Degradation kinetics of mometasone furoate in aqueous systems

Teng, Xiao Wei; Cutler, David C; Davies, Neal M.

doi:10.1016/s0378-5173(03)00226-6

Cited by 36 publications

(33 citation statements)

References 41 publications

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“…When the higher dose was used the cells were also occluded with Parafilm to maintain fixed boundary conditions. Furthermore, MF has very low water solubility and degrades at pH values above 4.9 [10]. To overcome these restrictions, we decided to use isotonic 20 mM citrate buffer (pH 4.5) mixed with 30 % (v/v) ethanol as receptor media.…”

Section: /7mentioning

confidence: 99%

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Topical Administration of Mometasone Furoate - A Combined Impedance Spectroscopy and In Vitro Drug Diffusion Study

Runnsjö¹

2015

JAPLR

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Section: /7mentioning

confidence: 99%

“…The low risk of side effects is largely due to the high lipophilicity (lg P 4.5), resulting in low solubility in aqueous fluids such as blood. Systemic uptake is further reduced by the ability of MF to degrade in aqueous solvents at pH values above 4.9 [10].…”

Section: Introductionmentioning

confidence: 99%

Topical Administration of Mometasone Furoate - A Combined Impedance Spectroscopy and In Vitro Drug Diffusion Study

Runnsjö¹

2015

JAPLR

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“…The MF presents their maximum stability in acidic conditions (Teng et al, 2003). In order to access the pH values stability of the emulsions, this parameter was evaluated during 60 d (Table 2).…”

Section: Physical and Chemical Stability Of Emulsionsmentioning

confidence: 99%

“…Mometasone furoate (MF) is a potent corticosteroid which presents an improved risk/benefit ratio. It is, therefore, of great value for inflammatory skin diseases, showing a strong anti-inflammatory action, rapid onset of action, and low systemic bioavailability after topical application (Teng et al, 2003;Valotis et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

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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“…Enhanced stability of the compound has also been found in gel formulations as compared to that of the cream formulations. The photostability of drugs has been evaluated with various stabilizers for creams containing ascorbic acid (9) and other drugs (10)(11)(12). Steroidal drugs in topical formulations have been stabilized against light using different techniques such as spectral overlay with suitable stabilizers, inclusion into liposomes, and protection with light-blocking agents (4,(13)(14)(15).…”

Section: Introductionmentioning

confidence: 99%

Photodegradation and Stabilization of Betamethasone-17 Valerate in Aqueous/Organic Solvents and Topical Formulations

et al. 2012

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Abstract. The effects of solvent [acetonitrile, methanol, and acetonitrile/water mixture (20:80, v/v)], buffer concentration (phosphate buffer, pH7.5), ionic strength and commonly employed adjuvants on the photodegradation of betamethasone-17 valerate in cream and gel formulations have been studied on exposure to UV light (300-400 nm). A validated high-performance liquid chromatography method has been used to determine the parent compound and its photodegraded products. The photodegradation data in the studied solvents showed greater decomposition of the drug in solvents with a lower dielectric constant. A comparatively higher rate of photodegradation was observed in the cream formulation compared to that for the gel formulation. The kinetic treatment of the photodegradation data revealed that the degradation of the drug follows first-order kinetics and the apparent first-order rate constants for the photodegradation reactions, in the media studied, range from 1.62 to 11.30×10. The values of the rate constants decrease with increasing phosphate concentration and ionic strength which could be due to the deactivation of the excited state and radical quenching. The second-order rate constant (k′) for the phosphate ion-inhibited reactions at pH 7.5 has been found to be 5.22×10−2 M −1 s −1 . An effective photostabilization of the drug has been achieved in cream and gel formulations with titanium dioxide (33.5-42.5%), vanillin (21.6-28.7%), and butyl hydroxytoluene (18.2-21.6%).

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Degradation kinetics of mometasone furoate in aqueous systems

Cited by 36 publications

References 41 publications

Topical Administration of Mometasone Furoate - A Combined Impedance Spectroscopy and In Vitro Drug Diffusion Study

Topical Administration of Mometasone Furoate - A Combined Impedance Spectroscopy and In Vitro Drug Diffusion Study

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

Photodegradation and Stabilization of Betamethasone-17 Valerate in Aqueous/Organic Solvents and Topical Formulations

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