Transdermal drug delivery using microemulsion and aqueous systems: Influence of skin storage conditions on the in vitro permeability of diclofenac from aqueous vehicle systems

Sintov, Amnon; Botner, Shafir

doi:10.1016/j.ijpharm.2005.12.019

Cited by 154 publications

(108 citation statements)

References 39 publications

Supporting

Mentioning

103

Contrasting

Unclassified

Order By: Relevance

“…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%

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

View full text Add to dashboard Cite

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.

show abstract

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

View full text Add to dashboard Cite

show abstract

“…It seems that the mechanism by which hydrophobic drugs such as diclofenac penetrate the skin depends on drug-vehicle interaction (Sintov and Botner, 2006). Therefore, the permeation of the drug from the aqueous control was higher compared with the Voltaren ® gel.…”

Section: Discussionmentioning

confidence: 99%

“…The diffusion area was 3.8 cm 2 and the receiver compartment volume was 30 mL. The environmental parameters selected were previously used by Sintov and Botner, (2006). Briefly, the porcine skin surface was maintained at 32 °C and PBS (pH 7.4) was used in the receiver compartment.…”

Section: Permeation Experimentsmentioning

confidence: 99%

Gellan gum fluid gels for topical administration of diclofenac

Mahdi

Conway

Mills

et al. 2016

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Diclofenac topical formulations are often preferred for drug administration to patients who experience serious GIT problems. Absorption of the drug through the skin, however, can be challenging due to the natural protective feature of the stratum corneum (SC). In this article, fluid gels prepared from gellan gum were explored as a topical drug delivery vehicle.Rheological analysis of the formulations showed that it was possible to produce a topical gel with a viscosity and the mechanical strength similar to that of the commercially available

show abstract

“…Microemulsion formulations can increase drug transdermal permeation, as has been demonstrated in numerous studies (Kreilgaard, Pedersen, Jaroszewski, 2000;Sintov, Sharipo, 2004;Hua et al, 2004;Sintov, Botner, 2006;Sintov, Brandys-Sitton, 2006;Heuschkel, Goebel, Neubert, 2008;Azeem et al, 2009;Neubert, 2011). Several hypotheses have been put forward for the mechanism of drug permeation enhancement.…”

Section: Introductionmentioning

confidence: 94%

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

Pascoa

Diniz

Florentino

et al. 2015

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

This article reports the development of a pharmaceutical product containing vegetable actives from a Brazilian medicinal plant. The possibility of forming a microemulsion using Pterodon emarginatus ("sucupira") oil was evaluated and the anti-inflammatory potential of this microemulsion was also examined. A formulation was developed using P. emarginatus oil, a mixture of ethoxylated Castor Oil (Ultramone ® R-540/propylene glycol 2:1) (surfactant/cosurfactant) and distilled water at a ratio of 10:15:75, respectively. The microemulsion which was selected was then subjected to the preliminary stability test and analyzed in terms of average diameter of droplets, pH, zeta potential, and polydispersity index, on the 1 st , 7 th , 15 th , and 30 th days after preparation and stored at different temperatures (5 ± 2 °C, 25 ± 2 °C, and 40 ± 2 °C). The anti-inflammatory in vivo activity of both oil and formulation were evaluated, using the experimental model of croton oil-induced ear edema. The preliminary stability test showed that the microemulsion stored at 5 and 25 °C retained its original features throughout the 30-day period. The anti-inflammatory potential of both oil and formulation was shown to be statistically significant (p < 0.001), when compared to the control group, however, the microemulsion proved to be more effective (p < 0.05) than the oil when applied directly to the ear. Descrevemos o desenvolvimento de um produto farmacêutico contendo ativo vegetal baseado em uma planta medicinal brasileira. Foi avaliada a habilidade de formação de uma microemulsão à base do óleo de Pterodon emarginatus (sucupira) e seu potential anti-inflamatório. Uma formulação foi desenvolvida utilizando o óleo de P. emarginatus, mistura de óleo de mamona etoxilado (Ultramona ® R-540)/propilenoglicol (2:1) (tensoativo/cotensoativo) e água destilada, na proporção de 10:15:75, respectivamente. A microemulsão selecionada foi submetida ao teste preliminar de estabilidade e foi analisada quanto ao diâmetro médio das gotículas, pH, potential zeta e índice de polidispersão, no 1º, 7º, 15º e 30º dias após o preparo e foram estocadas em diferentes temperaturas (5±2 °C, 25±2 °C e 40±2 °C). Avaliaram-se a atividade anti-inflamatória in vivo do óleo de sucupira e da formulação, usando o modelo experimental do edema de orelha induzido pelo óleo de cróton. No teste preliminar de estabilidade observou-se que a formulação estocada a 5 °C e a 25 °C mantiveram suas características originais durante 30 dias. O potencial anti-inflamatório de ambos, óleo de sucupira e formulação foi estatisticamente significativo (p <0.001), quando comparado ao controle, porém a microemulsão foi mais eficiente (p <0.05) que o óleo aplicado diretamente nas orelhas dos animais. Unitermos:Pterodon emarginatus/pharmacognosy. Pterodon emarginatus/óleo/atividade antiinflamatória. Plantas medicinais. Microemulsão. Fitoterápico. Tecnologia farmacêutica.

show abstract

Transdermal drug delivery using microemulsion and aqueous systems: Influence of skin storage conditions on the in vitro permeability of diclofenac from aqueous vehicle systems

Cited by 154 publications

References 39 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

Gellan gum fluid gels for topical administration of diclofenac

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

Contact Info

Product

Resources

About