Absorption improvement of tranilast by forming highly soluble nano-size composite structures associated with α-glucosyl rutin via spray drying

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Hideyuki SatoYuichi Tozuka

Abstract

Tranilast (TL) composite particles with α-glucosyl rutin (Rutin-G) were developed to improve the solubility and oral bioavailability of TL. Composite formulation of TL/Rutin-G was prepared using the spray-drying method, and their physicochemical properties were evaluated with respect to the morphology, particle size distribution, solubility and crystallinity. The nanostructure formation of Rutin-G was characterized by dynamic light scattering and transmission electron microscopy when Rutin-G or TL/Rutin-G spray-dried particles (SDPs) were introduced into water. A pharmacokinetic study was also performed to assess the improvement of oral absorption in rats. TL/Rutin-G SDPs were spherical particles with a diameter of 5.5μm. Even in the acidic condition, the remarkable improvement in solubility of TL was achieved, as evidenced by a 32.2-fold increase in solubility compared with untreated TL. The median size of Rutin-G nanostructures in water was 2nm. The formation of Rutin-G nanostructures and their drug inclusion properties may enhance the solubility and dissolution behavior of TL. A drastic increase was found in the exposure of TL in rats, with an increase in Cmax and AUC values of 114- and 36.4-fold, respectively, compared with...Continue Reading

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Citations

Sep 19, 2015·International Journal of Pharmaceutics·Juan DuYancai Wang
May 5, 2016·International Journal of Pharmaceutics·Gintare LeonaviciuteAndreas Bernkop-Schnürch
Aug 20, 2016·Journal of Pharmaceutical Sciences·Hiroshi UedaYuichi Tozuka
Jan 31, 2017·Journal of Agricultural and Food Chemistry·Hideyuki SatoSatomi Onoue
Jan 27, 2017·Drug Development and Industrial Pharmacy·Mohammed ManiruzzamanDennis Douroumis
Jan 27, 2018·Journal of Radiation Research·Yasushi AizawaMitsuru Uesaka
Jun 29, 2021·Advanced Drug Delivery Reviews·Danielle BrainNeill J Liptrott

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