils. This study supports the usage of seed oil as a UVB sun screen protector, an alternative source of nutrition and as well as renewable resources.

Antioxidant and photoprotective potential of Moringa oleifera Lam (Moringaceae) / Potencial antioxidante e fotoprotetor de Moringa oleifera Lam (Moringaceae)

Moringa oleifera Lam. (Moringaceae) is a plant with several biological activities and therapeutic properties. However, the complete knowledge about its pharmacological, biological and ecological effects, and about the active components present in each vegetable part are not still completely elucidated. This study aimed to evaluate the antioxidant and photoprotective activities of different extracts from leaves and flowers of M. oleifera. These activities were assessed through in vitro tests, DPPH radical scavenging method, iron ion chelating effect (FRAP), lipid peroxidation (TBARS), nitric oxide scavenging method and assessment of the activity against the lipid peroxidation through hemolytic method. The photoprotective activity was assessed through spectrophotometric analysis and through in vitro test with Labsphere. It was also determined the extract's phenolic content and total flavonoid through spectrophotometry and HPLC. The obtained results demonstrated that this species have components with antioxidant and photoprotective potential mainly in the extracts obtained from fresh leaves and flowers. Therefore, it was possible to verify that M. oleifera has potential to be used as source of antioxidant components with photoprotective activity mainly due to the presence of phenolic components and among these, the flavonoids.

Moringa oleifera Lam. (Moringaceae) é uma planta com várias atividades biológicas e propriedades terapêuticas. No entanto, o conhecimento completo sobre seus efeitos farmacológicos, biológicos e ecológicos, e sobre os componentes ativos presentes em cada parte vegetal não são ainda completamente elucidados. Este estudo teve como objetivo avaliar as atividades antioxidantes e fotoprotetoras de diferentes extratos de folhas e flores de M. oleifera. Estas atividades foram avaliadas através de testes in vitro, método de eliminação de radicais DPPH, efeito de quelação de íons de ferro (FRAP), peroxidação lipídica (TBARS), método de eliminação de óxido nítrico e avaliação da atividade contra a peroxidação lipídica através do método hemolítico. A atividade fotoprotetora foi avaliada através de análise espectrofotométrica e através de teste in vitro com Labsphere. Também foi determinado o conteúdo fenólico do extrato e o flavonoide total através de espectrofotometria e HPLC. Os resultados obtidos demonstraram que esta espécie possui componentes com potencial antioxidante e fotoprotetor principalmente nos extratos obtidos a partir de folhas frescas e flores. Por conseguinte, foi possível verificar que a M. oleifera tem potencial para ser utilizado como fonte de componentes antioxidantes com atividade fotoprotetora principalmente devido à presença de componentes fenólicos e entre estes, os flavonoides.

Research on sunscreen lipstick to protect UVA and UVB / 药学实践杂志

Objective To prepare the sunscreen lipstick in order to prevent UVA and UVB.Methods The ratio of bees-wax,castor oil and liquid paraffin were optimized with the orthogonal test based on viscosity and heat resistance.The spread-able ability,stability and the anti-ultraviolet effect of the optimized lipstick were investigated.Results The best ratio of bees-wax,castor oil and liquid paraffin was 8:5:4(w/w/w).The viscosity of the sunscreen lipstick was appropriate,easy to spread and stable,which was demonstrated the good prevention effect from UVA and UVB.Conclusion The advantages of the prepared sunscreen lipstick included simple preparation,low cost and stable quality.It could be a new type of sunscreen lipstick protecting from UVA and UVB.

Desenvolvimento e otimização de protetores solares empregando os conceitos de qualidade por design (QbD) e tecnologia analí­tica de processos (PAT) / Development and Optimization of sunscreen applying Quality by Design (QbD) and Process Analytical Technology (PAT), 2018. (Master Degree)

Os protetores solares (PS) são os grandes responsáveis pela proteção da pele quando exposta à radiação solar, por isso a importância sanitária de se otimizar o desenvolvimento deste cosmético tipo II e monitorar para que seja eficaz em seu propósito. O principal objetivo deste trabalho é aplicar os conceitos de Qualidade por Design (QbD), ferramentas estatísticas de desenho experimental (DoE - Design of Experiments) e o conceito de tecnologia analítica de processo (PAT - Process Analytical Technology) para desenvolver uma formulação e processo produtivo de um PS de modo a modernizar os processos da indústria cosmética, fazendo as análises durante o processo e eliminando o controle de qualidade final. Trata-se de um sistema de desenvolvimento sistematizado, onde se executa as ferramentas de QbD para avaliar os dados obtidos ao longo da fase experimental. Para a fase experimental, empregou-se o desenho fatorial e desenho do compósito central (CCD - Central Composite Design) como ferramenta estatística, para a execução do planejamento de experimentos (DoE - Design of Experiments). As respostas foram analisadas através da metodologia de superfície resposta (RSM - Response Surface Methodology). Tais ferramentas são fundamentais para a determinação do desenho de concepção (design space), para se obter o PS com as melhores características físico-químicas e de processo dentro do escopo delineado. Para o desenvolvimento da metodologia de análise in line, optou-se pela utilização da espectrometria UV, utilizando-se ferramentas como análise de regressão dos mínimos quadrados (PLS) devido a praticidade em transforma-la em uma ferramenta PAT, para isto, a quimiometria foi empregada para modelar sistemas que são desconhecidos e complexos, como um PS, e trazendo respostas diretas como a aprovação do produto antes de ser embalado, por exemplo. A abordagem apresentada baseia-se na construção da qualidade ao longo do desenvolvimento e otimização de PS e torna possível o monitoramento da qualidade em tempo real

The sunscreens are great responsible for the skin protection when it is exposed to direct sunlight, so it means a great importance of health to optimize the development of type II cosmetic and monitor for it to be effective in its purpose. The objective of this work is to apply the concepts of Quality by Design and statistical tools of experimental design (DoE - Design of experiments), as well as applying the process analytical technology (PAT - Process Analytical Technology) concept for formulation and manufacturing process development of a topical sunscreen being able to modernize the cosmetic industry processing, including real time analyses and eliminating quarantine step, which waits analysis approval performed by the quality assurance, and then release the product for sale. As it is a systematic development, where critical quality attributes and risk assessment were performed to evaluate over obtained data. During experimental phase, the factorial design was used as a statistical tool for design of experiments implementation, and the responses were analyzed by response surface methodology (RSM - Response Surface Methodology). This mapping is critical to determination of the product design (design space), i.e. get sunscreen with the best physical and chemical characteristics and processing within the outlined scope. For in line methodology development, UV spectrometry was opted to be used due to less effort in sample preparation and due to great easiness to turn it into a PAT tool. For this, chemometrics was used, which brings together chemical and statistical elements to obtain three main elements: empirical modeling, multivariate modeling and chemical data, making it able to model systems that are unknown and complex, as a sunscreen, getting direct answers as product release approval before being packed, for example. The presented approach was based on the construction of quality throughout the sunscreen development and optimization making possible the real time quality monitoring

Fotoprotetores bioativos contendo extrato de mirtilo (Vaccinium myrtillus L. ): caracterização físico-química e funcional / Bioactive sunscreens containing blueberry (Vaccinium myrtillus L. ): physicochemical and funcional characterization

Os efeitos deletérios causados pela radiação ultravioleta (UV) e o aumento significativo no diagnóstico de câncer de pele, confirmam a necessidade de um progresso significativo na pesquisa de produtos fotoprotetores eficazes e seguros, para proteção eficaz da pele. As formulações atuais associam filtros UV, orgânicos e inorgânicos, com eficácia limitada e que podem acarretar reações cutâneas adversas. O extrato de Vaccinium myrtillus L. (EVM) apresenta em sua composição compostos fenólicos, como as antocianinas, que possuem atividade antioxidante. O objetivo deste estudo foi avaliar formulações fotoprotetoras contendo extrato de Vaccinium myrtillus L. com amplo espectro de ação e concentrações reduzidas de filtros UV. As emulsões contendo ou não EVM e filtros orgânicos (octocrileno e metileno bis-benzotriazolil tetrametilbutilfenol) e inorgânico (dióxido de titânio) foram avaliadas e consideradas estáveis perante parâmetros pré-definidos. O perfil de segurança foi determinado pelo método in vitro Hen´s Egg Test - Chorioallantoic Membrane (HET-CAM) e o potencial antirradicalar do EVM foi confirmado pelo teste de DPPH• A formulação fotoprotetora acrescida de 5,0% de EVM foi avaliada quanto à eficácia fotoprotetora in vivo e in vitro e não demonstrou aumento significativo no FPS quando comparada à formulação que continha somente os filtros solares e, no ensaio referente à hidratação da pele, não houve alteração nos dados, segundo teste de eficácia clínica. Os resultados obtidos sugeriram que mesmo não apresentando aumento no valor de FPS in vivo, a formulação fotoprotetora contendo o extrato, poderia atuar como agente antioxidante evitando os danos provocados pela radiação UV

The deleterious effects caused by ultraviolet radiation (UV) and the significant increase in the diagnosis of skin cancer confirm the need for significant progress in researching effective and safe sunscreen products for effective skin protection. Current formulations associate UV, organic and inorganic filters with limited efficacy that can lead to adverse skin reactions. Vaccinium myrtillus extract (EVM) contains in its composition polyphenols compounds, such as anthocyanins, which have been antioxidant activity. The objective of this study was to evaluate sunscreens containing EVM with broad action spectrum and reduced concentrations of UV filters. Emulsions containing or not EVM and organic (octocrylene and methylene bis-benzotriazolyl tetramethylbutylphenol) and inorganic (titanium dioxide) filters were evaluated and considered stable under pre-defined parameters. The safety of the emulsion was assessed was determined by the in vitro Hen´s Egg Test - Chorioallantoic Membrane method (HET-CAM) and the antiradical potential of EVM was confirmed by the DPPH• test. The sunscreen formulation containing EVM 5.0% was photoprotective efficacy evaluated in vivo and in vitro and did not show a significant increase in SPF when compared the formulation only with UV filters and no improves skin hydration, according to clinical efficacy assay. The results of the study suggest that even without increase SPF in vivo, the sunscreen formulation containing the extract may show antioxidant activity avoiding damage caused by UV

Optimization and formulation of sunscreen creams / 中华医学美学美容杂志

Objective To optimize the formulation of the sunscreen used in military training.Methods The different formulations of sunscreen were prepared according to the orthogonal design,and then applied on 3M adhesive tape posted on the color dish with a certain amount;the absorbance in 280 nm-320 nm and 320 nm-400 nm of them were measured and the arithmetic mean (A) was concluded.By comparing A,the protective effect and the main factors affecting preventive bask were determined.The preventive bask test of the optimum formula was carried out in human trials using the method of multi point increasing ultraviolet irradiation.Results OMC,TinosorbTM M,rutin,pearl powder and baicalin all had significant effects in preventing UVA.OMC had a significant effect in preventing UVB.The formula 1 (containing the five materials mentioned above) had the best effects in preventing both UVA (SPF 18) and UVB (PA+).Conclusions The formula 1 has the best effects in preventing both UVA and UVB.

Fotoprotetores bioativos multifuncionais contendo rutina, octil dimetil PABA e avobenzona: caracterização físico-química, funcional e eficácia clínica / Bioactive sunscreens containing rutin, octyl dimethyl PABA and avobenzone: physicochemical, functional and clinical characterization

A exposição crônica à radiação solar pode contribuir para o aparecimento do câncer de pele, sendo o uso de fotoprotetores um fator primordial na prevenção desses efeitos deletérios. Atualmente, substâncias bioativas tais como a rutina têm sido foco de interesse da comunidade científica graças às suas propriedades fotoprotetoras e antioxidantes, que podem promover aumento dos valores de FPS, além de conferir características multifuncionais às formulações. Achados in vitro recentes indicam que a rutina, quando incorporada em emulsões fotoprotetoras óleo em água, promove aumento da atividade antioxidante e aumento do FPS. No entanto, a realização de estudos clínicos é fundamental para confirmar e quantificar esses resultados, já que a metodologia in vitro possui baixa repetibilidade e ausência de correlação com ensaios in vivo, principalmente quando as formulações analisadas apresentam substâncias antioxidantes em sua composição. O objetivo deste estudo foi avaliar pela primeira vez a atividade da rutina frente ao FPS e sua segurança clínica através da comparação de formulações fotoprotetoras contendo rutina 0.1% (w/w), avobenzona 3.0% (w/w) e octil dimetil PABA 8.0% (w/w) com uma preparação similar sem o composto bioativo. Adicionalmente, hidratação cutânea, FPS in vitro e atividade antioxidante da rutina em associação com outros filtros foram investigados. O perfil de segurança das formulações qualificou as fórmulas para os testes de eficácia clínica. O teste de DPPH confirmou a capacidade antioxidante da rutina, demonstrando cerca de 40% de aumento na capacidade de sequestro de radicais livres na presença do composto bioativo. A rutina em combinação com os filtros UV aumentou o FPS clínico de 7.30 ± 0.60 para 12.37 ± 1.13, o que representa cerca de 70% de aumento. Os resultados encontrados provam que a rutina em combinação com outros filtros pode aumentar significativamente o valor do FPS e que a mesma é segura para uso clínico

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 help to increase the SPF value and add multifunctional characteristics to the formulations. Recent in vitro findings indicated that rutin, when incorporated in oil-in-water photoprotective emulsions can provide antioxidant activity and SPF increase. However, clinical studies are fundamental to determine this activity duo to in vitro methodology lack of repeatability and correlation between the in vivo data, especially when the analyzed formulas contain antioxidant substances. The aim of this study was to evaluate for the first time to date the rutin in vivo SPF and clinical safety by comparing sunscreens formulations containing rutin 0.1% (w/w), butyl methoxydibenzoylmethane 3.0% (w/w) and octyl dimethylPABA 8.0% (w/w) with a similar bioactive-free preparation. Additionally, skin hydration, in vitro SPF and in vitro antioxidant activity of rutin, in association with the UV filters were investigated. The safety profile of the formulations under sun-exposed skin conditions qualified the formulas for clinical efficacy assays. DPPH test confirmed rutin antioxidant properties, demonstrating about 40% increase in radical scavenging potential when the bioactive compound was present. Rutin in combination with the UV filters increased the clinical SPF from 7.30 ± 0.60 to 12.37 ± 1.13, representing about 70% growth in the SPF value. The results obtained proved that rutin in combination with UV filters can improve the SPF value significantly and is safe for clinical use

Hydrolyzed collagen interferes with in vitro photoprotective effectiveness of sunscreens

ABSTRACT The chronological skin aging is a progressive and natural process with genetic and physiological changes. However, ultraviolet (UV) radiation may accelerate the oxidative stress, generating carcinogenesis and photoaging. Natural compounds and their applications are considered a trend in the cosmetic market. The protein-based film-forming compounds play an important role, once it collaborates for the better distribution of sunscreens on the skin. Here we investigated the in vitro photoprotective effectiveness of sunscreens containing the hydrolyzed collagen associated with UVA, UVB and/or inorganic filters. Sunscreens were developed with octocrylene (7.5%), butyl methoxydibenzoylmethane (avobenzone) (3.0%) and/or titanium dioxide (5.0%), associated or not with the hydrolyzed collagen (3.0%). In vitro photoprotective effectiveness was determined in a Labsphere(r) UV2000S by the establishment of the sun protection factor (SPF) and critical wavelength (nm) values. Physicochemical and organoleptic characteristics were also assayed. The hydrolyzed collagen subjectively improved the formulation sensory characteristics. However, this bioactive compound led to a decrease of the SPF values of the photoprotective formulations containing octocrylene alone and octocrylene + butyl methoxydibenzoylmethane + TiO2. This inadequate interaction may be considered during the development of new sunscreens intended to contain protein-based components.