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2.
Drug Dev Ind Pharm ; 45(4): 642-650, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30642209

RESUMO

OBJECTIVE: To develop an azelaic acid (AzA)-loaded nanoemulsion with hyaluronic acid (HA) as a double targeting strategy to increase drug retention and tyrosinase inhibition activity. SIGNIFICANCE: Dermic melasma is a recalcitrant disease. Therefore, the development of new technologies that allow a deeper penetration in the skin while enhancing the efficacy of a safe and well-known dermatological active, like AzA, is a very promising alternative to improve the treatment of this disease. METHODS: An oil-in-water nanoemulsion was developed and characterized according to its droplet size distribution, zeta potential, pH value, drug content, encapsulation efficiency, spectroscopic characteristics, morphology, and stability. In vitro mushroom tyrosinase inhibition assay, cytotoxicity, and permeation studies were performed. A descriptive sensory evaluation was also carried out. RESULTS: Drug content was 10 mg/ml, particle size 419 ± 23 nm with monomodal distribution, encapsulation efficiency was 84.65%, zeta potential -10.9 ± 0.44 mV and pH 5.01 ± 0.01. The nanoemulsion was stable for 30 days (30 °C/65% RH). The nanoemulsion decreased tyrosinase activity and permeated through the skin, reaching viable epidermis and dermis and did not show signs of cytotoxicity. Sensory evaluation profile showed a higher spreadability with lesser whitening residue. CONCLUSION: The nanoemulsion presented characteristics within the nanoscale and reached the deeper layers of the skin while improving in vitro tyrosinase inhibition; hence, it could be a promising treatment to dermic melasma.


Assuntos
Fármacos Dermatológicos/farmacologia , Ácidos Dicarboxílicos/farmacologia , Sistemas de Liberação de Medicamentos/métodos , Ácido Hialurônico/farmacologia , Preparações Clareadoras de Pele/farmacologia , Administração Cutânea , Animais , Sobrevivência Celular/efeitos dos fármacos , Fármacos Dermatológicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Emulsões , Voluntários Saudáveis , Humanos , Melanose/tratamento farmacológico , Monofenol Mono-Oxigenase/antagonistas & inibidores , Nanopartículas/química , Tamanho da Partícula , Pele/efeitos dos fármacos , Pele/metabolismo , Pele/patologia , Absorção Cutânea/efeitos dos fármacos , Preparações Clareadoras de Pele/uso terapêutico , Pigmentação da Pele/efeitos dos fármacos , Suínos
3.
Arch Dermatol Res ; 307(10): 905-15, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26472098

RESUMO

Several studies have reported an increase in the prevalence of adult female acne. This subtype of acne presents particular characteristics, and can be triggered by several factors such as smoking, stress, the use of oily cosmetics and even by poor sleep. Sleep quality is related to well-being and the maintenance of body homeostasis. In addition, several skin diseases present a bidirectional relationship with sleep, demonstrating an important connection between skin and the central nervous system. With this in mind, we aimed to compare the effect of two types of treatment for adult female acne (azelaic acid or a combined oral contraceptive) on sleep quality and on concentrations of stress hormones. Also, we proposed to assess the correlation of sleep and hormonal parameters with acne severity. In order to do this, 32 women underwent a clinical evaluation, completed the Pittsburgh Sleep Quality Index (PSQI) questionnaire and had their blood collected for hormone assays. These procedures were performed at baseline and after 6 months of treatment. At baseline there were no differences between the groups in terms of body mass index, age, acne severity and hormone concentrations. Results showed that both treatments demonstrated effectiveness but that women treated with azelaic acid presented a better sleep quality after the treatment compared to baseline and to the group treated with the combined oral contraceptive. The combined oral contraceptive group presented an increase in cortisol and a decrease in free testosterone concentration in relation to baseline. These data suggest that both azelaic acid and combined oral contraceptive are effective in the treatment of adult female acne but, azelaic acid seems to be a more suitable option for those women who may benefit from a better subjective sleep quality.


Assuntos
Acne Vulgar/tratamento farmacológico , Anticoncepcionais Orais Combinados/uso terapêutico , Anticoncepcionais Orais Hormonais/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Medicamentos Indutores do Sono/uso terapêutico , Sono/efeitos dos fármacos , Hormônio Adrenocorticotrópico/sangue , Adulto , Sistema Nervoso Central/fisiologia , Feminino , Humanos , Hidrocortisona/sangue , Fenômenos Fisiológicos da Pele , Inquéritos e Questionários , Testosterona/sangue
4.
J Clin Lipidol ; 9(3): 384-9, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26073398

RESUMO

Despite major advances in pharmacologic therapy over the last few decades, dyslipidemia remains a prevalent, insufficiently recognized, and undercontrolled risk factor for cardiovascular disease. Statins are the mainstay of hypercholesterolemia treatment, but because of adherence and tolerability issues that limit dose titration, there is a need for additional therapies with good efficacy and better tolerability. Adenosine triphosphate (ATP) citrate lyase, a cytoplasmic enzyme responsible for the generation of acetyl coenzyme A for the de novo synthesis of fatty acids and cholesterol, is a very interesting molecular target for the reduction of plasma lipids. Furthermore, ATP citrate lyase inhibition may be accompanied by activation of 5'-adenosine monophosphate-activated protein kinase, a key signaling molecule that acts a central hub in cellular metabolic regulation. ETC-1002 is a small molecule inhibitor of ATP citrate lyase that also activates 5'-adenosine monophosphate-activated protein kinase, effectively reducing low-density lipoprotein cholesterol and inducing some other positive metabolic changes. Recent evidence from phase I and II clinical trials in humans has shown a positive efficacy and safety profile of ETC-1002, with low-density lipoprotein cholesterol reductions similar to those attainable by usual doses of many statins and with no major apparent side effects. These results potentially introduce a new family of medications that may expand our therapeutic arsenal against hypercholesterolemia.


Assuntos
ATP Citrato (pro-S)-Liase , Ácidos Dicarboxílicos/uso terapêutico , Dislipidemias , Ácidos Graxos/uso terapêutico , ATP Citrato (pro-S)-Liase/antagonistas & inibidores , ATP Citrato (pro-S)-Liase/metabolismo , Animais , Colesterol/biossíntese , Ensaios Clínicos Fase I como Assunto , Ensaios Clínicos Fase II como Assunto , Coenzima A/biossíntese , Dislipidemias/tratamento farmacológico , Dislipidemias/enzimologia , Ácidos Graxos/biossíntese , Humanos
5.
Antibiot Khimioter ; 55(11-12): 17-21, 2010.
Artigo em Russo | MEDLINE | ID: mdl-21574420

RESUMO

High in vitro and in vivo efficacy of Ingavirin against the Mexican pandemic influenza virus A/H1N1/2009, strains A/California/04/2009 (H1N1) and A/California/07/2009 (H1N1) vs. the reference drug Arbidol was studied and verified when used therapeutically and prophylactically.


Assuntos
Amidas/uso terapêutico , Antivirais/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Imidazóis/uso terapêutico , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Influenza Humana , Caproatos , Humanos , Indóis/uso terapêutico , Influenza Humana/tratamento farmacológico , Influenza Humana/prevenção & controle
6.
Dermatol. rev. mex ; 36(3): 177-85, mayo-jun. 1992.
Artigo em Espanhol | LILACS | ID: lil-117384

RESUMO

Una revisión bibliográfica de los últimos años sobre terapéutica en acné nos muestra que constantemente se están probando sustancias para encontrar el medicamento tópico ideal, el cual debe ser comedolítico, antiinflamatorio no irritante, bien tolerado y aceptado por los pacientes. Esto aún no se ha logrado. Las tetraciclinas orales han demostrado su gran beneficio en el control del acné inflamatorio. Actualmente es posible controlar el acné severo con los retinoides orales; creo que serán usados más frecuentemente en un futuro próximo.


Assuntos
Humanos , Acne Vulgar/terapia , Ácidos Dicarboxílicos/uso terapêutico , Acne Vulgar/psicologia , Terapia a Laser , Hormônios/uso terapêutico , Peróxido de Benzoíla/uso terapêutico , Retinoides/uso terapêutico , Tetraciclina/uso terapêutico
7.
Int J Dermatol ; 30(12): 893-5, 1991 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-1816137

RESUMO

The efficacy of 20% azelaic acid cream and 4% hydroquinone cream, both used in conjunction with a broad-spectrum sunscreen, against melasma was investigated in a 24-week, double-blind study with 329 women. Over the treatment period the azelaic acid cream yielded 65% good or excellent results; no significant treatment differences were observed with regard to overall rating, reduction in lesion size, and pigmentary intensity. Severe side effects such as allergic sensitization or exogenous ochronosis were not observed with azelaic acid.


Assuntos
Fármacos Dermatológicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Hidroquinonas/uso terapêutico , Melanose/tratamento farmacológico , Administração Cutânea , Adolescente , Adulto , Fármacos Dermatológicos/efeitos adversos , Ácidos Dicarboxílicos/efeitos adversos , Método Duplo-Cego , Feminino , Humanos , Hidroquinonas/efeitos adversos , Melanose/patologia , Pessoa de Meia-Idade , Pomadas
10.
Med Cutan Ibero Lat Am ; 16(6): 511-4, 1988.
Artigo em Espanhol | MEDLINE | ID: mdl-3073279

RESUMO

A comparative double-blind study was carried out on sixty patients received oral contraceptives. Patients were treated with 20% azelaic acid or 4% hydroquinone. They were observed for 24 weeks and the results compared and checked for side effects. The results showed that the azelaic acid was not better than the hydroquinone in the treatment of melasma but it could be used as alternative drug.


Assuntos
Antineoplásicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Hidroquinonas/uso terapêutico , Melanose/tratamento farmacológico , Administração Tópica , Adolescente , Adulto , Antineoplásicos/administração & dosagem , Antineoplásicos/efeitos adversos , Ensaios Clínicos como Assunto , Ácidos Dicarboxílicos/administração & dosagem , Ácidos Dicarboxílicos/efeitos adversos , Método Duplo-Cego , Feminino , Humanos , Hidroquinonas/administração & dosagem , Hidroquinonas/efeitos adversos , Pomadas
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