Preparation, characterisation, and pharmacodynamic study of myricetin pH-sensitive liposomes

Abstract

Aims

Myricetin (MYR) was incorporated into pH-sensitive liposomes in order to improve its bioavailability and anti-hyperuricemic activity.

Methods

The MYR pH-sensitive liposomes (MYR liposomes) were prepared using thin film dispersion method, and assessed by particle size (PS), polydispersed index (PDI), zeta potential (ZP), encapsulation efficiency, drug loading, and in vitro release rate. Pharmacokinetics and anti-hyperuricemic activities were also evaluated.

Results

The PS, PDI, ZP, encapsulation efficiency, and drug loading of MYR liposomes were 184.34 ± 1.05 nm, 0.215 ± 0.005, −38.46 ± 0.30 mV, 83.42 ± 1.07%w/w, and 6.20 ± 0.31%w/w, respectively. The release rate of MYR liposomes was higher than free MYR, wherein the cumulative value responded to pH. Besides, the Cmax of MYR liposomes was 4.92 ± 0.20 μg/mL. The level of uric acid in the M-L-H group (200 mg/kg) was reduced by 54.74%w/v in comparison with the model group.

Conclusion

MYR liposomes exhibited pH sensitivity and could potentially enhance the oral bioavailability and anti-hyperuricemic efficacy of MYR.

Keywords:

• myricetin
• pH-sensitive liposomes
• in vitro release
• bioavailability
• anti-hyperuricemic activity

Disclosure statement

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

Additional information

Funding

This work was supported by the [the National Key Research and Development Program of China #1]under Grant [2018YFE0208600]; [National Natural Science Foundation of China #2] under Grant [81720108030, 8217131836 and 82173785]; [Postdoctoral Research Fund of Jiangsu Province #3] under Grant [2021K010A]; [Natural Science Foundation of the Higher Education Institutions of Jiangsu Province #4] under Grant [18KJB360001]; [Natural Science Foundation of Jiangsu Province #5] under Grant [BK20180866]; [Key Planning Social Development Projects of Zhenjiang in Jiangsu Province #6] under Grant [SH2021024]; [Natural Science Foundation of the Jiangsu Higher Education Institutions #7]; and [National Key Research and Development Program of China #8].