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Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (2): 99-108.DOI: 10.5246/jcps.2018.02.011

• Original articles • Previous Articles     Next Articles

Preparation, characterization and pharmacokinetic studies of total paeony glycoside nanocrystals

Jinfeng Zhang1, Fan Wu1, Jiayi Han1, Jinghong Rong1, Yi Li1, Yu Liu1, Xiao Liang1, Xin Wang1, Hao Pan1, Hongsheng Liu3, Lijiang Chen1,2*   

  1. 1. School of Pharmaceutical Sciences, Liaoning University, Shenyang 110036, China
    2. Liaoning Key Laboratory of New Drug Research & Development, Shenyang 110036, China
    3. School of Life Sciences, Liaoning University, Shenyang 110036, China
  • Online:2018-03-03 Published:2018-03-01
  • Contact: Tel.: +86-024-62202303, E-mail: chlj16@163.com
  • Supported by:

    Innovation Team Project (Grant No. LT2015011) from the Education Department of Liaoning Province, Important Scientific and Technical Achievements Transformation Project (Grant No. Z17-5-078) and Applied Basic Research Project (Grant No. F16205144) of Science and Technology Bureau of Shenyang, and the Liaoning Provincial Education Department Project of China (Grant No. L2015192).

Abstract:

Total paeony glycoside (TPG) is obtained from Radix Paeoniae Rubra with a variety of bioactivities. However, the low solubility and bioavailability limit its application. The present study aimed to develop TPG nanocrystals to increase the dissolution and then improve the oral bioavailability. TPG nanocrystals were prepared via precipitation and high-pressure homogenization method. The physical-chemical properties of the optimal TPG nanocrystals in terms of particle size, zeta potential, morphology and crystallinity were evaluated. The results showed that TPG nanocrystals had a mean particle size of (210.2±2.5) nm, a polydispersity index of 0.191±0.033 and a zeta potential of (–22.4±1.2) mV. The result of differential scanning calorimetry showed that the nanocrystals were still in crystalline state after the preparation procedure. Transmission electron microscopy (TEM) results showed that the nanosuspension was in spherical shape. The pharmacokinetics of TPG nanocrystals for rats was investigated by liquid chromatography-tandem mass spectroscopy (LC-MS/MS). Compared with the TPG coarse suspension, TPG nanocrystals exhibited significant increase in AUC0–∞ (approximately 1.85-fold). Taken together, TPG nanocrystals could be used as a promising drug delivery system due to the enhanced oral bioavailability of TPG. 

Key words: Total paeony glycoside, Nanocrystals, High-pressure homogenization, Pharmacokinetics, Bioavailability

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