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

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Zou L., Xiong S., Deng X., Liu J., Xiong R., Wang Z., Cao X., Chen Y., Guo Y., Tang G.

Acta Poloniae Pharmaceutica - Drug Research

2018

vol. 75

issue 6

1305-1312

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.

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1 Acta Poloniae Pharmaceutica - Drug Research

1 2018

1 Cao X.

1 Chen Y.

1 Deng X.

1 Guo Y.

1 Liu J.

1 Tang G.

1 Wang Z.

1 Xiong R.

1 Xiong S.

1 Zou L.

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