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Self-Double-Emulsifying Drug Delivery System Enteric-Coated Capsules: A Novel Approach to Improve Oral Bioavailability and Anti-inflammatory Activity of Panax notoginseng Saponins

  • Research Article
  • Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract
  • Published:
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Abstract

In this work, self-double-emulsifying drug delivery system enteric-coated capsules (PNS-SDE-ECC) were used to enhance the oral bioavailability and anti-inflammatory effects of Panax notoginseng saponins (PNS), which are rapidly biodegradable, poorly membrane permeable, and highly water-soluble compounds. The PNS-SDEDDS formulated by a modified two-step method spontaneously emulsified to W/O/W double emulsions in the outer aqueous solution, which significantly promoted the absorption of PNS in the intestinal tract. The release study revealed that PNS-SDE-ECC exhibited sustained release of PNS within 24 h and the stability study indicated that PNS-SDE-ECC were stable at room temperature for up to 3 months. Furthermore, compared to PNS gastric capsules, the relative bioavailability of NGR1, GRg1, GRe, GRb1, and GRd in PNS-SDE-ECC was increased by 4.83, 10.78, 9.25, 3.58, and 4.63 times, respectively. More importantly, PNS-SDE-ECC significantly reduced OXZ-induced inflammatory damage in the colon by regulating the expression of TNF-α, IL-4, IL-13, and MPO cytokines. Overall, the prepared PNS-SDE-ECC may serve as a viable vehicle for increasing the oral bioavailability of PNS and its anti-inflammatory action on ulcerative colitis.

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Data Availability

The data that support the findings of this study are available from the corresponding author upon reasonable request.

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Acknowledgements

The authors would like to thank the Shanghai University of Traditional Chinese Medicine Ethics Committee for their kind guidance in the animal experiments, the Shanghai University of Traditional Chinese Medicine for providing the technical platform, and the Guangxi Wuzhou Pharmaceutical (Group) Co., Ltd for providing funding support.

Funding

This work was supported by Guangxi Wuzhou Pharmaceutical (Group) Co., Ltd. (E4-D200004).

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Authors and Affiliations

  1. The MOE Key Laboratory for Standardization of Chinese Medicines and the SHTCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, 201210, China

    Yaru Wang, Yunxia Shang, Fengyu Tang, Kun Qiu, Xiaohui Wei & Zhengtao Wang

  2. Shanghai R&D Center for Standardization of Chinese Medicines, Shanghai, 201210, China

    Yaru Wang, Yunxia Shang, Fengyu Tang, Kun Qiu, Xiaohui Wei & Zhengtao Wang

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  1. Yaru Wang
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  2. Yunxia Shang
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  3. Fengyu Tang
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  4. Kun Qiu
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  5. Xiaohui Wei
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Contributions

Yaru Wang performed most of the experiments and data collection, analyzed the data, and wrote the manuscript. Yunxia Shang, Fengyu Tang, and Kun Qiu participated in completing the study of the ulcerative colitis experiment. Xiaohui Wei designed the experiments, supervised the study, and contributed to the finalizing of the manuscript. Zhengtao Wang provided valuable comments on the experimental design. All authors reviewed the manuscript and agreed to the published version of the manuscript.

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Correspondence to Xiaohui Wei.

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Wang, Y., Shang, Y., Tang, F. et al. Self-Double-Emulsifying Drug Delivery System Enteric-Coated Capsules: A Novel Approach to Improve Oral Bioavailability and Anti-inflammatory Activity of Panax notoginseng Saponins. AAPS PharmSciTech 24, 90 (2023). https://doi.org/10.1208/s12249-023-02549-0

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