Micelles of Licorice chalcone A for oral administration: preparation, in vitro, in vivo, and hepatoprotective activity evaluation.

Licorice chalcone A (LCA) possesses a variety of pharmacological activities amid poor solubility in water which consequently restricts its clinical application. In this study, LCA micelles (LCA-M) and LCA micelles modified with TPGS (LCA-M-T) were prepared, wherein in vitro, in vivo, and hepatoprotection potential of the formulations were evaluated. LCA-M-T and LCA-M were prepared by thin-film dispersion method and characterized by a transmission electron microscope (TEM). The encapsulation efficiency, in vitro release, and stability of LCA-M-T and LCA-M were detected by HPLC and UV, respectively. The pharmacokinetics, tissue distribution studies, and pharmacodynamics research were also carried out after oral administration. The sizes of micellar particles were 34.02 ± 0.29 nm (LCA-M) and 62.46 ± 0.51 nm (LCA-M-T) with 0.223 ± 0.021 (LCA-M) and 0.343 ± 0.006 (LCA-M-T) polydispersities, − 35.06 ± 2.27 mV (LCA-M) and − 38.58 ± 1.69 mV (LCA-M-T) zeta potentials, and 95.2 ± 0.27% (LCA-M) and 90.34 ± 0.31% (LCA-M-T) encapsulation efficiencies. The drug loadings were 8.56 ± 0.27% (LCA-M) and 8.04 ± 0.19% (LCA-M-T). The two preparations released quickly and reached over 95% in the four-dissolution media (pH = 1.2 pH = 6.8 pH = 7 pH = 7.4). The preparations of LCA showed significant elevation of cumulative release compared with the free LCA and more importantly 119% (LCA-M) and 285% (LCA-M-T) increments in the relative oral bioavailability of the drug. Preparations of LCA may act as a promising approach to improve solubility and enhance bioavailability and liver protective activity of LCA. [ABSTRACT FROM AUTHOR]