Cocrystallization as a novel approach to enhance the transdermal administration of meloxicam

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Tatiane Cogo MachadoThiago Caon

Abstract

Despite its large effectiveness, the long-term oral administration of high doses of meloxicam (MLX) may lead to gastrointestinal events such as abdominal pain, diarrhea, dyspepsia, ulceration, hemorrhage, and gastrointestinal perforation. Moreover, the pH-dependent solubility of MLX makes the development of new oral formulations even more challenging. As an alternative to overcome these limitations, the transdermal delivery of this drug has been purposed. Although various physical and chemical approaches to enhance the absorption of MLX may be found in literature, the use of cocrystallization has not been reported so far. Cutaneous permeation of MLX and 1:1 meloxicam-salicylic acid cocrystal (MLX-SLC) were evaluated using Franz diffusion cells. Cocrystal was suspended in an aqueous solution and in a gel to evaluate the vehicle effect on permeation parameters. In aqueous medium, the cocrystallization showed to enhance the drug permeation coefficient from 1.38 to 2.15 × 10-3 cm/h. MLX-SLC generated supersaturation with respect to the drug during dissolution studies simulating the conditions in the Franz cell donor chamber. This greater amount of free drug in the solution could contribute to explain the higher transdermal absorpti...Continue Reading

Citations

Aug 20, 2019·Chemphyschem : a European Journal of Chemical Physics and Physical Chemistry·Jean QuertinmontBenoît Champagne
May 31, 2021·Journal of Pharmaceutical and Biomedical Analysis·Marina AntonioRubén M Maggio
Jul 25, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ilma Nugrahani, Rismaya Desti Parwati

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