Nanodispersions of taxifolin: Impact of solid-state properties on dissolution behavior

Nanosizing is an advanced formulation approach to address the issues of poor aqueous solubility of active pharmaceutical ingredients. Here we present a procedure to prepare a nanoparticulate formulation with the objective to enhance dissolution kinetics of taxifolin dihydrate, a naturally occurring...

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Bibliographic Details
Published in:International journal of pharmaceutics 2009-07, Vol.377 (1), p.148-152
Main Authors: Shikov, Alexander N., Pozharitskaya, Olga N., Miroshnyk, Inna, Mirza, Sabiruddin, Urakova, Irina N., Hirsjärvi, Samuli, Makarov, Valery G., Heinämäki, Jyrki, Yliruusi, Jouko, Hiltunen, Raimo
Format: Article
Language:English
Subjects:
Chemistry, Pharmaceutical
Drug Carriers - chemistry
Drug Carriers - pharmacokinetics
Drug release kinetics
Freeze Drying
Lyophilization
Molecular Structure
Nanodispersion
Nanoparticles
Nanotechnology - methods
Particle Size
Povidone - chemistry
Quercetin - analogs & derivatives
Quercetin - chemistry
Quercetin - pharmacokinetics
Solid-state properties
Taxifolin
Technology, Pharmaceutical - methods
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Summary:Nanosizing is an advanced formulation approach to address the issues of poor aqueous solubility of active pharmaceutical ingredients. Here we present a procedure to prepare a nanoparticulate formulation with the objective to enhance dissolution kinetics of taxifolin dihydrate, a naturally occurring flavonoid with antioxidant, anti-inflammatory, and hepatoprotective activities. Polyvinylpirrolidone was selected as a carrier and the solid nanodispersions of varying compositions were prepared by a co-precipitation technique followed by lyophilization. The formulation technology reported herein resulted in aggregate-free, spherical particles with the mean size of about 150 nm, as observed by scanning electron microscopy and measured by photon correlation spectroscopy. Furthermore, the co-precipitation process caused taxifolin dihydrate to convert into an amorphous form as verified by X-ray powder diffraction, differential scanning calorimetry, hot stage microscopy and Raman spectroscopy. Finally, in vitro dissolution behavior of the nanodispersion of taxifolin was shown to be superior to that of either pure drug or a drug–polymer physical mixture, reaching 90% of taxifolin released after 30 min. Such enhanced drug release kinetics from the nanodispersion was attributed to both the reduced particle size and the loss of crystallinity.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2009.04.044