Estudo de liberação e permeação in vitro do diclofenaco de dietilamônio em microemulsão gel-like

Silva, José Alexsandro da; Santana, Davi Pereira de; Bedor, Danilo César Galindo; Borba, Valeria Ferreira da Costa; Lira, Ana Amélia Moreira; Egito, Eryvaldo Sócrates Tabosa do

doi:10.1590/s0100-40422009000600005

Cited by 29 publications

(19 citation statements)

References 22 publications

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“…It is noteworthy the existence of a variety of states, highlighting the presence of microemulsion formation areas, which are regions where the energy used and the components proportions were suitable to reduce the interfacial tension until the formation of a homogeneous, clear and translucent system (Silva et al , 2009a). …”

Section: Resultsmentioning

confidence: 99%

“…Under these conditions, all formulations exhibited a homogeneous appearance, without any evidence of phase separation or precipitate formation. As is well known, the optimum pH of a topical formulation must be selected so as to maximize the stability of active components and the tolerance of the skin, being acceptable values between 5.5 and 8.0 (Silva et al , 2009a). The pH values shown for ME-blank and ME-5CN05 were within this range, which would allow the topical application of the ME-5CN05 system.…”

Section: Discussionmentioning

confidence: 99%

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Antifungal activity of topical microemulsion containing a thiophene derivative

Guimarães¹,

Reis²,

Silva³

et al. 2014

Braz. J. Microbiol.

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Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05) embedded in a microemulsion (ME). The minimum inhibitory concentration (MIC) was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05) showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270–540 μg.mL−1) and good activity against C. neoformans (MIC = 17 μg.mL−1). Candida species were susceptible to ME-5CN05 (70–140 μg.mL−1), but C. neoformans was much more, presenting a MIC value of 2.2 μg.mL−1. The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans.

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Antifungal activity of topical microemulsion containing a thiophene derivative

Guimarães¹,

Reis²,

Silva³

et al. 2014

Braz. J. Microbiol.

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“…However, it remained within the ME range, i.e., 10-150 nm (Silva et al, 2009), or, according to Damasceno et al (2011), 10-300 nm (Table II). The increase in droplet diameter might suggest the location of the drug in the interfacial layer of surfactants, which may decrease the curvature of the micelle and thus change the size of the droplets (Gomes, 2010).…”

Section: Resultsmentioning

confidence: 71%

Phenobarbital loaded microemulsion: development, kinetic release and quality control

Figueiredo

Neves

Silva

et al. 2016

Braz. J. Pharm. Sci.

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This study aimed to obtain and characterize a microemulsion (ME) containing phenobarbital (PB). The PB was incorporated in the proportion of 5% and 10% in a microemulsion system containing Labrasol ® , ethanol, isopropyl myristate and purified water. The physicochemical characterization was performed and the primary stability of the ME was evaluated. An analytical method was developed using spectrophotometry in UV λ = 242 nm. The kinetics of the in vitro release (Franz model) of the ME and the emulsion (EM) containing PB was evaluated. The incorporation of PB into ME at concentrations of 5 and 10% did not change pH and resistance to centrifugation. There was an increase in particle size, a decrease of conductivity and a change in the refractive index in relation to placebo ME. The ME remained stable in preliminary stability tests. The analytical method proved to be specific, linear, precise, accurate and robust. Regarding the kinetics of the in vitro release, ME obtained an in vitro release profile greater than the EM containing PB. Thus, the obtained ME has a potential for future transdermal application, being able to compose a drug delivery system for the treatment of epilepsy.Uniterms: Microemulsion/physicochemical characterization. Microemulsion/In vitro release. Phenobarbital/microemulsion system/evaluation. Nanotechnology.O objetivo deste trabalho foi obter e caracterizar uma microemulsão (ME) contendo fenobarbital (FEN). O FEN foi incorporado na proporção de 5% e 10% em um sistema microemulsionado composto por labrasol ® , etanol, miristato de isopropila e água purificada. Foi realizada a caracterização físico-química e avaliada a estabilidade preliminar da ME. Desenvolveu-se um método analítico por espectrofotometria em UV λ = 242 nm. Foi avaliada a cinética de liberação in vitro (em modelo de Franz) da ME e da emulsão (EM) contendo FEN. A incorporação do FEN em ME nas concentrações de 5 e 10% não alterou o pH e a resistência à centrifugação. Houve aumento do tamanho da partícula, redução da condutividade e alteração do índice de refração em relação à ME placebo. A ME manteve-se estável nos ensaios de estabilidade preliminar. O método analítico demonstrou ser específico, linear, preciso, exato e robusto. Na cinética de liberação in vitro, a ME obteve um perfil de liberação in vitro superior a EM contendo FEN. Desta forma, a ME obtida tem potencial para uma futura aplicação transdérmica, podendo compor um sistema de liberação de fármacos para tratamento da epilepsia.Uniterms: Microemulsão/caracterização físico-química. Microemulsão/cinética de liberação in vitro. Fenobarbital/sistema microemulsionado/avaliação. Nanotecnologia.

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“…The DDA assay of the release test samples was performed by high performance liquid chromatography (HPLC) according to a method previously described in the literature (Silva et al, 2009), except that the injection volume of 30 µL was reduced to 20 µL. To verify that the method is suitable for this purpose the linearity, precision and specificity (analyzing the peak purity of the sample chromatograms) were evaluated.…”

Section: Dda Assay Of Release Test Samplesmentioning

confidence: 99%

“…In the case of DDA, reports in the literature indicate that it is very soluble in phosphate buffer pH 7.4, with solubility greater than 6.0 mg.mL -1 (Silva et al, 2009 Zatz and Segers (1998) discuss the selection of data points to calculate the in vitro release rate, and state that there is a time window during which the experiments should be performed. Data should be collected when the influence of the membrane and its associated stagnant layer are no longer present but before excessive drug depletion from semisolid occurs.…”

Section: Calculation Of the Release Rate (Flux)mentioning

confidence: 99%

In vitro release of diclofenac diethylamine from gels: evaluation of generic semisolid drug products in Brazil

Goebel

Sato

Souza

et al. 2013

Braz. J. Pharm. Sci.

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In order for the pharmacological action of a topical dermal drug product to occur, the drug must first be released from the vehicle to be available to penetrate the skin layers and reach the site of action. Drug release is mainly dependent on the characteristics of the formulation. Currently, to register a generic or a similar drug product in Brazil performance testing of topical drug products for local action is not required. In this context, this aim of this study was to evaluate the in vitro release of commercial diclofenac diethylamine gel products available on the Brazilian pharmaceutical market, using the vertical diffusion cell method. Factors which may influence the test, such as the type of membrane used, and the effect of the formulation characteristics on the diffusion rate were evaluated. Brazilian legislation currently allows generic drug products to contain excipients other than the reference drug, which may affect the drug release from the vehicle. Only one of the four generic drug products tested could be considered equivalent to the reference Cataflam Emulgel ® . The cellulose acetate and polyethersulfone membranes tested were found to be interchangeable in the in vitro release studies carried out on this product. Uniterms:In vitro release test. Diclofenac diethylamine/gel. Synthetic membranes. Generic semisolid drug products.Para exercer ação farmacológica, medicamentos tópicos de aplicação cutânea precisam, primeiramente, liberar o fármaco do veículo, para que desta forma ele se torne disponível para penetração nas camadas da pele, até atingir seu local de ação. A liberação do fármaco do veículo depende principalmente das características da formulação. Até a presente data, para registrar um medicamento genérico ou similar no Brasil não se exigem testes de desempenho para produtos tópicos de ação local. O presente trabalho teve como objetivo avaliar a liberação in vitro de especialidades farmacêuticas de diclofenaco dietilamônio gel do mercado farmacêutico brasileiro, usando o sistema de célula de difusão vertical. Avaliaram-se fatores que influenciam o teste como o tipo de membrana usada nos ensaios de liberação e características da formulação que impactam a velocidade de difusão. A legislação vigente no País permite que medicamentos genéricos contenham excipientes diferentes do medicamento referência. Esta diferença afetou a liberação do fármaco do veículo. Dos quatro medicamentos genéricos testados apenas um seria considerado equivalente ao medicamento referência Cataflam Emulgel ® . As membranas de acetato de celulose e polietersulfona testadas apresentaram-se intercambiáveis nos estudos de liberação desse produto.

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Estudo de liberação e permeação in vitro do diclofenaco de dietilamônio em microemulsão gel-like

Cited by 29 publications

References 22 publications

Antifungal activity of topical microemulsion containing a thiophene derivative

Antifungal activity of topical microemulsion containing a thiophene derivative

Phenobarbital loaded microemulsion: development, kinetic release and quality control

In vitro release of diclofenac diethylamine from gels: evaluation of generic semisolid drug products in Brazil

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