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Nanosuspension Development of scutellarein as an active and rapid orally absorbed precursor of its BCS class IV glycoside scutellarin
Yang X.2; Miao X.2; Cao F.1; Li S.2; Ai N.2; Chang Q.I.1; Lee S.M.Y.2; Zheng Y.2
2014
Source PublicationJournal of Pharmaceutical Sciences
ISSN15206017 00223549
Volume103Issue:11Pages:3576-3584
Abstract

This work addressed solubility and membrane permeability problems of Biopharmaceutics Classification System (BCS) Class IV glycoside scutellarin (SG) by developing a nanosuspension of its aglycone scutellarein (S) as a precursor. An S nanosuspension containing poloxamer 188 was prepared using antisolvent precipitation where hydroxypropyl-β-cyclodextrin was utilized as a lyophilizing protectant. Particle size and polydispersity index after redispersion were 342.6 ± 18.2 and 0.32 ± 0.06 nm, respectively. The dissolution rate of the S nanosuspension was superior compared with the physical mixture. No free S, but SG and SG's isomer were detected in plasma following oral delivery of SG or S, S nanosuspension or physical mixture of S. The C values of SG after dosing with the S nanosuspension were 12.0, 8.0, and 4.5-fold higher than the SG, S, or physical mixture, respectively. The T and mean residence time (MRTlast ) of SG after dosing with the S nanosuspension were significantly shorter than S and SG. Treatments with SG, S, or S nanosuspensions reduced the hemorrhage rate in a zebrafish model, but the S nanosuspension exhibited the strongest rescue effect. This study highlights a new strategy to circumvent BCS Class IV flavonoid glycosides using a formulation of their aglycone as a precursor to accelerate oral absorption and improve bioactivity.

KeywordAbsorption Cerebral Hemorrhage Metabolism Nanotechnology Oral Drug Delivery Precursor Scutellarin (Sg) Solubility Zebrafish
DOI10.1002/jps.24149
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS SubjectChemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
WOS IDWOS:000344145200024
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Cited Times [WOS]:8   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Chinese Academy of Medical Sciences
2.University of Macau
First Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Yang X.,Miao X.,Cao F.,et al. Nanosuspension Development of scutellarein as an active and rapid orally absorbed precursor of its BCS class IV glycoside scutellarin[J]. Journal of Pharmaceutical Sciences,2014,103(11):3576-3584.
APA Yang X..,Miao X..,Cao F..,Li S..,Ai N..,...&Zheng Y..(2014).Nanosuspension Development of scutellarein as an active and rapid orally absorbed precursor of its BCS class IV glycoside scutellarin.Journal of Pharmaceutical Sciences,103(11),3576-3584.
MLA Yang X.,et al."Nanosuspension Development of scutellarein as an active and rapid orally absorbed precursor of its BCS class IV glycoside scutellarin".Journal of Pharmaceutical Sciences 103.11(2014):3576-3584.
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