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Exploring the Potential of Mesoporous Silica as a Carrier for Puerarin: Characterization, Physical Stability, and In Vivo Pharmacokinetics

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Abstract

The aim of this study was to evaluate the use of a novel porous silica carrier, AEROPERL® 300 Pharma (AP), to improve the in vitro release and oral bioavailability of puerarin (PUE) in solid dispersions (SDs). PUE-AP SD formulations with different ratios of drug to silica (RDS) were prepared by the solvent method. The scanning electron microscopy (SEM) results indicated that the dispersion of PUE improved as the concentration of AP was increased. The differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results revealed that PUE mostly existed in an amorphous state in the SDs. The rate of drug dissolution from the SDs was significantly higher than that from the PUE powder (p < 0.05). The in vitro drug release percentage from the PUE-AP SDs increased as the RDS was reduced. The oral bioavailability of PUE from the SDs improved when using AP, as indicated by AUC(0–∞), which was 2.05 and 2.01 times greater than that of the PUE (API) and PVP K30 SDs, respectively (p < 0.05). The drug content, in vitro release profiles, and the amorphous state of PUE in the PUE-AP SDs showed no significant changes after being stored at room temperature for 6 months or under accelerated conditions (40 ± 2°C, 75 ± 5% relative humidity) for 3 months. AP has a high pore volume, large specific surface area, excellent flowability, and hydrophilic properties, making it capable of improving the dissolution and bioavailability of poorly water-soluble drugs.

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Funding

This study was financially supported by Evonik Specialty Chemicals (Shanghai) Co., Ltd. and the National Natural Science Foundation of China (81603308).

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Zhangjiang Hi-Tech Park, Pudong New District, Shanghai, 201203, China

    Zhi Wang, Bei-Ni Ye, Yong-Tai Zhang, Jian-Xu Xie, Wan-Si Li, Ying Liu & Nian-Ping Feng

  2. Preparation Department, Hangzhou Qingyue Pharmaceutical Technology Co., Ltd., Hangzhou, Zhejiang, China

    Bei-Ni Ye

  3. Resource Efficiency, Evonik Specialty Chemicals (Shanghai) Co., Ltd., Shanghai, China

    Hong-Tao Zhang

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  1. Zhi Wang
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  2. Bei-Ni Ye
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  4. Jian-Xu Xie
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  5. Wan-Si Li
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Correspondence to Nian-Ping Feng.

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All the animal experiments were carried out in accordance with the guidelines of the National Act on the Use of Experimental Animals and were approved by the local ethics committee (SCXK:2013-0016).

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Wang, Z., Ye, BN., Zhang, YT. et al. Exploring the Potential of Mesoporous Silica as a Carrier for Puerarin: Characterization, Physical Stability, and In Vivo Pharmacokinetics. AAPS PharmSciTech 20, 289 (2019). https://doi.org/10.1208/s12249-019-1502-0

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  • DOI: https://doi.org/10.1208/s12249-019-1502-0

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