Orientador: Marcos Antonio Corrêa / Banca: Bruna Galdorfini Chiari Andréo / Banca: Marilisa Guimarães Lara / Resumo: O mercado brasileiro de cosméticos está entre os mais importantes do mundo. Neste mercado, os produtos antienvelhecimento apresentam forte tendência de crescimento e dentre esses produtos se destacam os antioxidantes, tais como os compostos fenólicos que estão amplamente distribuídos no reino vegetal e em micro-organismos. Os ácidos cinâmicos fazem parte desses compostos, sendo o ácido ferúlico um dos seus representantes. Segundo a literatura, este ácido apresenta potencial antioxidante e propriedades anticancerígenas, anti-inflamatórias e antimicrobianas. O objetivo deste trabalho foi avaliar a eficácia in vitro e a citotoxicidade do AF para sua incorporação em uma emulsão cosmética. Foram realizados estudos da atividade antioxidante através de duas metodologias analíticas (DPPH e ABTS), da avaliação da atividade antimicrobiana, da atividade inibidora da tirosinase (despigmentante), além da avaliação do potencial citotóxico, utilizando duas linhagens de células (HaCat e HDFa), do desenvolvimento de emulsões, da validação de uma metodologia analítica para quantificação do ácido ferúlico por CLAE. Também foi realizado estudo de estabilidade acelerada e ensaios de liberação, permeação e retenção in vitro. O ácido ferúlico apresentou um IC50 = 12,21 μg.mL-1 para o radical DPPH e de 2,84 μg.mL-1 para o radical ABTS. Já no ensaio despigmentante, o ácido ferúlico apresentou um IC50 = 2,89 μg.mL-1. Na avaliação da atividade antimicrob... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: The Brazilian cosmetic market is among the most important in the world. In this market, anti-aging products have strong growth trend and among these products stand antioxidants such as phenolic compounds that are widely distributed in the plant kingdom and micro-organisms. Cinnamic acids are part of these compounds, ferulic acid being one of their representatives. According to the literature, this acid has antioxidant potential and anticancer, anti-inflammatory and antimicrobial properties. The objective of this work has been to evaluate the in vitro efficacy and the cytotoxicity of FA for its incorporation in a cosmetic emulsion. Studies of antioxidant activity through two analytical methodologies (DPPH and ABTS), tyrosinase inhibitory activity (depigmentation), antimicrobial activity, cytotoxic potential evaluation using two cell lines (Hacat and HDFa), validation of an analytical methodology for the quantification of ferulic acid by HPLC and release, permeation and retention in vitro. Ferulic acid showed an IC50 = 12,21 μg.mL-1 for DPPH radical and an IC50 = 2,84 μg.mL-1 for ABTS radical. In the evaluation of the antimicrobial activity, concentrations varying from 0,75 to 2,0 mg.mL-1 of the ferulic acid were required to inhibit the growth of the bacteria tested in this study. Already in the depigmenting assay, ferulic acid presented an IC50 = 2,89 μg.mL-1. From the cytotoxicity studies, it has been verified that the ferulic acid is not cytotoxic in the concentrations used ... (Complete abstract click electronic access below) / Mestre

Introdução: A luz intensa pulsada(LIP) tem sido muito utilizada no tratamento do fotoenvelhecimento sem completo conhecimento de seu mecanismo de ação. Métodos: Foram acompanhados 26 pacientes apresentando fotoenvelhecimento grau II-III (GLOGAU, 1994), os quais foram submetidas à avaliação clínica , histológica e imunoistoquímica 6 e 12 meses após o término do tratamento com LIP. Foram realizadas cinco sessões com intervalos de trinta dias. Além da quantificação histomorfométrica das fibras colágenas e elásticas na derme, foram avaliados CD1, CD4, CD8 e ICAM-1. Resultados: Após 6 meses houve melhora clínica moderada e intensa em 76,92% dos casos e a nota média de satisfação foi 8,57 correspondendo à melhora moderada. Após 12 meses do término do tratamento observou-se que 51,52% das pacientes apresentaram uma melhora clínica moderada em relação à clínica inicial. Os efeitos colaterais foram eritema (11/26), edema (10/26), ardência (7/26) e crostas (8/26). A quantificação das fibras colágenas mostrou aumento médio de 51,33% proporção média de fibra colágena na derme após 6 meses de tratamento e o aumento em relação a 12 meses do término do tratamento foi 30,17%; as fibras elásticas mostraram aumento de 44,13% após 6 meses e aumento de 143,19% após 12 meses do término do tratamento. Na análise imunoistoquímica não houve alteração de CD1 e CD8. Em relação ao CD4 houve redução significante após 12 meses do término do tratamento. Quanto ao ICAM-1 houve aumento em 6 meses com retorno aos níveis normais após 12 meses do término do tratamento. Conclusão: A melhora clínica observada foi comprovada pelo estudo histopatológico, que mostrou aumento das fibras colágenas e elásticas na derme. Após 12 meses do término do tratamento observou-se discreta redução do aspecto clínico da pele correlacionado ao histopatológico. Poucos efeitos colaterais foram observados, sendo todos reversíveis. Desta forma, a LIP constitui boa opção de tratamento para o fotoenvelhecimento cutâneo, sendo uma técnica não ablativa, segura e eficaz. / Introduction: The intense pulsed light has been used in the treatment of photoaging without full knowledge of its mechanism of action. Material and Methods: 26 patients were followed-up presenting photoaging grade II-III (GLOGAU, 1994), who were submitted to clinical evaluation, histological and immunohistochemistry 6 and 12 months after the treatment termination with LIP. Five sessions were made with 30-day intervals. In addition to histomorphometric quantification of collagen and elastic fibers in the dermis, CD1, CD4, CD8 and ICAM-1 were evaluated. Results: After 6 months there were moderate and intense clinical improvement on 76.92% of the cases and the mean score of satisfaction was 8.57 corresponding to moderate improvement. After 12 months of the treatment termination, it was observed that 51.52% of the patients presented a moderate clinical improvement in relation to initial clinic. The side effects were erythema (11/26), edema (10/26), burning (7/26) and crusts (8/26). The quantification of collagen fibers has shown mean increase of 51.33% in the dermis after 6 months of treatment and the increase regarding to 12 months of the treatment termination was of 30.17%; the elastic fibers has shown an increase of 44.13% after 6 months and increase of 143.19% after 12 months of the treatment termination. In the immunohistochemistry analysis there was no alteration of CD1 and CD8. In relation to CD4, there was a significant reduction after 12 months of treatment termination. Regarding the ICAM-1, there was an increase in 6 months with return to normal levels after 12 months of treatment termination. Conclusion: The observed clinical improvement was verified by the histopathologic study, which showed increase in the elastic and collagen fibers in the dermis. After 12 months of treatment termination, it was observed a discrete reduction of clinical aspect of skin correlated to histopathology. A few side effects were observed, being all reversible. Thus, LIP constitutes good option of treatment for skin photoageing, being a non-ablative, safe and effective technique.

Made available in DSpace on 2014-07-29T15:25:24Z (GMT). No. of bitstreams: 1 tese ana lucia zampieri.pdf: 1190339 bytes, checksum: 6544c1ca9cec719053f0ced26568005b (MD5) Previous issue date: 2009-12-16 / Isoflavones are phytoestrogens that have biological activities such as estrogenic and inhibiting enzymes that regulate the cell cycle, and for topic application it is highlighted antioxidant and anticancer activities. Amongst isoflavones, genistein shows the greatest biological activity, however, its low hydrosolubility damages incorporation in topic vehicles and passive permeation. Therefore, development of particulated nanocarrier systems, such as nanocapsules, aiming to increase genistein biological activities and make topic administration possible, became this work s objective. To do so, PLA nanocapsules containing genistein were prepared by interfacial polymer deposition method, then characterized, and their 90 days stability was evaluated. Later, free and nanoencapsulated genistein were incorporated into semi-solid formulations (gel and emulsion) and evaluated by in vitro models using classical Franz-type diffusion cells, to measure its ability to modulate swine skin and synthetic membranes penetration. Nanocapsules average diameter was 138,5 nm (DP± 2,95) and PDI found was 0,126 (DP± 0.03). After separation of free genistein, the drug was quantified by HPLC and showed 89,63% (DP±2,27) encapsulation efficiency, followed by loss by leaking to 63,80% (DP±11,26) in 90 days. Permeation tests demonstrated that gel formulation containing nanoencapsulated genistein presented the greatest permeated concentration, and there was significant difference for all tested formulations and similarity only between genistein quantity reminiscent in the dosage form of formulations containing gel and emulsion, as well as drug quantities retained in the skin of gel and emulsion formulations containing genistein. Nanoencapsulated forms kinetic parameters showed the greatest correlation coefficient for kinetic of zero order model, indicating that flow didn t depend on its concentration. Nanoencapsulated genistein concentrations permeation across synthetic and swine skin presented significant difference depending on time. Thus, the study performed showed that the polymeric system developed presents great potential for application as genistein nanocarrier in biological systems / As isoflavonas são fitoestrógenos que desempenham atividades biológicas como estrogênica e inibidora de enzimas reguladoras do ciclo celular, sendo para aplicação tópica ressaltada a atividade antioxidante e antitumoral. Dentre as isoflavonas, a genisteína apresenta atividade biológica mais pronunciada, entretanto, sua baixa hidrossolubilidade dificulta tanto sua incorporação em bases para administração tópica na pele, quanto sua permeação passiva. Assim, o desenvolvimento de sistemas nanocarreadores particulados, como as nanocápsulas, com o intuito de acentuar suas atividades biológicas e possibilitar sua administração sobre a pele, tornou-se o objetivo desse trabalho. Para tanto, nanocápsulas de PLA contendo genisteína foram preparadas pelo método de deposição interfacial do polímero pré-formado, caracterizadas e avaliadas quanto à estabilidade por 90 dias. Posteriormente genisteína livre e nanoencapsulada foi incorporada em formulações tópicas semi-sólidas (gel e emulsão) e avaliadas em modelos in vitro, quanto à habilidade de modularem a penetração na pele de suíno e membrana sintética. O diâmetro médio das nanocapsulas foi 138,5 nm (DP± 2,95) e índice de polidispersibilidade de 0,126 (DP± 0.03). Após separação da genisteína livre e nanoencapsulada, o fármaco foi quantificado por cromatografia líquida de alta eficiência e demonstrou 89,63% (DP±2,27) de eficiência de encapsulação, seguido de perda por vazamento para 63,80% (DP±11,26) em 90 dias. Os testes de permeação demonstraram que a formulação em gel contendo genisteína nanoencapsulada apresentou maior concentração permeada, havendo diferença significativa para todas as formulações testadas e semelhança, apenas entre a quantidade de GEN remanescente na forma farmacêutica das formulações contendo NC em gel e emulsão, bem como, entre as quantidades de fármaco retido na pele das formulações contendo genisteína livre em gel e emulsão. Os parâmetros cinéticos das formas nanoencapsuladas demonstraram maior coeficiente de correlação para o modelo cinético de ordem zero, indicando que o fluxo não dependeu de sua concentração. As concentrações de genisteína nanoencapsulada permeada através da membrana sintética e pele suína apresentaram diferença significativa havendo dependência com o tempo. Dessa forma, o estudo realizado demonstrou que o sistema polimérico desenvolvido apresenta grande potencial para aplicação como nanocarreador da genisteína em sistemas biológicos

Introdução: A luz intensa pulsada(LIP) tem sido muito utilizada no tratamento do fotoenvelhecimento sem completo conhecimento de seu mecanismo de ação. Métodos: Foram acompanhados 26 pacientes apresentando fotoenvelhecimento grau II-III (GLOGAU, 1994), os quais foram submetidas à avaliação clínica , histológica e imunoistoquímica 6 e 12 meses após o término do tratamento com LIP. Foram realizadas cinco sessões com intervalos de trinta dias. Além da quantificação histomorfométrica das fibras colágenas e elásticas na derme, foram avaliados CD1, CD4, CD8 e ICAM-1. Resultados: Após 6 meses houve melhora clínica moderada e intensa em 76,92% dos casos e a nota média de satisfação foi 8,57 correspondendo à melhora moderada. Após 12 meses do término do tratamento observou-se que 51,52% das pacientes apresentaram uma melhora clínica moderada em relação à clínica inicial. Os efeitos colaterais foram eritema (11/26), edema (10/26), ardência (7/26) e crostas (8/26). A quantificação das fibras colágenas mostrou aumento médio de 51,33% proporção média de fibra colágena na derme após 6 meses de tratamento e o aumento em relação a 12 meses do término do tratamento foi 30,17%; as fibras elásticas mostraram aumento de 44,13% após 6 meses e aumento de 143,19% após 12 meses do término do tratamento. Na análise imunoistoquímica não houve alteração de CD1 e CD8. Em relação ao CD4 houve redução significante após 12 meses do término do tratamento. Quanto ao ICAM-1 houve aumento em 6 meses com retorno aos níveis normais após 12 meses do término do tratamento. Conclusão: A melhora clínica observada foi comprovada pelo estudo histopatológico, que mostrou aumento das fibras colágenas e elásticas na derme. Após 12 meses do término do tratamento observou-se discreta redução do aspecto clínico da pele correlacionado ao histopatológico. Poucos efeitos colaterais foram observados, sendo todos reversíveis. Desta forma, a LIP constitui boa opção de tratamento para o fotoenvelhecimento cutâneo, sendo uma técnica não ablativa, segura e eficaz. / Introduction: The intense pulsed light has been used in the treatment of photoaging without full knowledge of its mechanism of action. Material and Methods: 26 patients were followed-up presenting photoaging grade II-III (GLOGAU, 1994), who were submitted to clinical evaluation, histological and immunohistochemistry 6 and 12 months after the treatment termination with LIP. Five sessions were made with 30-day intervals. In addition to histomorphometric quantification of collagen and elastic fibers in the dermis, CD1, CD4, CD8 and ICAM-1 were evaluated. Results: After 6 months there were moderate and intense clinical improvement on 76.92% of the cases and the mean score of satisfaction was 8.57 corresponding to moderate improvement. After 12 months of the treatment termination, it was observed that 51.52% of the patients presented a moderate clinical improvement in relation to initial clinic. The side effects were erythema (11/26), edema (10/26), burning (7/26) and crusts (8/26). The quantification of collagen fibers has shown mean increase of 51.33% in the dermis after 6 months of treatment and the increase regarding to 12 months of the treatment termination was of 30.17%; the elastic fibers has shown an increase of 44.13% after 6 months and increase of 143.19% after 12 months of the treatment termination. In the immunohistochemistry analysis there was no alteration of CD1 and CD8. In relation to CD4, there was a significant reduction after 12 months of treatment termination. Regarding the ICAM-1, there was an increase in 6 months with return to normal levels after 12 months of treatment termination. Conclusion: The observed clinical improvement was verified by the histopathologic study, which showed increase in the elastic and collagen fibers in the dermis. After 12 months of treatment termination, it was observed a discrete reduction of clinical aspect of skin correlated to histopathology. A few side effects were observed, being all reversible. Thus, LIP constitutes good option of treatment for skin photoageing, being a non-ablative, safe and effective technique.

Aging can be described as an extremely complex occurrence from which no organism can be excluded. Intrinsic and extrinsic aging make out the two components of skin aging and they differ on the macromolecular level while sharing specific molecular characteristics which include elevated levels of reactive oxygen species (ROS) and matrix metalloproteinase (MMP) while collagen synthesis decreases. The skin functions as a protective barrier against the harsh environment and is essential for regulating body temperature. The stratum corneum (SC) is responsible for the main resistance to the penetration of most compounds; nevertheless the skin represents as an appropriate target for delivery. The target site for anti-aging treatment includes the epidermal and dermal layers of the skin. Calendula oil and L-carnitine L-tartrate was utilised as the cosmeceutical actives as they can be classified as a mixed category of compounds/products that lie between cosmetics and drugs. Both show excellent properties which can prove valuable during anti-aging treatment, whether it is due to the scavenging of ROS (calendula oil), moisturising effects (calendula oil and L-carnitine L-tartrate) or the improvement of the skin turnover rate (L-carnitine L-tartrate). The Pheroid™ delivery system can enhance the absorption of a selection of active ingredients. The aim of this study was to determine whether the Pheroid™ delivery system will enhance the flux and/or delivery of the named actives to the target site by performing Franz cell diffusion studies over an 8 h period, followed by tape stripping experiments. The Pheroid™ results of the actives were compared to the results obtained when 1 00 % calendula oil was applied and the L-carnitine L-tartrate was dissolved in phosphate buffer solution (PBS), respectively. In the case of calendula oil only a qualitative gas chromatography mass spectrometry (GC/MS) method could be employed. No calendula oil was observed to permeate through the skin, but linoleic acid (marker compound) was present in the epidermis and dermis layers. Components in the Pheroid™ delivery system hampered the results as the marker compound identified is a fundamental component of the Pheroid™, making it difficult to determine whether or not the Pheroid™ delivery system enhanced calendula oil's penetration. The aqueous solubility and log D partition coefficient of L-carnitine L-tartrate was determined. Inspection of the log D value of -1.35 indicated that the compound is unfavourable to penetrate the skin, whereas the aqueous solubility of 16.63 mg/ml in PBS at a temperature of 32º C indicated favourable penetration. During the Franz cell diffusion and tape stripping studies it was determined by liquid chromatography mass spectrometry (LC/MS) that carnitine may be inherent to human skin. Pheroid™ enhanced the flux (average of 0.0361 µg/cm2.h, median of 0.0393 µg/cm2.h) of the L-carnitine L-tartrate when compared to PBS (average of 0.0180 µg/cm2.h, median of 0.0142 µg/cm2.h ) for the time interval of 2 -8 h. The PBS was more effective in delivering the active to the target site (0.270 µg/ml in the epidermis and 2.403 µg/ml in the dermis) than Pheroid™ (0.111 µg/ml and 1.641 µg/ml in the epidermis and dermis respectively). Confocal laser scanning microscopy (CLSM) confirmed the entrapment of L-carnitine L-tartrate in the Pheroid™ vesicle, while in the case of calendula oil it was impossible to differentiate between the oil and the Pheroid™ components. / Thesis (M.Sc. (Pharmaceutics))--North-West University, Potchefstroom Campus, 2009.

Aging can be described as an extremely complex occurrence from which no organism can be excluded. Intrinsic and extrinsic aging make out the two components of skin aging and they differ on the macromolecular level while sharing specific molecular characteristics which include elevated levels of reactive oxygen species (ROS) and matrix metalloproteinase (MMP) while collagen synthesis decreases. The skin functions as a protective barrier against the harsh environment and is essential for regulating body temperature. The stratum corneum (SC) is responsible for the main resistance to the penetration of most compounds; nevertheless the skin represents as an appropriate target for delivery. The target site for anti-aging treatment includes the epidermal and dermal layers of the skin. Calendula oil and L-carnitine L-tartrate was utilised as the cosmeceutical actives as they can be classified as a mixed category of compounds/products that lie between cosmetics and drugs. Both show excellent properties which can prove valuable during anti-aging treatment, whether it is due to the scavenging of ROS (calendula oil), moisturising effects (calendula oil and L-carnitine L-tartrate) or the improvement of the skin turnover rate (L-carnitine L-tartrate). The Pheroid™ delivery system can enhance the absorption of a selection of active ingredients. The aim of this study was to determine whether the Pheroid™ delivery system will enhance the flux and/or delivery of the named actives to the target site by performing Franz cell diffusion studies over an 8 h period, followed by tape stripping experiments. The Pheroid™ results of the actives were compared to the results obtained when 1 00 % calendula oil was applied and the L-carnitine L-tartrate was dissolved in phosphate buffer solution (PBS), respectively. In the case of calendula oil only a qualitative gas chromatography mass spectrometry (GC/MS) method could be employed. No calendula oil was observed to permeate through the skin, but linoleic acid (marker compound) was present in the epidermis and dermis layers. Components in the Pheroid™ delivery system hampered the results as the marker compound identified is a fundamental component of the Pheroid™, making it difficult to determine whether or not the Pheroid™ delivery system enhanced calendula oil's penetration. The aqueous solubility and log D partition coefficient of L-carnitine L-tartrate was determined. Inspection of the log D value of -1.35 indicated that the compound is unfavourable to penetrate the skin, whereas the aqueous solubility of 16.63 mg/ml in PBS at a temperature of 32º C indicated favourable penetration. During the Franz cell diffusion and tape stripping studies it was determined by liquid chromatography mass spectrometry (LC/MS) that carnitine may be inherent to human skin. Pheroid™ enhanced the flux (average of 0.0361 µg/cm2.h, median of 0.0393 µg/cm2.h) of the L-carnitine L-tartrate when compared to PBS (average of 0.0180 µg/cm2.h, median of 0.0142 µg/cm2.h ) for the time interval of 2 -8 h. The PBS was more effective in delivering the active to the target site (0.270 µg/ml in the epidermis and 2.403 µg/ml in the dermis) than Pheroid™ (0.111 µg/ml and 1.641 µg/ml in the epidermis and dermis respectively). Confocal laser scanning microscopy (CLSM) confirmed the entrapment of L-carnitine L-tartrate in the Pheroid™ vesicle, while in the case of calendula oil it was impossible to differentiate between the oil and the Pheroid™ components. / Thesis (M.Sc. (Pharmaceutics))--North-West University, Potchefstroom Campus, 2009.

Orientador: Man Chin Chung / Coorientador: Marcos Antonio Corrêa / Resumo: Eritemas, inflamação, fotoenvelhecimento e câncer de pele são os problemas mais comuns causadas por radiação UV, estratificada em 3 regiões do espectro de luz: UVA (320-400 nm), UVB (280-320 nm) e UVC (200-280 nm). As radiações UVA e UVB são as mais nocivas à pele, visto que a radiação UVC é retida pela camada de ozônio e só é utilizada artificialmente como germicida. A incidência da radiação UVA sobre a pele induz a formação de EROS (espécies reativas de oxigênio) que afeta de forma indireta o DNA humano podendo provocar câncer de pele. A radiação UVB afeta diretamente as bases pirimidínicas das moléculas de DNA dificultando o seu reparo, aumentando a chances do indivíduo desenvolver o câncer de pele. Para minimizar e prevenir os danos causados pela radiação UV à pele foram desenvolvidos os filtros solares, dividido entre orgânicos e inorgânicos que apresentam capacidade de bloquear (inorgânicos) ou absorver (orgânicos) a radiação UV incidente na pele. Entre os filtros orgânicos estão as benzofenonas e os cinamatos. Para auxiliar no efeito fotoprotetor dos filtros, a associação com moléculas antioxidantes têm sido recomendada. O objetivo deste trabalho foi planejar e desenvolver novos compostos híbridos de benzofenonas com ácidos cinâmicos com propriedades incrementais antioxidante, analisando a fotodegradação utilizando-se de espectrometria de massas por imagem, e verificando os efeitos da modificação molecular na absortividade no espectro de UV dos compostos. Os novos híbr... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: Erythema, inflammation, photoaging and skin cancer are the most common problems caused by UV radiation. Stratified into 3 regions of the light spectrum: UVA (320-400 nm), UVB (280-320 nm) and UVC (200-280 nm ). The UVA and UVB radiations are the most harmful to the skin, because the UVC radiation is retained by the ozone layer and is only used as a germicide artificially. The incidence of UVA radiation on the skin induces the formation of ROS (reactive oxygen species) that affects indirectly the human DNA and can induce skin cancer. UVB radiation directly affects the pyrimidine bases of DNA molecules making it difficult to repair, increasing the chances of the individual developing skin cancer. To minimize and prevent damage caused by UV radiation to the skin sunscreens have been developed. Divided into organic and inorganic, presenting ability to block (inorganic) or absorbing (organic) incident UV radiation on the skin. Among the organic filters are benzophenones and cinnamates. To assist in the photoprotective effect of the filters, the combination with antioxidant molecules have been recommended. The objective of this study was to plan and develop new hybrid compounds of benzophenone with cinnamic acids with antioxidant incremental properties, analyzing photodegradation using imaging mass spectrometry techinques, and checking the effects of molecular change in absorptivity in the UV spectrum of the compounds. The new hybrids were evaluated for potential photoprotection, p... (Complete abstract click electronic access below) / Doutor

Orientador: Marlus Chorilli / Coorientador: Valéria Valente / Banca: Rose Mary Zumstein Georgetto Naal / Banca: Gislaine Ricci Leonardi / Banca: Janice Rodrigues Perussi / Banca: Marcos Antonio Correa / Resumo: O trans-resveratrol (RES) atua na prevenção e no tratamento de desordens cutâneas, porém apresenta baixa biodisponibilidade e rápida metabolização quando administrado por via oral em humanos. As nanopartículas lipídicas sólidas (NLSs) têm sido exploradas para a administração cutânea de fármacos, em virtude das características de interação com a pele. Assim, o objetivo deste capítulo foi à avaliação in vitro e in vivo da atividade do RES incorporado em NLSs para administração cutânea, bem como a avaliação da atividade antinociceptiva e antiedematogênica in vivo e dos efeitos celulares em células HaCat e B16F10 dos sistemas nanoestruturados. As formulações desenvolvidas foram selecionadas através de design fatorial, as quais eram compostas por ácido esteárico (AE), como lipídeos sólidos e fosfatidilcolina de soja (FS), polissorbato 80 (T80) e poloxamer 407 (P407) como tensoativos (F1). A esta formulação foi acrescido brometo de cetrimônio (BC) como tensoativo catiônico para promoção de carga superficial positiva (F2). O RES foi adicionado na fase lipídica da formulação, obtendo-se as formulações F1.RES e F2.RES, respectivamente. O diâmetro hidrodinâmico médio das formulações foi de 195,0 ± 3,34 nm, 241,3 ± 48,33 nm, 159,15 ± 4,78 nm e 158,25 ± 33,92 nm para F1, F1.RES, F2 e F2.RES, respectivamente. O potencial zeta (mV) das formulações foi -25,5 ± 1,01; -26,0 ± 1,67; 30,6 ± 1,13 e 30,0 ± 1,85 mV para F1, F1.RES, F2 e F2.RES, respectivamente. O RES livre foi quantificado de acor... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: Not available / Doutor

La microscopie confocale de réflectance in-vivo (RCM) est un outil puissant pour visualiser les couches cutanées à une résolution cellulaire. Des descripteurs du vieillissement cutané ont été mis en évidence à partir d'images confocales. Cependant, leur évaluation nécessite une analyse visuelle des images par des dermatologues expérimentés. L'objectif de cette thèse est le développement d'une technologie innovante pour quantifier automatiquement le phénomène du vieillissement cutané en utilisant la microscopie confocale de réflectance in vivo. Premièrement, la quantification de l’état de l’épiderme est abordée. Ensuite, la jonction dermique-épidermique est segmentée, et sa forme est caractérisée. Les mesures proposées mettent en évidence une différence significative entre les groupes d'âge et l’exposition au soleil. Enfin, les méthodes proposées sont validées par des études cliniques et d'efficacité de produits cosmétiques / In-vivo reflectance confocal microscopy (RCM) is a powerful tool to visualize the skin layers at cellular resolution. Aging descriptors have been highlighted from confocal images. However, it requires visual assessment of images by experienced dermatologists to assess those descriptors. The objective of this thesis is the development of an innovative technology to automatically quantify the phenomenon of skin aging using in vivo reflectance confocal microscopy. First, the quantification of the epidermal state is addressed. Then, the Dermal-Epidermal Junction is segmented, and its shape is characterized. The proposed measurements show significant difference among groups of age and photo-exposition. Finally, the proposed methods are validated through both clinical and cosmetic product efficacy studies

Orientador: Vera Lucia Borges Isaac / Banca: Marilisa Guimarães Lara / Banca: Pedro Alves da Rocha Filho / Banca: Marcos Antonio Correa / Banca: Iguatemy Lourenço Brunetti / Resumo: Desde a antiguidade, as plantas são utilizadas com finalidade curativa e, além do emprego na terapêutica, os extratos vegetais têm sido amplamente utilizados na indústria cosmética, como ativos, uma vez que sua composição complexa pode proporcionar efeitos benéficos mais intensos do que substâncias puras. Dados da literatura apontam que amoreira preta (Morus nigra L.) contém alta quantidade de compostos fenólicos, incluindo flavonoides, os quais promovem efeitos antioxidante, anti-inflamatório, antibacteriano. Por isso, neste trabalho, foram obtidos quatro tipos de extratos de folhas de Morus nigra L. (aquoso - EAq, hidroetanólico 50% - E50, hidroetanólico 70% - E70 e hidroetanólico 90% - E90), determinado o teor de compostos fenólicos e flavonoides totais e avaliado o potencial antioxidante, a fim de determinar qual o extrato mais eficaz para utilização como ativo cosmetodermatológico. O extrato que apresentou melhor atividade antioxidante, foi utilizado para avaliação da citotoxicidade em células HepG2, HaCat e HDFa, avaliação do efeito quimioprotetor em células HepG2 e HaCat e avaliação ao estimulo à biossíntese de colágeno. Também foi desenvolvida uma emulsão, na qual o extrato foi incorporado e para posterior caracterização reológica. Os resultados obtidos indicaram que os quatro extratos contêm compostos fenólicos e flavonoides apresentando efeito antioxidante, porém, o que apresentou maior teor e maior efetividade foi o E70. Desta forma, foi avaliada a citotoxicidade d... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: Since ancient times the plants are used with curative purpose. Besides employment in therapy, plant extracts have been widely used in the cosmetic industry as active, because their complex composition. The extracts can provide more intense beneficial effects than pure substances. Literature data show that black mulberry (Morus nigra L.) contains phenolic compounds, including flavonoids, which promote antioxidant, anti-inflammatory, antibacterial effects. Therefore, in this study we were obtained four Morus nigra L. leaf extracts (aqueous - EAq, hydroethanol 50% - E50, hydroethanol 70% - E70 and hydroethanol 90% - E¬90). The total phenolic compounds, total flavnoid and antioxidant potential are evaluated in order to verify the most effective for use as cosmetic active. The extract that showed better antioxidant activity, was used to evaluation for cytotoxicity in HepG2, HaCaT and HDFa cells, quimioprotetor effect on HepG2 and HaCaT cells and stimulate collagen biosynthesis. The extract has been incorporated on emulsion and their rheological characterization was also developed. The results indicated that the four extracts contain phenolic compounds and flavonoids having antioxidant effect, however, with the highest levels was observed to E70. Thus, the cytotoxicity of E70 was measured and their use is considered safety at the concentrations required for antioxidant activity against biological radicals, such as superoxide anion, hypochlorous acid and prevention of lipid peroxida... (Complete abstract click electronic access below) / Doutor