Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 105, Issue 1, Pages 242-249Publisher
WILEY-BLACKWELL
DOI: 10.1016/j.xphs.2015.10.002
Keywords
nanotechnology; oral drug delivery; drug transport; dissolution; physical characterization; stabilization; bioavailability; oral absorption; pharmacokinetics; pharmacodynamics
Funding
- Priority Academic Program Development (PAPD) fund of Jiangsu Higher Education Institution
- Natural Science Foundation of Jiangsu Province [BK20141465]
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The aim of this study was to investigate the potential of nanosuspensions (NSs) in improving the dissolution and absorption of poorly water-soluble ginkgo lactones (GLs), including ginkgolide A, ginkgolide B, and ginkgolide C. Liquid GL-NSs were prepared by a combined bottom-up and top-down approach with response surface methodology design, followed by freeze-drying solidification. Physicochemical characterization of the prepared freeze-dried GL-NSs was performed by photon correlation spectroscopy, scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry. In vitro dissolution and in vivo bioavailability of ginkgolide A, ginkgolide B, and ginkgolide C in freeze-dried GL-NSs were evaluated with GLs coarse powder as control. Their inhibitory effects on platelet aggregation were also comparatively analyzed. GLs existed in an amorphous state in the prepared freeze-dried GL-NSs. The particle size, polydispersity index, zeta potential, and redispersibility index of freeze-dried GL-NSs were around 286 nm, 0.26, -25.19 mV, and 112%, respectively. The particle size reduction resulted in much more rapid and complete dissolution of ginkgolides from GL-NSs than coarse powder. Comparison with GLs coarse powder, freeze-dried GL-NSs showed a significant decreased T-max, 2-fold higher peak concentration, and 2-fold higher area under plasma concentrations curve for 3 ginkgolides and exhibited significantly higher antiplatelet aggregation effect. (C) 2016 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
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