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Formulation and Characterization of Novel Dry Suspension and Dry Emulsion of 20(S)-Protopanaxadiol

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Abstract

To improve the absorption of poorly water-soluble 20(S)-protopanaxadiol (20(S)-PPD), novel 20(S)-PPD-loaded redispersible dry suspension and dry emulsion were developed in this study. 20(S)-PPD dry suspension (PPD-DS) was prepared by enabling drug fully dispersed with suspending agent Avicel CL611 and solubilizer Poloxamer 188. 20(S)-PPD dry emulsion (PPD-DE) was prepared by employing oleic acid as oil phase, Cremophor RH-40 as surfactant, and n-butyl alcohol as co-surfactant. Both PPD-DS and PPD-DE were evaluated for their physicochemical characterization after being dispersed in distilled water. The in vivo pharmacokinetics was evaluated by UPLC-MS/MS. The droplet size of PPD-DS and PPD-DE was in the scope of 1446–1653 nm and 652.8–784.5 nm. The sedimentation volume ratios of PPD-DS and PPD-DE were both at value of 1. The zeta potential of PPD-DS and PPD-DE were from − 53.7 to − 70.4 mV and − 27.5 to − 34.5 mV, respectively, which indicated stable systems. PPD-DS and PPD-DE both achieved dramatically enhanced aqueous solubility and higher perfusion of 20(S)-PPD in rats’ intestine. Although statistically, no oral bioavailability enhancements of 20(S)-PPD were achieved in PPD-DE and PPD-DS, there were some improvements in the pharmacokinetic behaviors. Especially, PPD-DS could be a promising drug delivery carrier for 20(S)-PPD with the advantages of long-term stability, dosing flexibility, and the convenience of administering to infants and to those who have difficulty swallowing tablets or capsules.

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Acknowledgments

This work was supported by grants from Program of Shanghai Committee of Science and Technology (Grant No. 18401931400), Program of Shanghai Academic/Technology Research Leader (Grant No. 18XD1403700), National Scientific and Technological Major Special Project of China (Grant No. 2018ZX09201008-002), and Scientific Research Program of Shanghai University of Traditional Chinese Medicine (Grant No. 18TS087).

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Authors and Affiliations

  1. Foreign Languages Teaching Center, Shanghai University of Traditional Chinese Medicine, Shanghai, China

    Liying Zhang

  2. Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai, China

    Congcong Xu, Weiwei Wang, Han Han, Yiqiong Pu & Tong Zhang

  3. School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, China

    Congcong Xu, Weiwei Wang & Tong Zhang

  4. Luoxin Biotechnology (Shanghai) Co., Ltd, Shanghai, China

    Jingjing Mao

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  1. Liying Zhang
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Zhang, L., Xu, C., Mao, J. et al. Formulation and Characterization of Novel Dry Suspension and Dry Emulsion of 20(S)-Protopanaxadiol. AAPS PharmSciTech 20, 275 (2019). https://doi.org/10.1208/s12249-019-1487-8

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