cg9b00249_si_001.pdf (1.25 MB)
Cocrystal of Apigenin with Higher Solubility, Enhanced Oral Bioavailability, and Anti-inflammatory Effect
journal contribution
posted on 2019-09-18, 21:13 authored by Xiao-Qin Ma, Chong Zhuang, Bi-Chuan Wang, Yuan-Feng Huang, Qing Chen, Ning LinApigenin
(4′,5,7-trihydroxyflavone, APG) is a bioflavonoid
found in some herbs, vegetables, and fruits. APG can reduce inflammation,
which is associated with many chronic aging diseases. However, the
solubility and bioavailability of APG is quite low; thus, its utility
in the body is questionable. Herein, a new cocrystal (APG-BPY) assembled
by
APG and BPY (4,4′-bipyridine) has been successfully prepared.
A single-crystal structure of this cocrystal was illustrated, and
comprehensive characterizations were performed in detail. In aqueous
buffer, experiments with the dissolution profile of APG-BPY showed
that the maximum concentration of APG is approximately ∼40
times higher than that of APG raw material. This result yielded an
optimized pharmacokinetics performance, as demonstrated by the improved
relative bioavailability of Frel = 3.9.
Furthermore, the anti-inflammatory response in vivo was evaluated
by pharmacodynamic experiments; the percentage inhibition of inflammation
was 56% for APG-BPY, in comparison with 26% of pure APG. The enhanced
efficacy and low toxicity results indicate the development of a pharmaceutically
acceptable form of APG that may be potentially clinically available.