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Authors Wu X, Ge W, Shao T, Wu W, Hou J, Cui L, Wang J, Zhang Z
Received 18 October 2016
Accepted for publication 11 January 2017
Published 22 February 2017 Volume 2017:12 Pages 1475—1483
DOI https://doi.org/10.2147/IJN.S125041
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Jiang Yang
Peer reviewer comments 2
Editor who approved publication: Dr Linlin Sun
Abstract: Biochanin A (BCA), a natural dietary isoflavone, has been reported to
show anticancer activities. However, its low biological availability and poor
aqueous solubility limit its usefulness as a chemotherapeutic agent. We
developed BCA-loaded micelles with Pluronic F127 and Plasdone S630 (BCA-FS).
The optimized, spherical-shaped BCA-FS was obtained at a ratio of 1:1
(F127:S630). The particle size was 25.17±1.2 nm, and the zeta potential was −10.9±0.24
mV. BCA solubility in water increased to 5.0 mg/mL after encapsulation, and the
drug-loading efficiency was 5.88%±0.76%. In vitro release experiments showed a
delayed release of BCA from the mixed micelles. Furthermore, the BCA absorption
permeability across a Caco-2 cell monolayer from the apical side to the
basolateral side increased by 54% in BCA-FS. A pharmacokinetics evaluation
showed a 2.16-fold increase in the relative oral bioavailability of BCA-FS
compared with raw BCA, indicating that the mixed micelles may promote
absorption in the gastrointestinal tract. A gastrointestinal safety assay was
used to assess the reliability and safety of BCA-FS. On the basis of these
findings, we conclude that this simple nanomicelle system could be leveraged to
deliver BCA and other hydrophobic drugs.
Keywords: biochanin
A, mixed micelles, oral bioavailability, Pluronic F127, Plasdone S630