Preparation of scutellarin loaded TPGS polymeric micelles and evaluation of its pharmacokinetics and pharmacodynamics effects in rats

• Authors: Liu Zou , Shujuan Xiong , Xiangping Deng , Juan Liu , Runde Xiong , Zhe Wang , Xuan Cao , Yanming Chen , Yu Guo , Guotao Tang
• Languages of publication: EN

Abstracts

EN

To improve the clinical effect of scutellarin by extending the action time in vivo, scutellarin loaded polymeric micelles were developed by D-alpha tocopherol polyethylene glycol 1000 succinate (Scu/TPGS). Scu/TPGS were prepared using film solvent diffusion methods and characterized on the basis of their particle size, zeta potential, and drug encapsulation efficiency. Dynamic dialysis was used to study the release behavior of the polymeric micelles in vitro. Its pharmacokinetic characteristics and antithrombotic efficacy were studied by intravenous injection in rats. The results showed that Scu/TPGS were spherical, 20.09±2.62 nm in size and a slow release in vitro. The pharmacokinetic parameter T1/2 of Scu/TPGS was 762.12±46.56 min compared with commercial injection of 59.30±10.67 min (p<0.05). At the 1 mg/kg dose, the thrombolysis effect of micellar group was stronger than that of the commercial group (p<0.05). In conclusion, TPGS polymer micelles provided a valid strategy in chemotherapy for cerebrovascular diseases with poor water solubility and poor lipid solubility drugs such as scutellarin.

Keywords

EN

scutellarin; TPGS; polymeric micelles; antithrombotic drugs

• Journal: Acta Poloniae Pharmaceutica - Drug Research
• Year: 2018
• Volume: 75
• Issue: 6
• Pages: 1305-1312

Dates

published

2018-12-31

Contributors

author

Liu Zou

author

Shujuan Xiong

author

Xiangping Deng

author

Juan Liu

author

Runde Xiong

author

Zhe Wang

author

Xuan Cao

author

Yanming Chen

author

Yu Guo

author

Guotao Tang

Identifiers

DOI

10.32383/appdr/92248