Pinocembrin polymeric micellar drug delivery system: preparation, characterisation and anti-hyperuricemic activity evaluation

Abstract

Aim: Hydrophobic pinocembrin (PCB) was incorporated into a new nano-drug delivery system to enhance solubility, bioavailability and anti-hyperuricemic activity of the drug.

Methods: We fabricated PCB loaded polymeric micelles (PCB-FPM) by thin film dispersion method and appropriately determined their physical characteristics. The oral relative bioavailability and anti-hyperuricemic activity of PCB-FPM and free PCB were observed.

Results: The optimum particle size of the micelles was 19.90 ± 0.93 nm. PCB-FPM exhibited great stability within 18 days, coupled with lower cytotoxicity and higher biocompatibility. Moreover, the percent cumulative release of PCB-FPM was much higher than free PCB in the dissolution media. The oral bioavailability of PCB-FPM was increased by 2.61 times compared with free PCB. Uric acid (UA) level of rats was reduced in PCB-FPM group (200 mg/kg) by 78.82% comparable to the model control.

Conclusion: PCB-FPM may become an ideal strategy to increase oral in-vivo availability and anti-hyperuricemic activity of PCB.

Keywords:

• Pinocembrin
• polymer micelles
• oral bioavailability
• anti-hyperuricemic activity

Disclosure statement

No conflicting interest was declared by the author(s).

Additional information

Funding

This work was supported by the [National Key R&D Program of China #1] under Grant [2018YFE0208600]; [National Natural Science Foundation of China #2] under Grant [81720108030]; [National Natural Science Foundation of China #3] under Grant [8217131836]; [Postdoctoral Research Fund of Jiangsu Province in 2021 category A #4] under Grant [2021K010A]; [Natural Science Foundation of the Higher Education Institutions of Jiangsu Province #5] under Grant [18KJB360001]; [Natural Science Foundation of Jiangsu Province #6] under Grant [BK20180866] and [Key planning social development projects of Zhenjiang in Jiangsu Province #7] under Grant [SH2021024].