title: Development of nanosuspension formulation for oral delivery of quercetin.
abstract: With the aim to enhance dissolution rate and oral bioavailability of quercetin, a poorly water-soluble drug, quercetin loaded nanosuspension (QT-NS) was fabricated by a tandem of nano-precipitation (NP) and high pressure homogenization (HPH) method. The formulation of nanosuspension was optimized by screening different stabilizers. Characterization of the original QT powder and QT-NS was carried out by transmission electron microscopy and scanning electron microscopy, X-ray diffraction (XRD) and dissolution tests. QT-NS presented a sphere-like shape under transmission electron microscopy with an average diameter of 393.5 nm and the zeta potential of -35.75 mV. XRD study suggested that QT was maintained in the state of crystalline during the fabrication process. The solubility of QT in nanosuspension was about 70-fold that of crude QT, and the dissolution of QT from QT-NS was increased as compared to that of the original QT powder. In plasma, QT-NS exhibited a significant reduction of clearance rate (2 +/- 0.1 mL/min vs. 15 +/- 4 mL/min) and increase of AUC(0-infinity), (53995 +/- 4126 microg/mL x min versus 3470 +/- 110.1 microg/mL x min) compared with the control suspension. Our results showed that the developed nanosuspension formulation had a great potential as a possible formulation of the poorly water-soluble QT to enhance the bioavailability.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
authors.forename: Min
authors.initials: M
authors.lastname: Sun
authors.forename: Yan
authors.initials: Y
authors.lastname: Gao
authors.forename: Yan
authors.initials: Y
authors.lastname: Pei
authors.forename: Chenyu
authors.initials: C
authors.lastname: Guo
authors.forename: Houli
authors.initials: H
authors.lastname: Li
authors.forename: Fengliang
authors.initials: F
authors.lastname: Cao
authors.forename: Aihua
authors.initials: A
authors.lastname: Yu
authors.forename: Guangxi
authors.initials: G
authors.lastname: Zhai
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D008297:Male; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D036103:Nanotechnology; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011409:Propylene Glycols / Q000737:chemistry; D011794:Quercetin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013535:Suspensions
chemical_list: C116176:PEO-PPO-PEO; D004364:Pharmaceutical Preparations; D011409:Propylene Glycols; D013535:Suspensions; D011092:Polyethylene Glycols; D011794:Quercetin