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Fabrication of Stable Apigenin Nanosuspension with PEG 400 as Antisolvent for Enhancing the Solubility and Bioavailability

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Abstract

The purpose of this paper is to prepare a stable apigenin nanosuspension with a drug concentration of 1.11 mg/mL through green and efficient antisolvent method. Compared with the traditional preparation process that may use toxic reagents, in this study, a green and effective strategy was applied for the preparation of stable apigenin nanosuspension by using an antisolvent method with PEG 400 as antisolvent to improve the solubility and bioavailability. It was found that the particle size of apigenin nanosuspension was about 280 nm, and the solubility and dissolution of the nanosuspension were 33 and 3 times higher than that of the apigenin, respectively. Pharmacokinetic study showed that the Cmax and AUC 0–8 h values of the nanosuspension in fasting rats achieved about 6- and 2.5-fold enhancement than that of the apigenin, respectively. Stability test showed that the apigenin nanosuspension could be stored stably for 12 months at 25℃. Taken together, the antisolvent method with PEG 400 was proven to be a green and effective method to prepare the stable nanosuspension of poorly soluble drugs.

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Funding

This work was supported by grants from Qing Miao Plan of Hubei University of Chinese Medicine (1008010511).

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Author notes

  1. Renjie Xu and Cuiping Jiang contributed equally to this work.

Authors and Affiliations

  1. School of Pharmacy, Hubei University of Chinese Medicine, Wuhan, 430065, People’s Republic of China

    Renjie Xu, Lijing Zhou, Bin Li, Yi Hu, Yujie Guo, Xuecheng Xiao & Shan Lu

  2. School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, 510515, People’s Republic of China

    Cuiping Jiang

  3. Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Southern Medical University, Guangzhou, 510515, People’s Republic of China

    Cuiping Jiang

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  1. Renjie Xu
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  4. Bin Li
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Contributions

Conceptualization: Shan Lu and Xuechen Xiao. Methodology: Lijing Zhou and Renjie Xu. Formal analysis and investigation: Yi Hu and Bin Li. Writing-original draft preparation: Renjie Xu. Writing-review and editing: Cuiping Jiang and Yujie Guo. Funding acquisition: Yujie Guo and Shan Lu. Resources: Yujie Guo and Shan Lu. Supervision: Shan Lu and Xuechen Xiao. All authors read and approved the final manuscript.

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Correspondence to Yujie Guo, Xuecheng Xiao or Shan Lu.

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Xu, R., Jiang, C., Zhou, L. et al. Fabrication of Stable Apigenin Nanosuspension with PEG 400 as Antisolvent for Enhancing the Solubility and Bioavailability. AAPS PharmSciTech 23, 12 (2022). https://doi.org/10.1208/s12249-021-02164-x

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