Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

Fini, Adamo; Bergamante, Valentina; Ceschel, G. C.; Ronchi, Celestino; Moraes, Carlos Alberto Fonseca de

doi:10.1208/s12249-008-9107-z

Cited by 47 publications

(42 citation statements)

References 15 publications

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“…It was been demonstrated that, at a given concentration, the release is ordinarily faster from the vehicle in which the drug is completely solubilized (Katz & Poulsen, 1972). As demonstrated in previous studies (Raghavan et al, 2001;Fini et al, 2008), MF is insoluble in water and exponentially increases as the amount of glycol is increased. It was shown that in co-solvent mixtures, the solubility of MF was similar for the two glycols, around 3 mg/100 mL.…”

Section: Discussionsupporting

confidence: 71%

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

et al. 2014

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Over the years, research has focused on strategies to increase benefit/risk ratio of corticoids. However, vehicles intended for topical glucocorticoids delivery with an improved benefit/risk ratio are still on demand. The aim of this work was the in vitro and in vivo characterization of cold processed oil-in-water (o/w) emulsions intended for mometasone furoate (MF) delivery to induce drug targeting to upper skin strata, decreasing adverse effects. Two o/w emulsions, containing 0.1% of MF, were developed differing in the glycol used (2-methyl-2,4-pentanediol -PT and ethoxydiglycol -TC emulsions). In vitro permeation studies revealed that these emulsions are suitable vehicles for the delivery of MF containing ingredients which are responsible for a drastically increased on the permeability coefficients of MF from a theoretical value of 1.18 Â 10 À4 cm/h to 5.20 Â 10 À4 AE 2.05 Â 10 À4 cm/h and 6.30 Â 10 À4 AE 2.94 Â 10 À4 cm/h, for PT and TC, respectively. The tape stripping results showed that the amount of drug that reached the viable skin layers was very low (1.99 %) and the amount that remained in the stratum corneum (SC) was 10.61%. The in vivo studies showed that the developed formulations decreased the edema and erythema in mice skin in more that 90%, assuring, at least, the same anti-inflammatory effect compared with the commercial cream. PT placebo demonstrated to contribute to restore the skin barrier by increasing the amount of lipids within the human skin.

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Section: Discussionsupporting

confidence: 71%

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

et al. 2014

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“…Our results also demonstrated that the penetration-enhancing effect of ME-hi was significantly higher than ME-lo at 8-12 h postapplication, but affected PGT and ADN delivery differently. A possible explanation for the superiority of ME-hi may rely on differences in the internal structure of the two microemulsions, which leads to different drug release from the formulations and, consequently, different skin penetration (2,11,21). This possibility, however, is not supported by our observation that both microemulsions provided similar release profiles of PGT and ADN.…”

Section: Discussionmentioning

confidence: 59%

Microemulsions Containing Medium-Chain Glycerides as Transdermal Delivery Systems for Hydrophilic and Hydrophobic Drugs

et al. 2009

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Abstract. We evaluated the ability of microemulsions containing medium-chain glycerides as penetration enhancers to increase the transdermal delivery of lipophilic (progesterone) and hydrophilic (adenosine) model drugs as well as the effects of an increase in surfactant blend concentration on drug transdermal delivery. Microemulsions composed of polysorbate 80, medium-chain glycerides, and propylene glycol (1:1:1, w/w/w) as surfactant blend, myvacet oil as the oily phase, and water were developed. Two microemulsions containing different concentrations of surfactant blend but similar water/oil ratios were chosen; ME-lo contained a smaller concentration of surfactant than ME-hi (47:20:33 and 63:14:23 surfactant/oil/water, w/w/w). Although in vitro progesterone and adenosine release from ME-lo and MEhi was similar, their transdermal delivery was differently affected. ME-lo significantly increased the flux of progesterone and adenosine delivered across porcine ear skin (4-fold or higher, p<0.05) compared to progesterone solution in oil (0.05±0.01 μg/cm 2 /h) or adenosine in water (no drug was detected in the receptor phase). The transdermal flux of adenosine, but not of progesterone, was further increased (2-fold) by ME-hi, suggesting that increases in surfactant concentration represent an interesting strategy to enhance transdermal delivery of hydrophilic, but not of lipophilic, compounds. The relative safety of the microemulsions was assessed in cultured fibroblasts. The cytotoxicity of ME-lo and ME-hi was significantly smaller than sodium lauryl sulfate (considered moderate-to-severe irritant) at same concentrations (up to 50 μg/mL), but similar to propylene glycol (regarded as safe), suggesting the safety of these formulations.

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“…Microemulsions are emulsions producing a transparent product that has a very small droplet size and does not have tendency to coalesce. A large amount of drug can in fact be incorporated in these formulations, Due to the high solubilising capacity of hydrophobic drugs [10]. …”

Section: Microemulsionmentioning

confidence: 99%

Effect of Penetration Enhancer DMSO on In-Vitro Skin Permeation of Acyclovir Transdermal Microemulsion Formulation.

Kumar¹,

Jain²,

Prajapati³

2011

Int J Drug Del

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The aim of this research was to enhance the flux of transdermal drug delivery by using penetration enhancers DMSO. Skin penetration enhancers have been used to improve bioavailability and increase the range of drugs for which topical and transdermal delivery is a viable option which penetrate into skin to reversibly decrease the barrier resistance. Penetration enhancing activity of dimethylsulphoxide (DMSO) at 5% w/w and 10% w/w concentration were determined in aqueous solution of ACV and in microemulsion formulations though calculation of transdermal flux of ACV with Keshary Chein Frenz Diffusion cell by using wistar albino rat skin. The transdermal flux of formulations PD, PD5D, PD10D, ME1 and ME10D was found to be 2.47, 50.7529, 119.7691, 238.1432 and 266.6721µg/cm 2 /h. The flux of microemulsion formulation ME10D was found 266.6721± 8.49 µg/cm 2 /h. Which showed highest value and skin flux of the drug could be enhanced up to 107 fold compared to its aqueous solution by preparing microemulsion ME10D. DMSO in microemulsion formulation is safe to the skin at 10% DMSO w/w.

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Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

Cited by 47 publications

References 15 publications

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

Microemulsions Containing Medium-Chain Glycerides as Transdermal Delivery Systems for Hydrophilic and Hydrophobic Drugs

Effect of Penetration Enhancer DMSO on In-Vitro Skin Permeation of Acyclovir Transdermal Microemulsion Formulation.

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