Novel Self-Assembled Ibrutinib-Phospholipid Complex for Potently Peroral Delivery of Poorly Soluble Drugs with pH-Dependent Solubility

@article{Qiu2018NovelSI,
  title={Novel Self-Assembled Ibrutinib-Phospholipid Complex for Potently Peroral Delivery of Poorly Soluble Drugs with pH-Dependent Solubility},
  author={Qiujun Qiu and Mei Lei Lu and Cong Li and Xiang Yong Luo and Xinrong Liu and Ling Hu and Mingqi Liu and Huangliang Zheng and Hongxia Zhang and Min Liu and Chaoyang Lai and Yanzhi Song and Yihui Deng},
  journal={AAPS PharmSciTech},
  year={2018},
  volume={19},
  pages={3571-3583}
}
As an irreversible small-molecule kinase inhibitor, ibrutinib (IBR) exhibits excellent tumor suppression in various tumor cells. However, IBR is insoluble at neutral pH and can dissolve only at low pH: thus, commercial IBR products present poor bioavailability and weakened in vivo antitumor activity. Therefore, we aimed to develop a stable IBR-phospholipid complex (IBR-PC) using egg phosphatidylglycerol (EPG) as excipients to improve the bioavailability of IBR and further enhance its antitumor… CONTINUE READING
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