Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol

Abstract

The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in Polygonum cuspidatum extract (PCE) by hot melt extrusion (HME). In addition, the role of the auxiliary substances in PCE was also studied. The solid dispersion of Polygonum cuspidatum extract was prepared by hot-melt extrusion. The optimum formula was selected by single factor design and orthogonal test. The optimum formula was barrel temperature 140 °C, screw rotation speed 40 rpm/min, and the ratio of Polygonum cuspidatum extract to HPMCAS was 1:2. The dissolution test showed that PCE-SD increased the dissolution of RES from 46.75 ± 0.47% to 130.06 ± 0.12%. The pharmacokinetics curve of rats showed that PCE-SD increased AUC0-t of RES from 111,471.22 ± 11.4% to 160,458.968 ± 15.7%, indicating an approximately 1.44-fold increase in absorption. In addition, the rotation speed of PCE-SD screw is less than that of RES-SD screw. The bioavailability of PCE-SD was slightly better than that of RES-SD. PCE-SD is more hygroscopic than RES-SD. PCE-SD increased the solubility and oral bioavailability of RES. The auxiliary substances in Polygonum cuspidatum extract have influence on its preparation technology, stability, and bioavailability.

Accelerated Oral Healing by Angelica gigas Nakai from Hot Melt Extrusion Technology: An In Vitro Study

“…A previous study regarding HME-orientated antihypertensive molecules revealed high levels of bioavailability in a rat model [28]. Another study on HME-orientated resveratrol confirmed an improvement in the solubility and oral bioavailability of resveratrol [29]. A previous animal study also confirmed improvements in the oral bioavailability and biological effects of cyclosporine through HME [30].…”

The genus Polygonum: An updated comprehensive review of its ethnomedicinal, phytochemical, pharmacological activities, toxicology, and phytopharmaceutical formulation

“… PCE-SD improved RES's oral bioavailability and solubility. [ 246 ] AUC0-t: the extrapolated area under the concentration-time curve; CPP: cell-penetrating peptide; EtOH: ethanol; HUVECs: human umbilical vein endothelial cells; H 2 O: water; IC50: half-maximal inhibitory concentration; MeOH: methanol; RES: resveratrol; SD: solid dispersion. …”