title: Enhanced oral bioavailability of glycyrrhetinic acid via nanocrystal formulation.
abstract: The purpose of this study was to prepare solid nanocrystals of glycyrrhetinic acid (GA) for improved oral bioavailability. The anti-solvent precipitation-ultrasonication method followed by freeze-drying was adopted for the preparation of GA nanocrystals. The physicochemical properties, drug dissolution and pharmacokinetic of the obtained nanocrystals were investigated. GA nanocrystals showed a mean particle size of 220 nm and shaped like short rods. The analysis results from differential scanning calorimetry and X-ray powder diffraction indicated that GA remained in crystalline state despite a huge size reduction. The equilibrium solubility and dissolution rate of GA nanocrystal were significantly improved in comparison with those of the coarse GA or the physical mixture. The bioavailability of GA nanocrystals in rats was 4.3-fold higher than that of the coarse GA after oral administration. With its rapid dissolution and absorption performance, the solid nanocrystal might be a more preferable formulation for oral administration of poorly soluble GA.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia, 750004, China.
authors.forename: Yaya
authors.initials: Y
authors.lastname: Lei
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia, 750004, China.
authors.forename: Yindi
authors.initials: Y
authors.lastname: Kong
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia, 750004, China.|Ningxia Engineering and Technology Research Center for Modernization of Hui Medicine, Yinchuan, Ningxia, 750004, China.|Key Lab of Hui Ethnic Medicine Modernization, Ministry of Education, Yinchuan, Ningxia, 750004, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Sui
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia, 750004, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Feng
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia, 750004, China.
authors.forename: Rongyue
authors.initials: R
authors.lastname: Zhu
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia, 750004, China. wpwang2015@126.com.|Ningxia Engineering and Technology Research Center for Modernization of Hui Medicine, Yinchuan, Ningxia, 750004, China. wpwang2015@126.com.|Key Lab of Hui Ethnic Medicine Modernization, Ministry of Education, Yinchuan, Ningxia, 750004, China. wpwang2015@126.com.
authors.forename: Wenping
authors.initials: W
authors.lastname: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D065546:Drug Liberation; D006034:Glycyrrhetinic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D051381:Rats; D012995:Solubility
chemical_list: D006034:Glycyrrhetinic Acid
keywords: Anti-solvent precipitation; Bioavailability; Glycyrrhetinic acid; Nanocrystal; Oral administration; Ultrasonication