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Development, characterisation, and in vitro anti-tumor effect of self-microemulsifying drug delivery system containing polyphyllin I

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Abstract

Polyphyllin I (PPI), an effective active ingredient in Paris polyphylla, has a diverse set of pharmacological properties. However, due to its poor solubility and oral absorption, its application and development are limited. In the study, we were committed to improving the solubility of PPI by developing a self-microemulsifying drug delivery system of PPI (PPI-SMEDDS), screening the best preparation process, and evaluating the quality and the in vivo pharmacokinetics of PPI, and PPI-SMEDDS following oral administration to rats were also studied. In addition, the pharmacological activities against human lung adenocarcinoma cell A549 in vitro were assessed. The best formulation had 15.89% ethyl oleate, 47.38% Cremophor RH40, and 36.73% 1,2 propylene glycol. The produced PPI-SMEDDS was clear and transparent, with an average particle size of 24.51 nm and a zeta potential of −17.54 ± 0.51 mV. In vitro, the cumulative release rate of PPI-SMEDDS was nearly 80% within 2 h. PPI-SMEDDS had a substantially greater area under the curve than PPI following oral treatment in rats, and the relative bioavailability of PPI in rats was 278.99%. More importantly, the anti-tumor effect of PPI-SMEDDS in vitro was significantly greater than that of PPI. These findings suggested that PPI-SMEDDS has the potential to improve the solubility, oral bioavailability of PPI, and anti-tumor effect, laying the groundwork for future research on the new PPI dosage form.

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Acknowledgements

The authors are sincerely thankful to the Animal Experiment Center, Affiliated Hospital of Shandong University of Traditional Chinese Medicine for providing the facility for carrying out the research work.

Funding

This study was supported by the National Natural Science Foundation of China (81873330, 82104506, and 82074066).

Author information

Author notes

  1. Xin Wang, Rui Zhang, and Shu Wang contributed equally to this work.

Authors and Affiliations

  1. Grade Three Laboratory of Traditional Chinese Medicine Preparation of the National Administration of Traditional Chinese Medicine, Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, 250014, China

    Xin Wang, Minju Gu, Yuan Li, Peimin Yang, Gongling Guo & Ping Sun

  2. School of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China

    Xin Wang, Rui Zhang, Xiuping Zhuang, Chao Chen & Peimin Yang

  3. Institute of Chinese Medicine Resources, Shandong Academy of Chinese Medicine, Jinan, 250014, China

    Shu Wang

Authors
  1. Xin Wang
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  2. Rui Zhang
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  4. Minju Gu
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  5. Yuan Li
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Contributions

Conceptualization, Xin Wang and Ping Sun; Methodology, Rui Zhang and Shu Wang; Data curation, Minju Gu and Yuan Li; Software, Xiuping Zhuang and Chao Chen; Writing-original draft, Xin Wang and Rui Zhang; Writing- review & editing, Peimin Yang and Gongling Guo. All authors have read and agreed to the published version of the manuscript.

Corresponding authors

Correspondence to Gongling Guo or Ping Sun.

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Ethics approval and consent to participate

All animal protocols were approved by the Animal Center, Beijing SPF Weitonglihua Laboratory Animal Technology Co., Ltd. (Beijing, Certificate No. SCXK 2016–0006). All institutional and national guidelines for the care and use of laboratory animals were followed.

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The authors declare no competing interests.

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Wang, X., Zhang, R., Wang, S. et al. Development, characterisation, and in vitro anti-tumor effect of self-microemulsifying drug delivery system containing polyphyllin I. Drug Deliv. and Transl. Res. 13, 356–370 (2023). https://doi.org/10.1007/s13346-022-01212-8

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