In vitro release of diclofenac diethylamine from caprylocaproyl macrogolglycerides based microemulsions

Djordjevic, Ljiljana; Primorac, Marija; Stupar, M.

doi:10.1016/j.ijpharm.2005.02.014

Cited by 81 publications

(42 citation statements)

References 18 publications

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“…The maximum flux value of diclofenac diethylamine was obtained from w/o microemulsion containing the highest percentage of water. 15 In this study, MP has the highest water content and highest flux value of DS among the formulations studied and this fact supports the observation above (Table 3). This observation also agrees with the earlier study, which indicated that the release rate of diclofenac diethylammonium from the investigated systems depends significantly on the water volume fractions.…”

Section: Resultssupporting

confidence: 90%

“…3,4 There are many studies on microemulsions as topical drug delivery vehicles, and it has been shown that microemulsion formulations have improved transdermal and dermal delivery properties. [5][6][7][8][9][10][11][12][13][14][15][16] In this study, non-ionic surfactants (Brij 58 and Span 80), which are also compatible with the other 3 classes of surfactants and retain this utility over a broad range of pH values, were used in preference, because they have minimal toxicity. 3,4 As the study aimed to examine the in vitro release of microemulsion (M) formulations, diclofenac sodium (DS) was selected as a model drug.…”

Section: Introductionmentioning

confidence: 99%

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Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Kantarcı¹,

Özgüney²,

Karasulu³

et al. 2007

AAPS PharmSciTech

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The aim of the present study was to make a comparison of the in vitro release rate of diclofenac sodium (DS) from microemulsion (M) vehicles containing soybean oil, nonionic surfactants (Brij 58 and Span 80), and different alcohols (ethanol [E], isopropyl alcohol [I], and propanol [P]) as cosurfactant. The optimum surfactant:cosurfactant (S:CoS) weight ratios and microemulsion areas were detected by the aid of phase diagrams. Three microemulsion formulations were selected, and their physicochemical properties were examined for the pH, viscosity, and conductivity. According to the release rate of DS, M prepared with P showed the significantly highest flux value (0.059 ± 0.018 mg/cm 2 /h) among all formulations (P G .05). The conductivity results showed that DS-loaded microemulsions have higher conductivity values (18.8-20.2 microsiemens/cm) than unloaded formulations (16.9-17.9 microsiemens/cm), and loading DS into the formulation had no negative effect on system stability. Moreover, viscosity measurements were examined as a function of shear rate, and Newtonian fluid characterization was observed for each microemulsion system. All formulations had appropriate observed pH values varying from 6.70 to 6.85 for topical application. A skin irritation study was performed with microemulsions on human volunteers, and no visible reaction was observed with any of the formulations. In conclusion, M prepared with P may be a more appropriate formulation than the other 2 formulations studied as drug carrier for topical application.

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Section: Resultssupporting

confidence: 90%

Section: Introductionmentioning

confidence: 99%

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Kantarcı¹,

Özgüney²,

Karasulu³

et al. 2007

AAPS PharmSciTech

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“…The maximised NE region was observed at S/CoS ratio 1 : 1 with highest oil solubilisation (29% w/w) at a relatively low surfactant mixture of 62% w/w. Probably, Õ (PEG-20 castor oil) at equal mixture with Acconon CC6 Õ forms more flexible surfactant/co-surfactant interfacial film, which determines the existence of NE region [41]. Similar observation was reported previously that at equal mass ratio of surfactant/co-surfactant mixture maximised NE region which could be attributed to maximum oil solubility at optimum surfactant/co-surfactant ratio [23].…”

Section: Construction Of Pseudo-ternary Phase Diagramssupporting

confidence: 83%

Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

Rizwan¹,

Aqil²,

Azeem³

et al. 2010

Journal of Experimental Nanoscience

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The aim of the present study was to develop nanoemulsion as a possible vehicle for enhanced transdermal penetration of carvedilol (CVD). For screening of nanoemulsion components, solubility of CVD in oils, surfactants and co-surfactants was determined. Various surfactants and co-surfactants were screened for their ability to nanoemulsify the selected oily phases. The obtained results indicated that Acconon CC6Õ had shown good nanoemulsification efficiency (minimum surfactant required S min ¼ 46.52% w/w) among the selected surfactants and further improved in presence of Õ (S min ¼ 37.11% w/w). The ranges of nanoemulsion existence were delineated through the construction of the pseudo-ternary phase diagram at different ratio of surfactant mixture (S/ CoS), and various nanoemulsions were selected from phase diagram of S/CoS ratio 1 : 1. The effect of content of oil and S/CoS (1 : 1) on the skin permeation of CVD was evaluated through an excised wistar rat skin using Franz diffusion cell. All the nanoemulsions showed a high skin permeation rate (92.251-161.53 mg/ cm 2 /h), good enhancement ratio (3.5-6.2) and high permeability coefficient in comparison to control groups. The optimised nanoemulsion formulation with the highest skin permeation rate (161.53 mg/cm 2 /h) consisted of 0.25% w/w CVD, 12.5% w/w Miglyol 810 Õ , 50% w/w Acconon CC6 Õ /CO-20 Õ (1 : 1) and water. The above formulation had the smallest mean globules size (9.28 nm). The superior transdermal flux of CVD may be due to nanorange size of oil globules that lead to intimate contact with the skin layer. These studies suggest that the nanoemulsion system is a promising vehicle for the transdermal delivery of CVD.

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“…15 Provavelmente, a liberação do DDA da MEG, comparada com o emulgel genérico, foi dificultada pelas combinações moleculares do DDA com a fração aquosa e interface do sistema, o qual causou um incremento da viscosidade formando uma malha gelificada que dificultou sua liberação. Esse resultado está em concordância com Djordjevic et al, 15 que relatam que ME contendo um glicerídeo cáprico caprílico e poligliceril-6 dioleato, associado com miristato de isopropila, pode dificultar a liberação de drogas anfifílicas por interações moleculares.…”

Section: Caracterização Físico-química Da Megunclassified

“…5,7 Além disso, o DDA apresenta metabolismo hepático, tempo de meia-vida curto, 14 não sofre metabolismo na pele, não induz tolerância e tem bom coeficiente de partição. 15 Com base nas colocações acima e na importância do tema, o objetivo do presente trabalho foi a obtenção e a caracterização de uma ME, na forma gel (MEG) contendo DDA, como sistema promotor de permeação do fármaco, e a avaliação do seu perfil de liberação e permeação in vitro em comparação a uma formulação convencional emulgel comercial genérico.…”

Section: Introductionunclassified

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

Silva¹,

Santana²,

Bedor³

et al. 2009

Quím. Nova

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Recebido em 25/3/08; aceito em 25/2/09; publicado na web em 3/7/09 IN VITRO RELEASE AND PERMEATION OF A DICLOFENAC DIETHYLAMINE FROM MICROEMULSION GEL-LIKE.The goal of this study was to produce and characterize a new microemulsion gel-like carrier system (MEG) by using the pseudoternary phase-diagram concept. The diclofenac diethylamine (DDA) was incorporated in the MEG and its in vitro release and permeation profiles were performed using Franz-type diffusion cells. The results revealed that the commercial DDA emulgel provided significantly higher K p of DDA (2.2-fold) as compared to the MEG. Similar data were obtained in the permeation studies in which DDA K p 4.7-fold higher. Therefore, MEG presents higher potential as a topical delivery system for DDA when compared to the commercial DDA emulgel.Keywords: diclofenac diethylamine; in vitro release; microemulsion gel-like. INTRODUÇÃOA administração tópica é conhecida como via alternativa da administração oral de ativos medicamentosos e oferece muitas vantagens como a ausência de efeito de primeira passagem, o fato de ser indolor e a facilidade de aplicação. 1 Todavia, uma eficácia tópica só é obtida a partir de fármacos potentes com adequado grau de penetração na pele. 2 Isto tem levado a um crescente interesse pela utilização de promotores de permeação em formulações tópicas, assim como o uso de sistemas de liberação de fármacos com esta capacidade promotora de permeação. 3 As microemulsões (ME) são dispersões isotrópicas, transparentes, termodinamicamente estáveis, usualmente formadas por misturas de quatro componentes, água, óleo, tensoativo e cotensoativo. Apresentam grande potencial como sistemas de liberação e de direcionamento de fármacos, pelas propriedades de solubilizar fármacos hidrofílicos em meio lipofílico, lipofílicos em meio aquoso e anfifílicos na interface óleo/água. 4-10 Além disso, estes sistemas apresentam capacidade de se formarem espontaneamente, podendo existir sob várias formas estruturais (globular a/o e o/a, bicontínuas, cúbicas ou lamelares), 11,12 e atuam como promotores de permeação de vários fármacos, devido ao reduzido tamanho das gotículas formadas, assim como ao seu alto conteúdo de tensoativo, que desorganiza os lipídeos da pele. 5 O diclofenaco de dietilamônio (DDA) é um anti-inflamatório não esteroidal (AINEs) capaz de formar micelas e cristais líquidos liotrópicos em água. 13 Apresenta a capacidade de interagir com os fosfolipídeos da pele, contribuindo para aumentar a fluidez do mesmo no estrato córneo, fazendo com que os lipídios passem de uma forma cristalina ordenada para uma forma líquida desordenada, aumentando, portanto, a permeabilidade cutânea. 5,7 Além disso, o DDA apresenta metabolismo hepático, tempo de meia-vida curto, 14 não sofre metabolismo na pele, não induz tolerância e tem bom coeficiente de partição. 15 Com base nas colocações acima e na importância do tema, o objetivo do presente trabalho foi a obtenção e a caracterização de uma ME, na forma gel (MEG) contendo DDA, como sistema promotor de permeação do f...

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In vitro release of diclofenac diethylamine from caprylocaproyl macrogolglycerides based microemulsions

Cited by 81 publications

References 18 publications

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

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

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