Hyperoside-loaded TPGs/mPEG-PDLLA self-assembled polymeric micelles: preparation, characterization and in vitro/in vivo evaluation

Abstract

Hyperoside (Hyp) self-assembled polymeric micelles (Hyp-PMs) were purposely developed to enhance aqueous solubility, in vivo availability and anti-oxidative effect of Hyp. In preparing Hyp-PMs, we employed the thin film dispersion method with the micelles consisting of TPGs and mPEG2000-PDLLA3000. The particle size, polydispersity index and zeta potential of Hyp-PMs were 67.42 ± 1.44 nm, 0.229 ± 0.015 and −18.67 ± 0.576 mV, respectively, coupled with high encapsulation efficiency （EE）of 90.63 ± 1.45% and drug loading (DL) of 6.97 ± 1.56%. Furthermore, the value of critical micelle concentration (CMC) was quite low, which indicated good stability and improved self-assembly ability of Hyp-PMs. Also, trend of in vitro Hyp release from Hyp-PMs demonstrated enhanced solubility of Hyp. Similarly, in comparison with free Hyp, oral bioavailability of Hyp-PMs was improved (about 8 folds) whilst half-life of Hyp-PMs was extended (about 3 folds). In vitro anti-oxidative effect showed obvious strong scavenging DPPH capability of Hyp-PMs, which may be attributed to its smaller size and better solubility. Altogether, Hyp-PMs may serve as a possible strategy to potentially enhance aqueous solubility, bioavailability and anti-oxidative effect of Hyp, which may play a key role in Hyp application in the pharmaceutical industries.

Graphical Abstract

Keywords:

• Hyperoside
• TPGs
• mPEG-PDLLA
• critical micelle concentration (CMC)
• Bioavailability
• In vitro release
• antioxidant effect

Acknowledgements

We are grateful to the Pharmacy Institute at Jiangsu University, Zhenjiang-China, for supplying the requisite logistics that enabled us to write this manuscript. Also, the authors thank the Care and Use Committee for Animal Experiments.

Ethics statement

We followed the guidelines laid down for care and use of animals in the laboratory by national and institutional agencies.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This work was funded by National Key R&D Program of China [grant numbers: 2018YFE0208600], National Natural Science Foundation of China [grant numbers: 81720108030 and 8217131836], Jiangsu Postdoctoral Research Foundation [grant numbers:2021K010A], Natural Science Foundation of Jiangsu Province [grant numbers: BK20180866], Natural Science Foundation of Jiangsu Universities [grant numbers: 18KJB360001], and Key planning social development projects of Zhenjiang in Jiangsu Province [grant numbers:SH2021024].