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1.
Daru ; 28(2): 635-646, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32856238

RESUMO

BACKGROUND: The purpose of the present study was to investigate the antioxidant and antimicrobial activities of a conventional preservative system containing desferrioxamine mesylate (DFO) and optimize the composition of the system through mathematical models. METHODS: Different combinations of ethylenediaminetetraacetic acid (EDTA), sodium metabisulfite (SM), DFO and methylparaben (MP) were prepared using factorial design of experiments. The systems were added to ascorbic acid (AA) solution and the AA content over time, at room temperature and at 40 °C was determined by volumetric assay. The systems were also evaluated for antioxidant activity by a fluorescence-based assay. Antimicrobial activity was assessed by microdilution technique and photometric detection against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus brasiliensis. A multi-criteria decision approach was adopted to optimize all responses by desirability functions. RESULTS: DFO did not extend the stability of AA over time, but displayed a better ability than EDTA to block the pro-oxidant activity of iron. DFO had a positive interaction with MP in microbial growth inhibition. The mathematical models showed adequate capacity to predict the responses. Statistical optimization aiming to meet the quality specifications of the ascorbic acid solution indicated that the presence of DFO in the composition allows to decrease the concentrations of EDTA, SM and MP. CONCLUSION: DFO was much more effective than EDTA in preventing iron-catalyzed oxidation. In addition, DFO improved the inhibitory response of most microorganisms tested. The Quality by Design concepts aided in predicting an optimized preservative system with reduced levels of conventional antioxidants and preservatives, suggesting DFO as a candidate for multifunctional excipient.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Ácido Ascórbico/farmacologia , Desferroxamina/química , Conservantes Farmacêuticos/química , Anti-Infecciosos/química , Antioxidantes/química , Ácido Ascórbico/química , Aspergillus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Ácido Edético/química , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Modelos Teóricos , Parabenos/química , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Sulfitos/química
2.
Curr Top Med Chem ; 18(4): 275-286, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29637863

RESUMO

It is challenging to disperse lipophilic substances in a validated cytotoxicity assay, especially for compounds with log Kow greater than or equal to 5 that may show false negative results. The purpose of this study was to explain the challenges in conducting a cytotoxicity validated test of lipophilic substances: Minthostachys setosa, Pimenta pseudocaryophyllus, and Drimysbrasiliensis essential oils. Additionally, we compared the equivalence of Neutral Red (NR) and 3- (4,5-dimethylthiazol-2-yl) -5- (3- carboxymethoxyphenyl) -2- (4-sulfophenyl) -2H -tetrazolium, inner salt (MTS) in detecting cell viability. The Hydrophile-Lipophile Balance (HLB) technique was used to evaluate the dispersion of essential oils and cytotoxicity in accordance to the guidelines of the OECD / GD 129 validated cytotoxicity assay. We compared the equivalence of vital dyes by TOST equivalence test. According to the results, we demonstrated the possibility of using other ways to disperse the lipophilic substances. Based on the HLB theory, we selected polysorbate 20 as the best solubilizing agent of the essential oils studied in D10 culture medium.


Assuntos
Óleos Voláteis/química , Óleos Voláteis/toxicidade , Animais , Células 3T3 BALB , Sobrevivência Celular/efeitos dos fármacos , Drimys/química , Lamiaceae/química , Camundongos , Óleos Voláteis/isolamento & purificação , Pimenta/química , Reprodutibilidade dos Testes
3.
Skin Pharmacol Physiol ; 31(1): 1-9, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29131088

RESUMO

The use of sunscreen products is widely promoted by schools, government agencies, and health-related organizations to minimize sunburn and skin damage. In this study, we developed stable solid lipid nanoparticles (SLNs) containing the chemical UV filter octyl methoxycinnamate (OMC). In parallel, we produced similar stable SLNs in which 20% of the OMC content was replaced by the botanical urucum oil. When these SLNs were applied to the skin of human volunteers, no changes in fluorescence lifetimes or redox ratios of the endogenous skin fluorophores were seen, suggesting that the formulations did not induce toxic responses in the skin. Ex vivo (skin diffusion) tests showed no significant penetration. In vitro studies showed that when 20% of the OMC was replaced by urucum oil, there was no reduction in skin protection factor (SPF), suggesting that a decrease in the amount of chemical filter may be a viable alternative for an effective sunscreen, in combination with an antioxidant-rich vegetable oil, such as urucum. There is a strong trend towards increasing safety of sun protection products through reduction in the use of chemical UV filters. This work supports this approach by producing formulations with lower concentrations of OMC, while maintaining the SPF. Further investigations of SPF in vivo are needed to assess the suitability of these formulations for human use.


Assuntos
Lipídeos/química , Nanopartículas/química , Óleos de Plantas/química , Protetores Solares/química , Química Farmacêutica/métodos , Cinamatos/administração & dosagem , Cinamatos/química , Humanos , Permeabilidade/efeitos dos fármacos , Óleos de Plantas/administração & dosagem , Pele/efeitos dos fármacos , Absorção Cutânea/efeitos dos fármacos , Protetores Solares/administração & dosagem , Raios Ultravioleta/efeitos adversos
4.
J Trace Elem Med Biol ; 41: 16-22, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28347458

RESUMO

Iron acquisition by bacteria and fungi involves in several cases the promiscuous usage of siderophores. Thus, antibiotic resistance from these microorganisms can be circumvented through a strategy of loading toxic metals into siderophores (Trojan Horse Effect). Desferrioxamine (dfo) and its cell-permeant derivative desferrioxamine-caffeine (dfcaf) were complexed with aluminum or gallium for this purpose. The complexes Me(dfo) and Me(dfcaf) (Me=Al3+ and Ga3+) were synthesized and characterized by mass spectroscopy and cyclic voltammetry. Their relative stabilities were studied through competitive equilibria with fluorescent probes calcein, fluorescein-desferrioxamine and 8-hydroxyquinoline. Me(dfo) and Me(dfcaf) were consistently more toxic than free Me3+ against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Candida albicans, demonstrating the Trojan Horse Effect. Wide spectrum antimicrobial action can be obtained by loading non-essential or toxic metal ions to microbes via a convenient siderophore carrier.


Assuntos
Alumínio/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Cafeína/farmacologia , Desferroxamina/farmacologia , Gálio/farmacologia , Alumínio/química , Antibacterianos/química , Antioxidantes/química , Cafeína/química , Candida albicans/efeitos dos fármacos , Desferroxamina/química , Relação Dose-Resposta a Droga , Portadores de Fármacos/química , Portadores de Fármacos/farmacologia , Escherichia coli/efeitos dos fármacos , Gálio/química , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
5.
Drug Dev Ind Pharm ; 43(2): 246-256, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27627681

RESUMO

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.


Assuntos
Compostos Azo/química , Ácidos Cumáricos/química , Fenóis/química , Protetores Solares , Tecnologia Farmacêutica/métodos , Triazinas/química , Desenho de Fármacos , Tecnologia Farmacêutica/normas , Raios Ultravioleta
6.
Braz. J. Pharm. Sci. (Online) ; 53(2): e16119, 2017. tab
Artigo em Inglês | LILACS | ID: biblio-839468

RESUMO

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.


Assuntos
Protetores Solares/farmacologia , Colágeno/administração & dosagem , Resultado do Tratamento , Agentes Molhantes/farmacologia , Fator de Proteção Solar/estatística & dados numéricos
7.
Braz. j. pharm. sci ; 52(4): 603-612, Oct.-Dec. 2016. tab, graf
Artigo em Inglês | LILACS | ID: biblio-951888

RESUMO

ABSTRACT Glutaraldehyde (GTA) has been extensively used as a gelatin crosslinking agent, however, new natural ones have been suggested as more biocompatible. Polyphenols are possible candidates and the flavonols, such as rutin (RUT), also exhibit potential synergism with sunscreens and antioxidant agents used in cosmetics. In this work, gelatin microspheres (M0) were obtained and crosslinked with GTA 10 mM (MG) or RUT 10 mM (MR), dissolved in acetone:NaOH 0,01M (70:30 v/v). MG exhibited crosslinking extent of 54.4%. Gelatin, M0, MG and MR did not elicit any signs of skin damage, regarding the formation of erythema, the barrier function disruption and negative interference in the stratum corneum hydration. Oily dispersions containing M0, MG or MR, isolated or combined with benzophenone-3 or octyl methoxycinnamate, suggested that the microspheres, at a 5.0% w/w, had no additional chemical or physical photoprotective effect in vitro. Crosslinking with RUT had occurred, but in a lower degree than GTA. Microspheres had not improved sun protection parameters, although, non-treated gelatin interfered positively with the SPF for both UV filters. The in vivo studies demonstrated that these materials had very good skin compatibility.


Assuntos
Rutina/efeitos adversos , Glutaral/efeitos adversos , Gelatina/análise , Microesferas , Protetores Solares , Produtos Biológicos/farmacologia , Cosméticos/classificação
8.
Braz. j. pharm. sci ; 52(2): 273-280, Apr.-June 2016. tab, graf
Artigo em Inglês | LILACS | ID: lil-795004

RESUMO

ABSTRACT The physicochemical attributes of emulsified systems are influenced by the characteristics of their internal phase droplets (concentration, size and morphology), which can be modified not only by the formulation components, but also by the analytical methodology employed. Thus, the aim of this work involved the physicochemical characterization of cosmetic emulsions obtained from different surfactants, as well as the introduction of the optical coherence tomography (OCT) as the analytical technique employed for the morphological characterization and particle size determination of the formulations. Three emulsions were prepared, differing at the type and concentration of the surfactant used, and their droplet sizes were evaluated through optical microscopy, laser diffraction and OCT. The microscopic analysis and the laser diffraction techniques provided an average particle size minor than 6.0 µm, not detected by the OCT technique, which could identify only bigger particles of the emulsified systems' internal phase. The results testify that OCT was suitable for the morphological characterization of cosmetic emulsions; however, the technique needs to be improved to ensure a better sensitivity in the analysis of smaller particles.


RESUMO Os atributos físico-químicos de sistemas emulsionados são influenciados pelas características de suas gotículas de fase interna (concentração, tamanho e morfologia), as quais podem ser modificadas não apenas pelos componentes da formulação, mas também pela metodologia analítica empregada. Desta forma, o objetivo deste trabalho envolveu a caracterização físico-química de emulsões cosméticas obtidas a partir de diferentes tensoativos, bem como a introdução da tomografia de coerência óptica (OCT) como a técnica analítica utilizada para a caracterização morfológica e determinação do tamanho de partícula das formulações. Três emulsões foram preparadas, diferindo no tipo e concentração do tensoativo empregado, e seus tamanhos de gotícula foram avaliados por meio das técnicas de microscopia óptica, difração a laser e OCT. As técnicas de microscopia óptica e difração a laser forneceram tamanhos de partícula médios menores de 6.0 µm, não detectados pela técnica de OCT, que permitiu apenas a identificação de partículas maiores pertencentes à fase interna dos sistemas emulsionados. Os resultados reforçam a introdução da OCT como metodologia promissora para a caracterização morfológica de emulsões cosméticas; no entanto, a técnica requer aprimoramento para garantir maior sensibilidade na análise de partículas de menor tamanho.


Assuntos
Tomografia de Coerência Óptica/métodos , Emulsões/análise , Tensoativos/análise
9.
J Photochem Photobiol B ; 148: 154-159, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25920069

RESUMO

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.


Assuntos
Pele/efeitos dos fármacos , Protetores Solares/farmacologia , Raios Ultravioleta , Adulto , Alcanos/química , Antioxidantes/química , Benzofenonas/química , Chalconas/química , Estabilidade de Medicamentos , Feminino , Humanos , Masculino , Propiofenonas , Rutina/química , Pele/metabolismo , Pele/efeitos da radiação , Protetores Solares/química , Adulto Jovem
10.
Acta sci., Biol. sci ; 37(1): 9-13, jan.- mar. 2015. tab, ilus
Artigo em Inglês | LILACS | ID: biblio-847938

RESUMO

Senna species have been widely used by American, African and Indian ethic groups mainly in the treatment of feebleness, constipation, liver disorders and skin infections. Senna occidentalis (L.) Link is a perennial shrub native to South America and indigenous to tropical regions throughout the world. Current study evaluated the antimicrobial activity of aqueous and hydroalcoholic extracts from S. occidentalis prepared from different parts of the plant. Antimicrobial activity was assessed against standard pharmaceutical microorganisms by spectrophotometry and microdilution technique. Escherichia coli was sensitive only to compounds extracted from seeds which may be proteinaceous. A broader antimicrobial spectrum was demonstrated by the hydroalcoholic extract of seeds, mostly against Pseudomonas aeruginosa. The in vitro toxicity using mouse fibroblasts indicated that the extract might be a biocompatible ingredient for topical formulations, while the hydroalcoholic extract of aerial parts demonstrated to be potentially cytotoxic.


Espécies de Senna são amplamente utilizadas por tribos americanas, africanas e indianas, principalmente para tratar a fraqueza, a constipação, as desordens do fígado e também em preparações tópicas para infecções de pele. A Senna occidentalis (L.) Link é um arbusto perene nativo da América do Sul encontrado em regiões tropicais. Este trabalho avaliou a atividade antimicrobiana de extratos aquosos e hidroalcoólicos de diferentes partes da planta. A atividade antimicrobiana foi estabelecida frente aos microrganismos padrões farmacêuticos por espectrofotometria e técnica de microdiluição. A Escherichia coli apresentou sensibilidade apenas a componentes extraídos das sementes, os quais podem ser de natureza proteica. O espectro mais amplo de atividade antimicrobiana foi obtido com o extrato hidroalcoólico das sementes, principalmente contra Pseudomonas aeruginosa. A toxicidade in vitro utilizando fibroblastos de camundongo indicou que este extrato pode ser um ingrediente biocompatível para formulações de uso tópico. Já o extrato hidroalcoólico de partes aéreas demonstrou ser potencialmente citotóxico.


Assuntos
Antibacterianos , Antifúngicos , Fabaceae , Fibroblastos , Medicina Tradicional , Senna (Planta)/citologia
11.
Pharm Dev Technol ; 20(2): 197-203, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-24286179

RESUMO

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.


Assuntos
Antifúngicos/administração & dosagem , Antifúngicos/química , Desenho de Fármacos , Piridonas/administração & dosagem , Piridonas/química , Absorção Cutânea , Pele/metabolismo , Administração Cutânea , Animais , Antifúngicos/farmacocinética , Química Farmacêutica , Ciclopirox , Cultura em Câmaras de Difusão , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Técnicas In Vitro , Permeabilidade , Piridonas/farmacocinética , Pele/efeitos dos fármacos , Creme para a Pele , Suínos
12.
Artigo em Inglês | LILACS | ID: lil-672213

RESUMO

A pesquisa tem como objetivo a aplicação da transmitância espectral utilizando uma esfera de integração para estimar o Fator de Proteção Solar (FPS) de fotoprotetores comerciais para o uso infantil. Fotoprotetores com FPS 30 (A, B e C), disponíveis comercialmente, foram selecionados para avaliação conforme as seguintes metodologias: valor de pH, perfil reológico, e valor de FPS in vitro por espectroscopia. As amostras A, B e C apresentaram, respectivamente, os seguintes valores de pH: 7.8, 7.4 e 7.0. O perfil reológico identificou os sistemas como semissólidos pseudoplásticos não-Newtonianos, com área de histerese. O teste-T (p < 0.05) foi utilizado para confrontar o FPS alegado (FPS = 30) com o estimado por espectroscopia. Estudos in vitro foram considerados de grande importância para a área cosmética, podendo corroborar, previamente, a realização dos estudos de eficácia in vivo. De acordo com os resultados, as amostras A, B e C apresentaram valores de FPS sem diferença estatisticamente significativa, quando comparados àqueles citados nos rótulos. A transmitância espectral utilizando esfera de integração provou ser uma metodologia conveniente, rápida e reprodutível para a avaliação estimada do FPS.


This research focused on the measurement of spectral transmittance using an integrating sphere to estimate the Sun Protection Factor (SPF) of commercial sunscreens oriented for child use. Commercially available SPF 30 sunscreens (A, B and C) were selected and assessed by the following methodology: pH measurement; rheological profile analysis; and in vitro SPF estimation by spectroscopy. Samples A, B and C exhibited, respectively, pH values of 7.8, 7.4 and 7.0. The rheological profile identified the systems as pseudoplastic non-Newtonian semisolids with hysteresis loops. The t-test (p < 0.05) was used to confront the claimed SPF (SPF = 30) with that estimated by spectroscopy. In vitro tests are considered of utmost importance in the cosmetic , since their results may be used to validate submission to subsequent in vivo efficacy experiments. According to our results, sunscreens A, B and C generated SPF values without any significant difference from those claimed on the commercial sunscreen labels. The measurement of spectral transmittance with an integrating sphere proved to be a convenient, fast and reproducible method for SPF estimation.


Assuntos
Reologia , Análise Espectral , Protetores Solares
13.
J Photochem Photobiol B ; 120: 142-7, 2013 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-23380541

RESUMO

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.


Assuntos
Álcoois/química , Tinturas para Cabelo , Cabelo/efeitos dos fármacos , Cabelo/efeitos da radiação , Lythraceae/química , Extratos Vegetais/farmacologia , Raios Ultravioleta/efeitos adversos , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Humanos , Fenômenos Mecânicos , Extratos Vegetais/isolamento & purificação
14.
Pharm Dev Technol ; 18(5): 1247-54, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-22670808

RESUMO

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.


Assuntos
Primaquina/química , Química Farmacêutica/métodos , Preparações de Ação Retardada/química , Difusão , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Cinética , Metilcelulose/química , Fosfatos/química , Polietilenoglicóis/química , Primaquina/administração & dosagem , Solubilidade , Comprimidos/química
15.
J Trace Elem Med Biol ; 27(2): 103-8, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23122029

RESUMO

Molecules naturally designed for the acquisition of essential metals can be used as a shuttle to deliver toxic metal ions to target organisms. In this study, we describe for the first time the synthesis of a derivative of cadmium and desferrioxamine B, a bacterial siderophore. The new compound was characterized by elemental analysis, vibrational (infrared and Raman) spectroscopy, mass coupled thermal analyses and X-ray diffraction methods. Studies on the in vitro toxicity toward a fungus and two bacterial strains indicated that the coordination compound is more active against microrganisms than cadmium chloride on a Cd-concentration basis, indicating that desferrioxamine can work as a "Trojan horse" in the delivery of a toxic metal.


Assuntos
Bactérias/efeitos dos fármacos , Cádmio/toxicidade , Desferroxamina/química , Fungos/efeitos dos fármacos , Varredura Diferencial de Calorimetria , Espectrometria de Massas , Testes de Sensibilidade Microbiana , Pós , Espectroscopia de Infravermelho com Transformada de Fourier , Análise Espectral Raman , Termogravimetria , Difração de Raios X
16.
Braz. j. pharm. sci ; 49(2): 251-261, Apr.-June 2013. ilus, graf, tab
Artigo em Inglês | LILACS | ID: lil-680636

RESUMO

Nanotechnology applies to diverse sectors of science. In cosmetic area, investments have strengthened the idea that nanoproducts provide innumerable benefits to consumers. Extreme exposition to solar light can cause undesirable effects, thus, adding UV filters in cosmetic products are often used as prevention. Ethylhexyl methoxycinnamate and benzophenone-3 are UV filters widely used in sunscreen formulations, this UV filters absorb UVB and UVA radiation, respectively. In this study, sunscreen formulations were developed as nano and macroemulsion, but composed by the same raw material. Nanoemulsion was obtained by phase inversion temperature method (PIT). Physical and functional properties were evaluated by visual analysis, particle size distribution and by diffuse reflectance spectrophotometry. Achieved nanoemulsion showed bluish brightness aspect, less apparent consistency than macroemulsion, stability longer than 48 hours (22.0 ± 2.0 °C) and bimodal particle size distribution with average (mean) sizes around 10 nm (61%) and 4.5 µm (39%). Macroemulsion showed milky aspect, higher consistency than nanoemulsion, instability after 48 hours (22.0 ± 2.0 °C) and bimodal particle size distribution with average (mean) size around 202 nm (9%) and 10.4 µm (91%). Effectiveness profile of sunscreen formulations remained apparently similar, based on achieved results of in vitro SPF, UVA/UVB ratio and critical wavelength assays.


A nanotecnologia se aplica a diversos setores da ciência. Na área de cosméticos, os investimentos têm reforçado a idéia de que nanoprodutos oferecem inúmeros benefícios para os consumidores. A exposição excessiva à luz solar pode causar efeitos indesejáveis, logo, a adição de filtros UV em produtos cosméticos é frequentemente usada como prevenção. O p-metoxicinamato de octila e a benzofenona-3 são filtros UV amplamente utilizados em formulações de protecção solar, que absorvem radiações UVB e UVA, respectivamente. Neste estudo, desenvolveram-se formulações de protetores solares na forma de nano e macroemulsão, mas compostos pelas mesmas matérias-primas. A nanoemulsão foi obtida pelo método da temperatura de inversão de fases (PIT). As propriedades físicas e funcionais foram avaliadas por análise visual, distribuição de tamanho de partículas e por espectrofotometria de reflectância difusa. A nanoemulsão obtida apresentou brilho azulado, menor consistência aparente quando comparada `a macroemulsão, estabilidade superior a 48 horas (22,0 ± 2,0 ° C) e distribuição de tamanhos de partícula bimodal, com média (média) de tamanhos ao redor de 10 nm (61%) e 4,5 µm (39%) . A macroemulsão apresentou aspecto leitoso, maior consistência aaprente do que nanoemulsão, instabilidade após 48 horas (22,0 ± 2,0 ºC) e distribuição de tamanhos de partícula bimodal, com média (média) de tamanhos ao redor de 202 nm (9%) e 10,4 µm (91%). O perfil de eficácia das formulações fotoprotetoras permaneceu aparentemente similar, com base em resultados obtidos por ensaios de FPS in vitro, relação UVA/UVB e comprimento de onda crítico.


Assuntos
Tamanho da Partícula , Protetores Solares/análise , Técnicas In Vitro , Benzofenonas/análise , Inversão Térmica , Nanotecnologia , Filtros Ultravioletas
17.
Braz. j. pharm. sci ; 49(2): 293-299, Apr.-June 2013. tab
Artigo em Inglês | LILACS | ID: lil-680640

RESUMO

Rising global demand for natural products whose production is harmless to the environment has stimulated the development of natural cosmetics and, within this category, organics (95% organic raw materials). The image of environmentally friendly production is one of the strongest attractions of organic products. Lip balm is a cosmetic product similar to lipstick whose purpose is to prevent lip dryness and protect against adverse environmental factors. The product's characteristics are: resistance to temperature variations, pleasant flavor, innocuousness, smoothness during application, adherence and easy intentional removal. This work involved the development of a lip balm formulated with certified organic raw materials and the execution of stability tests: fusion point determination, evaluation of organoleptic characteristics (color, odor and appearance) and functionality evaluation (spreadability test). The formulation selected after the Preliminary Stability Test was submitted to the Normal Stability Test under the following storage conditions (temperature): Room Temperature (22.0 ± 3.0 ºC), Oven (40.0 ± 2.0 ºC) and Refrigerator (5.0 ± 1.0 ºC), for 90 days. Under the Refrigerator and Room Temperature conditions, spreadability proved adequate, but the surface presented white spots, characterizing the fat bloom, a phenomenon involving the recrystallization of cocoa butter. Storage at 40.0 ± 2.0 ºC (Oven) caused loss of functionality according to the spreadability test, in addition to changes in color, although the aspect was uniform since the fat bloom was not observed (white spots on the surface). The odor remained stable under all conditions as did the melting point, which had a mean of 72.9 ± 1.7 ºC throughout the course of stability testing (90 days).


O aumento da demanda global por produtos naturais, cuja produção não envolva nenhum dano ao meio ambiente, tem estimulado o desenvolvimento de cosméticos naturais e, dentro desta categoria, dos produtos orgânicos (que contêm 95% de matérias-primas orgânicas). O protetor labial é um produto cosmético semelhante ao batom que tem a finalidade de prevenir o ressecamento dos lábios, mantendo a hidratação, e protegê-los contra fatores ambientais adversos. Este trabalho envolveu o desenvolvimento de um protetor labial formulado com matérias-primas orgânicas e avaliação dos parâmetros de estabilidade, como ponto de fusão, características organolépticas e funcionalidade (teste de espalhabilidade). A formulação selecionada após o Estudo de Estabilidade Preliminar foi submetida à Avaliação Normal de Estabilidade, nas seguintes condições de armazenamento (temperatura): Ambiente (22,0 ± 3,0 ºC), Estufa (40,0 ± 2,0 ºC) e Geladeira (5,0 ± 1,0 ºC), por 90 dias. Nas condições de armazenamento em geladeira ou ambiente, a espalhabilidade foi adequada, mas a superfície apresentou pontos esbranquiçados, caracterizando o fenômeno chamado fat bloom, que está relacionado à recristalização da manteiga de cacau. O armazenamento à temperatura elevada (40,0 ± 2,0 ºC) provocou perda de funcionalidade, de acordo com o teste de espalhabilidade, e mudança de cor, apesar do aspecto permanecer uniforme, visto que não foi observado o fenômeno fat bloom. O odor manteve-se estável em todas as condições, assim como o ponto de fusão, com valor médio de 72,9 ºC ± 1,7 ºC durante todo o período de avaliação do teste de estabilidade (90 dias).


Assuntos
Produtos para Lábios , Estabilidade de Cosméticos , /classificação , Produtos Biológicos/análise , Cosméticos/farmacocinética , Manteiga de Cacau
18.
Eur J Dermatol ; 22(1): 8-13, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22217508

RESUMO

In recent years, several studies have demonstrated the protective effect of Heat Shock Proteins (HSP) on different organs and tissues under stressful conditions. However, most research explores the performance of those molecular chaperones during immune responses or pathological conditions like cancer, whereas the number of studies related to the performance of HSPs in the skin during diverse natural or physiopathological conditions is very low. Therefore, the aim of this article was to summarize the main concepts concerning the expression and performance of HSPs, from analysis of current medicine and cosmetics publications, as well as exploring the importance of these proteins in the dermatological area in physiological events such as cutaneous aging, skin cancer and wound healing and to present final considerations related to biotechnology performance in this area.


Assuntos
Proteínas de Choque Térmico/metabolismo , Envelhecimento da Pele , Neoplasias Cutâneas/metabolismo , Pele/metabolismo , Proteínas de Choque Térmico/efeitos dos fármacos , Humanos , Cicatrização
19.
Braz. j. pharm. sci ; 48(3): 507-518, July-Sept. 2012. ilus, tab
Artigo em Inglês | LILACS | ID: lil-653465

RESUMO

Expired or unused medication at people's homes is normally disposed of in normal garbage, sewage system or, in certain cases, returned to the public health system. There is still no specific legislation regarding this leftover medication to regulate and orient the handling and correct disposal of medication waste. However, there is defined regulation regarding health services' solid waste. This article has the objective of discussing management models for the disposal of medication waste and the recommendations made by pertinent national and international legislation. By means of literature reviews, the management structure for medication waste of international legislation and the regulations regarding the environment, as well as the national legislation for the solid waste from health services was analyzed. Through the analysis it was possible to present better clarifications as to the possible impacts to the environment, to the public's health and alternatives in order to obtain the efficient disposal of medication, reducing and/or avoiding sanitary risk, guaranteeing the quality and safety of public health.


As sobras de medicamentos oriundas do desuso ou da expiração do prazo de validade que constam nos domicílios da população, normalmente, são destinadas diretamente para o lixo comum, rede de esgoto ou, em alguns casos, devolvidas para a rede pública. Sobre essas sobras, ainda não há legislação específica que regulamenta e orienta sobre a manipulação e destinação correta do descarte dos resíduos de medicamentos. Entretanto, sobre os resíduos sólidos de serviços de saúde já se possui regulamentações definidas. O presente artigo tem como objetivo discutir modelos de gestão de descarte de resíduos de medicamentos e as recomendações de legislações internacionais e nacionais pertinentes. Por meio de revisão de literatura, analisou-se a estrutura do gerenciamento de resíduos para medicamentos de legislação internacional e as regulamentações relacionadas ao meio ambiente, assim como a legislação nacional de resíduos sólidos de serviços de saúde. Com a análise foi possível apresentar melhores esclarecimentos quanto aos possíveis impactos ao meio ambiente, à saúde da população e alternativas para se obter gestão eficaz de descarte de medicamentos, reduzindo e/ou evitando o risco sanitário, garantindo qualidade e segurança da saúde pública.


Assuntos
Eliminação de Resíduos de Serviços de Saúde/legislação & jurisprudência , Descarga de Resíduos Sólidos , Risco à Saúde Humana , Poluição Ambiental/prevenção & controle
20.
An Bras Dermatol ; 86(4): 732-42, 2011.
Artigo em Inglês, Português | MEDLINE | ID: mdl-21987140

RESUMO

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.


Assuntos
Roupa de Proteção , Proteção Radiológica/métodos , Queimadura Solar/prevenção & controle , Protetores Solares/administração & dosagem , Raios Ultravioleta/efeitos adversos , Humanos
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