Enhancing the Oral Bioavailability of Biochanin A by Encapsulation in Mixed Micelles Containing Pluronic F127 and Plasdone S630
Overview
Affiliations
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.
Bhalodi K, Kothari C, Butani S Naunyn Schmiedebergs Arch Pharmacol. 2024; .
PMID: 39527309 DOI: 10.1007/s00210-024-03582-x.
Chemical and Biological Properties of Biochanin A and Its Pharmaceutical Applications.
Feng Z, Lai W Pharmaceutics. 2023; 15(4).
PMID: 37111591 PMC: 10143291. DOI: 10.3390/pharmaceutics15041105.
White J, Garza A, Griebler J, Bates F, Calabrese M Langmuir. 2023; 39(14):5084-5094.
PMID: 36971824 PMC: 10593112. DOI: 10.1021/acs.langmuir.3c00088.
Hodel K, Machado B, Sacramento G, Maciel C, Oliveira-Junior G, Matos B Pharmaceutics. 2022; 14(6).
PMID: 35745794 PMC: 9228207. DOI: 10.3390/pharmaceutics14061222.
White J, Calabrese M Colloids Surf A Physicochem Eng Asp. 2022; 638.
PMID: 35221534 PMC: 8880963. DOI: 10.1016/j.colsurfa.2021.128246.