In vitro Penetration and in vivo Distribution of Honokiol into the Intervertebral Disc in Rat

Abstract

Honokiol is a potential candidate for the treatment of intervertebral disc (IVD) degeneration. In this study, we develop in vitro and in vivo methods to detect the distribution of honokiol in intervertebral discs using high-performance liquid chromatography. A rat tail disc was used for both experimental models. For the in vivo animal experiment, blood samples and tail discs were collected at 15, 30, 60, 120 and 240 min after honokiol administration (30 mg/kg, i.v.). The analyte was separated by a mobile phase of methanol and 10 mM NaH2PO4 buffer at pH 2.8 (78:22, v/v) and pumped through a reversed-phase analytical column (250 × 4.6 mm, particle size 5 μm) at room temperature. The in vitro experimental results demonstrated that honokiol diffused into the intervertebral disc and was concentration-dependent. The active concentration is obtained for the therapeutic level at 15 and 30 min after honokiol administration in the in vivo model.

Plant-Derived Senotherapeutics for the Prevention and Treatment of Intervertebral Disc Degeneration and Aging

“…A specific and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed for the identification and quantification of myricetin in the rat plasma after oral and intravenous administrations, which indicated that myricetin would be poorly absorbed in the gastrointestinal tract, possibly due to its low water solubility, low stability in the gastrointestinal fluid and rapid biotransformation [ 300 ]. A validated reversed-phase HPLC method was developed to determine the in vitro penetration and in vivo distribution of honokiol into the IVD, suggesting that the penetration of honokiol into the IVD is sufficient to achieve a therapeutic concentration after honokiol administration [ 301 ].…”

Natural Products of Pharmacology and Mechanisms in Nucleus Pulposus Cells and Intervertebral Disc Degeneration

“…Animal experiments have shown that HKL has a therapeutic effect on IDD. Chen et al [ 77 ] used high-performance liquid chromatography to explore the distribution of HKL in rat intervertebral discs. In vitro analysis showed that HKL diffusion into the discs was concentration-dependent.…”