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

作者：Xu, Renjie; Jiang, Cuiping; Zhou, Lijing; Li, Bin; Hu, Yi; Guo, Yujie^*; Xiao, Xuecheng^*; Lu, Shan^*

来源：AAPS PHARMSCITECH, 2021, 23(1): 12.

DOI：10.1208/s12249-021-02164-x

• nanosuspension
• polyethylene glycol 400
• solubility
• stability

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 C-max 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 25celcius. 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.

• 单位
  南方医科大学