Incorporation of 2-amino-thiophene derivative in nanoparticles: enhancement of antifungal activity.

The objective of this study was to evaluate the effects of nanoparticles (nanospheres and nanocapsules) of the promising antifungal 2-amino-thiophene (6CN10) and 6CN10 complexed with 2-hydroxypropyl-ß-cyclodextrin (6CN10:HP-ß-CD) in vitro and compared with free drug against Candida and Cryptococcus, using a microdilution method to measure susceptibility. The Candida and Cryptococcus clinical strains were identified using phenotypic methods and matrix-assisted laser desorption/ionization-time of flight (MALDI-TOF). To measure in vitro antifungal susceptibility, we used microdilution trials. Serial drug or nanoparticle dilutions were prepared according to the CLSI M27-A3 guidelines. Anti-biofilm activity was verified for Cryptococcus neoformans. All Candida isolates were sensitive to the free drug (MIC = 41.66-333.33 µg/mL) and were able to grow even at the higher concentration tested for all 6CN10 nanoparticles. However, the Cryptococcus neoformans strains presented MIC values of 0.32-83.33 µg/mL for 6CN10 nanoparticles, and MIC values of 0.1-0.2 µg/mL for 6CN10:HP-ß-CD nanoparticles, i.e., 3333 times more active than the free drug (MIC values 166.66-333.33 µg/mL), and presenting activity greater than that of the reference drug amphotericin B (MIC = 0.5-0.125 µg/mL). 6CN10:HP-ß-CD nanosphere also showed high anti-biofilm potential. The in vitro study showed that the nanoparticles allowed better drug efficiency against Cryptococcus than did the free drug. These results suggest that 6CN10-loaded nanoparticles may become a future alternative for cryptococcosis and candidiasis therapy. In vivo experiments are essential prior to clinical use.

Combinação terapêutica no tratamento do melasma / Combinada en el tratamiento melasma / Combination therapy in the treatment of melasma terapia

Introdução: Melasma é uma discromia comum crônica, localizada, simétrica e adquirida, que acomete áreas fotoexpostas,preferencialmente a face. Mais frequente entre mulheres adultas, causa por cicatriz inestética, estresse emocional e impacto social,interferindo na autoestima e qualidade de vida pessoal. De patogênese não totalmente compreendida, tem alguns fatores de riscoconhecidos, como a história familiar, exposição solar, gravidez, hormônios sexuais, cosméticos, medicamentos fotossensibilizantes eevidente predisposição genética. A inibição eficiente da tirosinase humana, principal enzima envolvida na produção de melanina, diretae indiretamente promovida por ativos despigmentantes, como também o uso de diversos tipos de laser, fitoterápicos de uso oral como oPolypodium leucotomos, moléculas antioxidantes e indutores de reparação celular, usados de forma combinada, associados à adequadaproteção aos raios ultravioletas têm proporcionado avanços no tratamento, contribuindo para restabelecer a qualidade de vida. Objetivo:Apresentar os resultados de um caso clínico em que se utilizou tratamento combinado a uma paciente com melasma e relatar a eficáciadas combinações terapêuticas...

Introduction: Melasma is a chronic, localized, symmetrical and acquired common dyschromia that affects photo exposed areas, preferablythe face. More frequent among adult women, it causes, due to esthetic cicatrix problems, emotional stress and social impact by interferingin self-esteem and personal quality of life. Its pathogenesis is not fully understood but there are some known risk factors, such as familyhistory, sun exposure, pregnancy, sex hormones, cosmetics, photosensitizing drugs and an obvious genetic predisposition. The efficientinhibition of human tyrosinase, the key enzyme involved in melanin production, directly and indirectly promoted by active lighteners,as well as the use of various types of laser, oral herbal medicines, such as Polypodium Leucotomos, antioxidant molecules and cellularrepair inducers, used in a combined way, associated with adequate protection from ultraviolet rays, have provided advances in thetreatment, helping to restore the quality of life. Objective: To present the results of a clinical case in which we used combined treatmentin a female patient with melasma and to report the effectiveness of therapeutic combinations compared to monotherapy in the treatmentof this disease. Material and Method: It is a descriptive study developed through the report of a clinical trial in which we used for thetreatment of melasma an oral peeling in association with antioxidants for 60 days, as well as a topic and oral sunscreen. Result: Therewas a remarkable improvement in melasma...

Introdución: El melasma es un dischromia crónica común situada, simétrica y adquirida que afecta a las áreas foto expuestas,preferentemente la cara. Más común entre las mujeres adultas, debido a que el esfuerzo de impacto cicatriz antiestético, emocional ysocial, que afecta a la autoestima y la calidad de vida personal. La patogénesis no se entiende completamente y tiene algunos factoresde riesgo conocidos como los antecedentes familiares, la exposición al sol, el embarazo, las hormonas sexuales, cosméticos, fármacosfotosensibilizantes y la predisposición genética obvia. La inhibición eficiente de la tirosinasa humana, la principal enzima implicada en laproducción de melanina, directa e indirectamente promovido por aclaradores activos, así como el uso de varios tipos de láser, uso orala base de hierbas como Polypodium leucotomos, moléculas antioxidantes e inductores de reparación celular utilizados en combinación,asociados a una adecuada protección a los rayos ultravioleta han proporcionado avances en el tratamiento, ayudando a restaurar lacalidad de vida. Objetivo: Presentar los resultados de un caso clínico, que usa el tratamiento combinado a un paciente con el melasma yel informe de la eficacia de las terapias de combinación en comparación con la monoterapia en el tratamiento de esta condición. Materialy Métodos: Se realizó un estudio descriptivo desarrollado por el informe de un ensayo clínico en el que se empleó descamación oral encombinación con antioxidantes durante 60 días y uso de protección sola...