Publications by authors named "Maria Valéria Robles Velasco"

41 Publications

An Overview on Topical Administration of Carotenoids and Coenzyme Q10 Loaded in Lipid Nanoparticles.

Antioxidants (Basel) 2021 Jun 26;10(7). Epub 2021 Jun 26.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo 05508-900, Brazil.

Carotenoids and coenzyme Q10 are naturally occurring antioxidant compounds that are also found in human skin. These bioactive compounds have been the focus of considerable research due to their antioxidant, anti-inflammatory, and photoprotective properties. In this review, the current state of the art in the encapsulation of carotenoids and coenzyme Q10 in lipid nanoparticles to improve their bioavailability, chemical stability, and skin absorption is discussed. Additionally, the main findings are highlighted on the cytotoxic and photoprotective effects of these systems in the skin.
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http://dx.doi.org/10.3390/antiox10071034DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8300771PMC
June 2021

Potential use of essential oils in cosmetic and dermatological hair products: A review.

J Cosmet Dermatol 2021 Jun 15. Epub 2021 Jun 15.

Institute of Physics, University of São Paulo, São Paulo, Brazil.

Background: Essential oils have great interest among the increasing demand for herbal cosmetics in the market. They are natural sources of biologically active ingredients due to the wide application of such compounds as well as their particular chemical composition. Several researches have evaluated the effectiveness of these bioactive ingredients for use in cosmeceuticals, mainly in both hair scalp and shaft hair damage repair. Thus, the amounts and their associations define the properties of these compositions with interest for hair cosmetic use, such as antioxidant, inflammatory, and antimicrobial activities. Because they are complex compounds, their actions on the skin, hair scalp, and shaft are not yet fully understood.

Aims: The purpose of this review is to highlight the relevant researches and findings on essential oils in hair care.

Methods: In order to achieve this objective, the present work comprises an updated bibliographic review related to essential oils used in hair care.

Results: It was possible to observe that cosmeceuticals containing essential oils applied to the scalp are preferable for topical activity. Also, it was noticed that there are few reports regarding their use in hair shaft. However, it was found that some oils are used to intensify the brightness and fix the hair color.

Conclusions: This work demonstrated that the use of essential oils in both cosmetic products (industrial application) and those associated with oils carriers (as individual protocols) may lead to satisfactory results in the treatment of some scalp dysfunctions.
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http://dx.doi.org/10.1111/jocd.14286DOI Listing
June 2021

Vitamin E-loaded bigels and emulsions: Physicochemical characterization and potential biological application.

Colloids Surf B Biointerfaces 2021 May 21;201:111651. Epub 2021 Feb 21.

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl. 15, 05508-900, São Paulo, SP, Brazil. Electronic address:

Bigels have been studied as topical formulations for its benefits over sensory and drug delivery parameters. However, there is still few evidences about the properties of the combination of organogelators, oily phases and bioactive molecules into rheological and stability behavior. We investigated the use of classical organogelators (candelilla wax and 12-hydroxystearic acid) and oily phases (sunflower and mineral oil) in 5/95 organogel/polymeric hydrogel ratio to compare vitamin E bigels with its corresponding emulsions. The rheological measurements, microstructure, physical and oxidative stability properties and biological behavior were evaluated. The obtained oil-in-water bigels and emulsions showed crystallization pattern at the interface with high thermal and centrifuge-stress stability. Viscoelastic weak gels were obtained with higher thixotropy and consistency of 12-hydroxystearic bigels. The diameter of the inner phase was increased by vitamin E, despite its little influence over physical and oxidative stability of bigels and emulsions. Those findings indicated that sensory attributes may be regulated by the organogel composition.
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http://dx.doi.org/10.1016/j.colsurfb.2021.111651DOI Listing
May 2021

Analytical tools for urocanic acid determination in human samples: A review.

J Sep Sci 2021 Jan 3;44(1):438-447. Epub 2020 Nov 3.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.

Urocanic acid is a chromophore found in the skin that has been identified as an important immunosuppressant and carcinogenesis mediator through its photoisomerization from trans to cis form induced by ultraviolet radiation. Research on analytical methods that explore urocanic acid isomerization is indispensable to fully understand the deleterious effects mediated by this biomarker. In this context, the current relevant analytical methods for determination of these isomers in human samples are summarized in this review. The methods presented here are applicable to human samples collected by noninvasive methods (or minimally invasive), encompassing an array of analytical techniques, including high-performance capillary electrophoresis, confocal Raman spectroscopy, gas chromatography, high-performance liquid chromatography, and mass spectrometry, among others. Developed high-performance liquid chromatography methods have proven to be advantageous, allowing noninvasive collections for in vivo analysis and the confocal Raman, specially, for real-time analysis. Among all these methods, high-performance liquid chromatography is the most investigated one with mass spectrometry or ultraviolet detector, and the mass spectrometry detector being the most studied in the last years, demonstrating high sensitivity, very low detection limits, and accurate identification, especially for clinical investigations.
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http://dx.doi.org/10.1002/jssc.202000713DOI Listing
January 2021

(Bio)Technological aspects of microalgae pigments for cosmetics.

Appl Microbiol Biotechnol 2020 Nov 5;104(22):9513-9522. Epub 2020 Oct 5.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl.15, São Paulo, 05508-900, Brazil.

Photosynthetic microorganisms convert carbon dioxide and solar radiation into interesting bioactive compounds not yet entirely explored. Several species of microalgae are known to be rich in colored high-valuable components that, although remarkable, are poorly explored as natural sources of pigments for cosmetics. Pigments associated to photosynthetic activity include chlorophyll, β-carotene, astaxanthin, xanthophylls, and phycobiliproteins, many of which have shown high potential as cosmetic actives due to their antioxidant, immune-enhancing, and anti-inflammatory properties. In the last decade, concern with a young and beautiful appearance has emerged, encouraging many consumers to use anti-aging cosmetics daily. As a result, the cosmetic market has been growing and evolving rapidly to meet consumer expectations. However, due to regular use and the sensitive nature of facial skin, local adverse reactions may often occur, such as irritation, sensitization, or photoreactions, and safety evaluation is mandatory prior to marketing. It is, therefore, understandable that new actives from natural sources, such as microalgae, are perceived as attractive alternatives for consumers who seek ingredients without allergenic potential. Thus, the cosmetic industry has recently started to explore the inclusion of compounds extracted from microalgae and cyanobacteria in innovative formulations. Herein, we revised nontraditional microalgae species for pigment production with cosmetic applications, indicating those that could also be considered potential ingredients for innovative cosmetics. KEY POINTS: • Extraction methods for pigments from photosynthetic microorganisms were compiled. • Innovative cosmeceuticals could be developed with natural pigments. • Safety features of such natural pigments were also described.
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http://dx.doi.org/10.1007/s00253-020-10936-xDOI Listing
November 2020

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

Eur J Pharm Sci 2021 Jan 28;156:105578. Epub 2020 Sep 28.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil. Electronic address:

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.
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http://dx.doi.org/10.1016/j.ejps.2020.105578DOI Listing
January 2021

A short review of alternative ingredients and technologies of inorganic UV filters.

J Cosmet Dermatol 2021 Apr 16;20(4):1061-1065. Epub 2020 Sep 16.

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.

Background: The growing need to use sunscreens is a concrete reality, and it is associated with the increase in the population's awareness of the ultraviolet (UV) radiation damage. Inorganic UV filters promote the formation of particles/pigments film over the skin surface, reflecting, dispersing, and absorbing the radiation. Investigations of this class of filters demonstrate the emergence of alternative ingredients and new technologies.

Aims And Methods: In this review, we presented potential candidates for alternative UV inorganic filters, such as hydroxyapatite, cerium dioxide, and hydrotalcite.

Results: Specialized literature identified hydroxyapatite and cerium dioxide as actives with good performances, with a broad spectrum of absorption against UV radiation. Both of them were considered safe against degradation and skin erythema formation. Inorganic compounds as an alternative to circumvent degradation problems of organic UV filters containing PABA were also analyzed, with hydrotalcite having a good performance in improving the performance of classic ingredients, bypassing photoinstability, and improving safety, in addition to preventing skin irritability.

Conclusion: Further investigations of these ingredients and interactions with sunscreen formulations are necessary to overall explore their safety and efficacy, encouraging future researches for more inorganic UV filters.
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http://dx.doi.org/10.1111/jocd.13694DOI Listing
April 2021

In vivo SPF from multifunctional sunscreen systems developed with natural compounds-A review.

J Cosmet Dermatol 2021 Mar 29;20(3):729-737. Epub 2020 Jul 29.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.

Background: The use of sunscreens is mandatory, especially in countries with high ultraviolet (UV) incidence. In consequence, there has been a growing interest in using compounds from natural sources to develop new multifunctional products that protect human skin from the consequences of UV exposition. Even though there are in vitro methods to determine anti-UV efficacy, it is still required to test photoprotection activity on human skin to validate product performance.

Aim And Methods: In this review, we summarized all reported clinical studies about sun protection factor (SPF) measurements of sunscreens with natural compounds. We also discussed the probable action mechanism of those actives.

Results: Herein, we provided an overview on recent studies concerning photoprotection activity of compounds from natural sources, for example, rutin, ferulic acid, caffeine, shea butter, and plant extracts, mainly presented in sunscreen systems with efficacy clinically established by SPF.

Conclusion: Our review suggested that even when the in vivo SPF evaluation has inherent difficulties, it is essential to assure the real efficacy of sunscreens. Furthermore, the incorporation of natural compounds could enhance the in vivo SPF values of such sunscreens by different mechanisms. Finally, some compounds derived from natural resources with skin benefits could be used as "green"/natural UV filters that provide broad-spectrum sunscreens with further upgrading of the multifunctional dermocosmetic formulation to enhance aesthetics and even skin health.
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http://dx.doi.org/10.1111/jocd.13609DOI Listing
March 2021

Assessment of the Potential Skin Application of Benth.

Pharmaceuticals (Basel) 2020 Jun 10;13(6). Epub 2020 Jun 10.

CBIOS-Universidade Lusófona Research Centre for Biosciences & Health Technologies, Campo Grande 376, 1749-024 Lisbon, Portugal.

Benth. has widespread ethnobotanical use in African folk medicine for its medicinal properties in skin conditions. In this study, two different basic formulations containing extracts were prepared, one in an organic solvent and the other using water. The aqueous extract only contained rosmarinic acid (RA) at 2.02 mM, and the organic extract contained RA and parvifloron D at 0.29 and 3.13 mM, respectively. RA in aqueous solution permeated skin; however, in organic extract, this was not detected. Thus, aqueous extract was further studied and combined with benzophenone-4, which elevated the sun protection factor (SPF) by 19.49%. No significant cytotoxic effects were observed from the aqueous extract. The strain was used to determine a minimum inhibitory concentration (MIC) value of 10 µg.mL. The aqueous extract inhibited the activity of acetylcholinesterase by 59.14 ± 4.97%, and the IC value was 12.9 µg.mL. The association of the extract with a UV filter substantially elevated its SPF efficacy. Following the multiple bioactivities of the extract and its active substances, a finished product could be claimed as a multifunctional cosmeceutical with broad skin valuable effects, from UV protection to antiaging action.
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http://dx.doi.org/10.3390/ph13060120DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7345374PMC
June 2020

Using ordered mesoporous silica SBA-15 to limit cutaneous penetration and transdermal permeation of organic UV filters.

Int J Pharm 2019 Oct 19;570:118633. Epub 2019 Aug 19.

School of Pharmaceutical Sciences, University of Geneva & University of Lausanne, Switzerland. Electronic address:

Avobenzone (AVO), oxybenzone (OXY), and octyl methoxycinnamate (OMC), are widely used UV filters. The aim of this study was to investigate the effect of incorporation in mesoporous silica (SBA-15) on their cutaneous deposition and permeation. Stick formulations containing "free" and "incorporated" UV filters (SF1 and SF2, respectively) were prepared and characterized with respect to their physicochemical, thermal, and functional properties. Cutaneous delivery experiments using porcine skin with quantification by UHPLC-MS/MS, demonstrated that skin deposition of AVO and OXY after application of SF2 for 6 and 12 h was significantly lower than that from SF1 at each time-point (Student t-test, p < 0.05): e.g. OXY permeation across the skin was 30-, 12- and 1.5-fold lower after 6, 12 and 24 h, respectively, following application of SF2. Cutaneous biodistribution profiles of AVO and OXY to 800 µm evidenced a significant decrease in the amounts in the viable epidermis and dermis. In contrast, deposition of the more lipophilic OMC was not significantly different (p ˃ 0.05). In vitro photoprotective efficacy results demonstrated that adsorption/entrapment of UV filters enhanced the sun protection factor by 94%. In conclusion, SBA-15, an innovative mesoporous material, increased photoprotection by UV filters while reducing their cutaneous penetration and transdermal permeation.
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http://dx.doi.org/10.1016/j.ijpharm.2019.118633DOI Listing
October 2019

Impact of acid straightener's pH value in the hair fiber properties.

J Cosmet Dermatol 2020 Feb 26;19(2):508-513. Epub 2019 Jun 26.

Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.

Background: Acid straightener products are widely used, and it can cause changes in the hair shaft properties. The pH value of these products established by ANVISA (Brazil's National Health Surveillance Agency) as secure is above 2.0. However, the industries are interested in working at lower pH values in order to increase the straightening effect. Unfortunately, there are a lot of products in the market with pH value under the permitted.

Objective: Analyze two different pH values (1.0 and 2.0) of acid straightener formulation and the influence of this difference in the hair shaft properties. In order to provide information to professionals as cosmetologists, dermatologists, and hairdressers.

Methods: Combing and colorimetric analyses, tensile strength, differential scanning calorimetry (DSC), environmental scanning electron microscope (ESEM), and tryptophan content.

Results: The tresses treated at pH 1.0 had a better result in the straightening capacity, improving the combing test in 59.4%, while those at pH 2.0, only in 33.0% compared with virgin hair. However, the tensile strength, at pH 1.0 decreased by 16.0% and 9.0% to the pH 2.0. In addition, the tryptophan content was lower in the tresses treated with formulation at pH 1.0. The DSC analysis showed impairment in the straightened tresses. The images by ESEM, indicated a possible formation of a film around the fiber.

Conclusions: It was possible to conclude that the pH value interferes in the hair shaft properties. Tresses treated with pH 1.0 had more modifications than tresses treated with pH 2.0.
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http://dx.doi.org/10.1111/jocd.13006DOI Listing
February 2020

Another Reason for Using Caffeine in Dermocosmetics: Sunscreen Adjuvant.

Front Physiol 2019 3;10:519. Epub 2019 May 3.

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.

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 and 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, hydration, skin barrier and colorimetry were assessed in healthy subjects before and after skin treatment with the samples. The efficacy of the sunscreens was assessed , using PMMA plates and a spectrophotometer equipped with an integrating sphere; and by the determination of the sun protection factor (SPF). None of the formulations caused erythema or impaired the skin barrier function. The functional characterization showed higher SPF values for the caffeine formulation. The 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 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.
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http://dx.doi.org/10.3389/fphys.2019.00519DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6509748PMC
May 2019

Heat-damaged evaluation of virgin hair.

J Cosmet Dermatol 2019 Dec 12;18(6):1885-1892. Epub 2019 Mar 12.

Institute of Chemistry, University of São Paulo, São Paulo, Brazil.

Background: Hair-straightening treatments may involve the use of thermal devices, which potentially cause damages in the cuticle and cortex of the hair fibers. Particularly, the heat causes denaturation of the α-keratin and the degradation of the components of the hair cortex.

Objectives: The aim of this study was to evaluate the effect of heating on the cuticle and cortex of the Caucasian and Asian virgin hair by using heat iron flat.

Methods: The effects of the heating in the tresses of Caucasian and Asian virgin hair were analyzed by thermogravimetry/differential scanning calorimetry-Fourier transform infrared/mass spectrometry (TG/DSC-MS/FTIR), protein loss analysis (PLA), Fourier transform infrared (FTIR-ATR), and scanning electron microscope (SEM).

Results: TG/DSC-MS/FTIR results were: formation of the H O between 25-170°C and CO , SCO and H S from 200°C. Denaturation temperature = 237°C. Protein loss: Asian hair>Caucasian hair. Data presented statistically significant alterations, α = 5, P ≤ 0.05, n = 3. FTIR-ATR: changes in the secondary structural conformation of the protein of hair cuticle. SEM: heat caused damage to hair cuticle.

Conclusions: The results evidenced the importance of the control of temperature in the procedures involving heat. The damage caused by thermal devices showed be dependent of the ethnicity analyzed (Caucasian and Asian hair).
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http://dx.doi.org/10.1111/jocd.12892DOI Listing
December 2019

SPF enhancement provided by rutin in a multifunctional sunscreen.

Int J Pharm 2018 Dec 8;552(1-2):401-406. Epub 2018 Oct 8.

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, SP, Brazil. Electronic address:

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.
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http://dx.doi.org/10.1016/j.ijpharm.2018.10.015DOI Listing
December 2018

Is Vitamin D Transdermal Formulation Feasible? An Ex Vivo Skin Retention and Permeation.

AAPS PharmSciTech 2018 Jul 4;19(5):2418-2425. Epub 2018 Jun 4.

Department of Pharmacy, University of São Paulo (USP), Sao Paulo, Brazil.

Vitamin D supplementation is important to prevent and treat hypovitaminosis that is a worldwide public health issue. Most types of supplementation are by oral route or fortification foods. The alternative route must be investigated, as transdermal route, for people with fat malabsorption or other diseases that impair the absorption of vitamin D. This study focused on verifying the feasibleness of vitamin D skin retention and permeation with the presence of chemical penetration enhancers (soybean lecithin, isopropyl palmitate, propylene glycol, ethoxydiglycol, and cereal alcohol) at different pharmaceutical forms (gel and cream) through a human skin. The integrity of skin was evaluated by transepidermal water loss (TEWL) during the skin retention and permeation test. The combination of chemical penetration enhancers presented in cream did not compromise the skin, different from the gel that association of cereal alcohol and propylene glycol compromised the skin in 24 h. Gel formulation showed vitamin D detection at stratum corneum in 4 h and at epidermis and dermis in 24 h. Vitamin D demonstrated an affinity with the vehicle in the cream formulation and was detected at the skin surface. No active was found at receptor fluid for both formulations. In conclusion, the vitamin D did not indicate feasibleness for transdermal use probably due to its physical-chemical characteristics such as high lipophilicity since it was not permeated through a human skin. Nevertheless, the transdermal route should be continuously investigated with less lipophilic derivates of vitamin D and with different combination of penetration enhancers.
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http://dx.doi.org/10.1208/s12249-018-1065-5DOI Listing
July 2018

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

J Photochem Photobiol B 2018 Aug 26;185:46-49. Epub 2018 May 26.

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, SP, Brazil. Electronic address:

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.
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http://dx.doi.org/10.1016/j.jphotobiol.2018.05.026DOI Listing
August 2018

Safety and Antioxidant Efficacy Profiles of Rutin-Loaded Ethosomes for Topical Application.

AAPS PharmSciTech 2018 May 29;19(4):1773-1780. Epub 2018 Mar 29.

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl. 15, São Paulo, SP, 05508-900, Brazil.

Topical application of dermocosmetics containing antioxidant and/or the intake of antioxidants through diet or supplementation are remarkable tools in an attempt to slow down some of the harmful effects of free radicals. Rutin is a strong antioxidant compound used in food and pharmaceutical industries. It was established that rutin presents a low skin permeation rate, a property that could be considered an inconvenience to the satisfactory action for a dermocosmetic formulation to perform its antioxidant activity onto the skin. Therefore, it is indispensable to improve its delivery, aiming at increasing its antioxidant capacity in deeper layers of the epidermis, being a possibility to associate the rutin to liposomal vesicles, such as ethosomes. Thus, in this work, the pre-clinical safety of rutin-loaded ethosomes was investigated employing an in vitro method, and the clinical safety and efficacy were also assessed. Rutin-loaded ethosomes were efficaciously obtained in a nanoscale dimension with a relevant bioactive compound loading (80.2%) and provided antioxidant in vitro activity in comparison with the blank sample. Pre-clinical and clinical safety assays assured the innocuous profile of the rutin-loaded ethosomes. The ethosomes containing the bioactive compound accomplished a more functional delivery system profile, since in the tape stripping assay, the deeper layers presented higher rutin amounts than the active delivered in its free state. However, the ex vivo antioxidant efficacy test detected no positive antioxidant activity from the rutin-loaded ethosomes, even though the in vitro assay demonstrated an affirmative antioxidant action.
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http://dx.doi.org/10.1208/s12249-018-0994-3DOI Listing
May 2018

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

Drug Dev Ind Pharm 2017 Feb 13;43(2):246-256. Epub 2016 Oct 13.

a Department of Pharmacy, Faculty of Pharmaceutical Sciences , University of São Paulo , São Paulo , Brasil.

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.
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http://dx.doi.org/10.1080/03639045.2016.1236809DOI Listing
February 2017

Optical coherence tomography to evaluate the effects of oxidative hair dye on the fiber.

Skin Res Technol 2016 Nov 21;22(4):430-436. Epub 2016 Jan 21.

Laboratory of Cosmetology, Pharmaceutical Sciences School, University of São Paulo, São Paulo, Brazil.

Background/purpose: Oxidative hair dyes can damage the hair, since these chemical procedures are involved to change the fiber structure and therefore changes in their mechanical and surface properties. Evaluate and compare the effect of the two colors of oxidative hair dye emulsions on Caucasian hair. This research analyzed the Dark brown hair untreated (I); Dark brown hair treated with light brown dye (II); Dark brown hair treated with light blond dye (III); Light blond hair untreated (IV); Light blond hair treated with light brown dye (V); Light blond hair treated with light blond dye (VI) on Caucasian hair.

Methods: The hair samples were submitted to breaking strength, color, and optical coherence tomography (OCT) analysis.

Results: For the breaking strength assay no presented statistically significant differences between treatments. The parameters of color and brightness can differ in some hair dye formulations, but also the hair type can respond differently. The OCT images of the sample I and IV was possible observed, clearly Medulla and Cortex, which was not observed clearly after treatment with both oxidative hair dye colors.

Conclusion: Based on the results, the oxidative hair dyes increased alteration in color and ultrastructure of hair.
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http://dx.doi.org/10.1111/srt.12283DOI Listing
November 2016

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

Colloids Surf B Biointerfaces 2016 Apr 18;140:531-537. Epub 2015 Nov 18.

Laboratory of Cosmetology, Department of Pharmacy, School of Pharmaceutical Sciences of University of São Paulo, São Paulo, SP, Brazil.

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.
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http://dx.doi.org/10.1016/j.colsurfb.2015.11.031DOI Listing
April 2016

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

Eur J Pharm Sci 2016 Jan 30;81:1-9. Epub 2015 Sep 30.

Laboratory of Cosmetology, Department of Pharmacy, School of Pharmaceutical Sciences of University of São Paulo, São Paulo, SP, Brazil.

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.
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http://dx.doi.org/10.1016/j.ejps.2015.09.016DOI Listing
January 2016

Functional photostability and cutaneous compatibility of bioactive UVA sun care products.

J Photochem Photobiol B 2015 Jul 20;148:154-159. Epub 2015 Apr 20.

Department of Pharmacy, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl. 15, Conjunto das Químicas, Cidade Universitária, 05508-900 São Paulo, SP, Brazil.

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.
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http://dx.doi.org/10.1016/j.jphotobiol.2015.04.007DOI Listing
July 2015

Development of ciclopirox olamine topical formulations: evaluation of drug release, penetration and cutaneous retention.

Pharm Dev Technol 2015 Mar 29;20(2):197-203. Epub 2013 Nov 29.

Faculdade de Ciências Farmacêuticas da, Universidade de São Paulo , São Paulo, SP , Brazil.

With the aim of reducing system absorption and consequently, the side effects, and simultaneously select a penetration enhancing, three topical formulations with 0.5% ciclopirox olamine (CO) and 15% of propylene glycol (PG), ethoxydiglycol or oleic acid were developed and evaluated regarding the skin penetration and cutaneous retention of the drug using Franz diffusion cells. Release experiments were performed through synthetic membrane while dermatomed pig ear skin was used to evaluate CO skin penetration and skin retention. Retention studies were carried out applying tape stripping method and dosing CO in stratum corneum and in epidermis and dermis. A HPLC method was validated for quantifying CO. All formulations tested with synthetic membrane presented no retention of the drug. Permeation data suggested that there was no systemic absorption of ciclopirox olamine from the studied formulations, even when the skin penetration enhancers were applied. Higher concentrations of the drug were found in the stratum corneum (SC) and also in epidermis and dermis, for all of the developed formulations. The addition of enhancers improved the penetration and cutaneous retention of CO, and propylene glycol promoted higher concentrations in epidermis and dermis, probably because its cumulative effect on the skin and by an efficient solvent power.
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http://dx.doi.org/10.3109/10837450.2013.860544DOI Listing
March 2015

Efficacy of Punica granatum L. hydroalcoholic extract on properties of dyed hair exposed to UVA radiation.

J Photochem Photobiol B 2013 Mar 5;120:142-7. Epub 2013 Jan 5.

School of Pharmaceutical Sciences of University of São Paulo, 580 Prof. Lineu Prestes Avenue, Bl-13/15, São Paulo, SP, Brazil.

The solar radiation promotes color fading of natural and dyed hair by free radical generation, which oxidize the pigments, and it has been proposed the incorporation of antioxidants in order to reduce the alterations of hair color. Due to its high content of polyphenols and tannins, which are potent antioxidants, the hydroalcoholic extract of Punica granatum L. (pomegranate) was used in this research. Hair care formulations containing pomegranate extract were applied to red dyed hair tresses, and these were exposed to UVA radiation. Non-ionic silicone emulsion presenting color protection properties were also used for comparison purpose between the results obtained with different treatments, including silicone in combination with the pomegranate extract. The pomegranate extract at 5.0% and 10.0%w/w was effective in preventing the hair color fading in 37.6% and 60.8%, respectively, but the association of hydroalcoholic extract and non-ionic silicone emulsion is not encouraged. Mechanical properties were not affected by UVA radiation, since significant differences in breaking strength were not observed. Considering the conditions which the tresses have been exposed, it was concluded that the pomegranate extract at 10.0% w/w in hair care formulations are effective in reducing color fading of red dyed hair.
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http://dx.doi.org/10.1016/j.jphotobiol.2012.12.011DOI Listing
March 2013

Optimization of primaquine diphosphate tablet formulation for controlled drug release using the mixture experimental design.

Pharm Dev Technol 2013 Sep-Oct;18(5):1247-54. Epub 2012 Jun 7.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo, Brazil.

A tablet formulation based on hydrophilic matrix with a controlled drug release was developed, and the effect of polymer concentrations on the release of primaquine diphosphate was evaluated. To achieve this purpose, a 20-run, four-factor with multiple constraints on the proportions of the components was employed to obtain tablet compositions. Drug release was determined by an in vitro dissolution study in phosphate buffer solution at pH 6.8. The polynomial fitted functions described the behavior of the mixture on simplex coordinate systems to study the effects of each factor (polymer) on tablet characteristics. Based on the response surface methodology, a tablet composition was optimized with the purpose of obtaining a primaquine diphosphate release closer to a zero order kinetic. This formulation released 85.22% of the drug for 8 h and its kinetic was studied regarding to Korsmeyer-Peppas model, (Adj-R(2) = 0.99295) which has confirmed that both diffusion and erosion were related to the mechanism of the drug release. The data from the optimized formulation were very close to the predictions from statistical analysis, demonstrating that mixture experimental design could be used to optimize primaquine diphosphate dissolution from hidroxypropylmethyl cellulose and polyethylene glycol matrix tablets.
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http://dx.doi.org/10.3109/10837450.2012.693508DOI Listing
February 2014

Ultraviolet radiation protection: current available resources in photoprotection.

An Bras Dermatol 2011 Jul-Aug;86(4):732-42

University of Sao Paulo School of Pharmaceutical Sciences, Brasil.

Ultraviolet radiation can damage the DNA, cause immunosuppression, chemical and histological alterations in the epidermis, early photoaging, cataracts and carcinogenesis, among others. Photoprotection prevents these and other harmful effects of ultraviolet radiation. Sunscreens, protective clothing, proper accessories and safe sun exposure are essential photoprotection tools. The main forms of photoprotection are presented and discussed in this article, including sunscreens containing organic and inorganic filters, the assessment of their efficacy and current developments on the topic.
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http://dx.doi.org/10.1590/s0365-05962011000400016DOI Listing
February 2012

Rubus rosaefolius extract as a natural preservative candidate in topical formulations.

AAPS PharmSciTech 2011 Jun 4;12(2):732-7. Epub 2011 Jun 4.

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Brazil.

Even though the synthetic preservatives may offer a high antimicrobial efficacy, they are commonly related to adverse reactions and regarded as having potentially harmful effects caused by chronic consumption. The development of natural preservatives provides a way of reducing the amount of synthetic preservatives normally used in pharmaceutical and cosmetic preparations. In addition, these agents have less toxic effects and represent a possible natural and safer alternative of the preservatives. The purpose of this research was to evaluate the Rubus rosaefolius Smith extract efficiency as a natural preservative in base formulations. Of the extract, 0.2% (w/w) was assayed for its effectiveness of antimicrobial protection in two different base formulations (emulsion and gel). The microbial challenge test was performed following the standard procedures proposed by The United States Pharmacopoeia 33nd, European Pharmacopoeia 6th, Japanese Pharmacopoeia 15th, and the Cosmetics, Toiletries, and Fragrance Association using standardized microorganisms. The results demonstrated that R. rosaefolius extract at the studied concentration reduced the bacterial inocula, satisfying the criterion in all formulations, even though it was not able to present an effective preservative behavior against fungi. Thus, the investigation of new natural substances with preservative properties that could be applied in pharmaceutical and cosmetic products is relevant due to the possibility of substituting or decreasing the concentration of synthetic preservatives, providing a way for the development of safer formulas for the use of consumers.
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http://dx.doi.org/10.1208/s12249-011-9635-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3134679PMC
June 2011

Prospective ultramorphological characterization of human hair by optical coherence tomography.

Skin Res Technol 2009 Nov;15(4):440-3

Laboratory of Cosmetology, Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.

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.

Methods: In this work, we used the optical coherence tomography (OCT) technique to produce in vitro transversal section-images of human hair. We also compared the OCT signal before and after chemical treatment with an 18% w/w ammonium thioglycolate solution.

Results: The mean diameter of the medulla was 29+/-7 microm and the hair diameter was 122+/-16 microm in our samples of standard Afro-ethnic hair. A three-dimensional (3D) image was constructed starting from 601 cross-sectional images (slices). Each slice was taken in steps of 6.0 microm at eight frames per second, and the entire 3D image was constructed in 60 s.

Conclusion: It was possible to identify, using the A-scan protocol, the principal structures: the cuticle, cortex and medulla. After chemical treatment, it was not possible to identify the main structures of hair fiber due to index matching promoted by deleterious action of the chemical agent.
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http://dx.doi.org/10.1111/j.1600-0846.2009.00386.xDOI Listing
November 2009

Hydrating effects of moisturizer active compounds incorporated into hydrogels: in vivo assessment and comparison between devices.

J Cosmet Dermatol 2009 Mar;8(1):32-9

Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, SP, Brazil.

Background: Water is an important factor on the appearance and function of the skin and, when dehydrated, it becomes rough and flaky. The measurement of stratum corneum hydration is widely employed to verify the moisture effect of topical products.

Aims: This study has evaluated in vivo the stratum corneum hydration, by the electrical measurements of skin, after treatment with different moisturizers presented in gel base. MoistureMeter and Corneometer were used as bio-instruments. Urea, the herbal extract (Imperata cylindrical), the NMF components and the carbohydrate derivate compound (xylityglucoside, anhydroxylitol, and xylitol) were used as the active substances.

Methods: The study protocol was carried out according to the three-factor factorial design. The gels were applied on both forearms of eight female volunteers. However, each volunteer had one untreated skin area as the skin moisture control. The electrical capacitance of the skin was measured by both instruments in different times: after application (0 time), 30, 60, 120, 240 and 360 min.

Results: Gel base, gel containing herbal extract, and gel containing NMF components statistically have equal moisture effect measurements, according to both bio-instruments. However, the values obtained for urea, carbohydrate derivate compound, and untreated skin (control) have statically different results in both devices.

Conclusion: The gel containing urea and the carbohydrate derivate compound gel have promoted the most intense moisture effect compared with the other formulations. The measurements of hydration between the devices generated different absolute values; however, the statistical analysis has shown similar precision among the measurements.
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http://dx.doi.org/10.1111/j.1473-2165.2009.00421.xDOI Listing
March 2009

Influence of urea, isopropanol, and propylene glycol on rutin in vitro release from cosmetic semisolid systems estimated by factorial design.

Drug Dev Ind Pharm 2009 Mar;35(3):272-82

Laboratory of Cosmetology, Department of Pharmacy, School of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo, Brazil.

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 (microg/cm(2).h); apparent permeability coefficient (cm/h); rutin amount released (microg/cm(2)); 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 microg/cm(2).h; apparent permeability coefficient = 7.01 +/- 0.572 cm/h; rutin amount released = 648.80 +/- 53.01 microg/cm(2); and liberation enhancement factor = 1.21 +/- 0.07.
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http://dx.doi.org/10.1080/03639040802277664DOI Listing
March 2009
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