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Nanocrystals for Improving Oral Bioavailability of Drugs: Intestinal Transport Mechanisms and Influencing Factors

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Abstract

With the limitation of solubility and dissolution rate of insoluble drugs, following oral administration, they would rifely prove poor and volatile bioavailability, which may fail to realize its therapeutic value. The drug nanocrystals are perceived as effective tactic for oral administration of insoluble drugs attributes to possess many prominent properties such as elevating dissolution rate and saturation solubility, high drug loading capacity, and improving oral bioavailability. Based on these advantages, the application of nanocrystals in oral drug delivery has acquired significant achievement, and so far more than 20 products of drug nanocrystals have been confirmed in the market. However, the oral absorption of drug nanocrystals is still facing huge challenges due to the limitation of many factors. Intrinsic properties of the drugs and complex physiological environment of the intestinal tract are the two most important factors affecting the oral bioavailability of drugs. In addition, the research on the multi-aspect mechanisms of nanocrystals promoting gastrointestinal absorption and bioavailability has been gradually deepened. In this review, we summarized recent advances of the nanocrystals delivered orally, and provided an overview to the research progress for crossing the intestinal tract transport mechanisms of the nanocrystals by some new research techniques. Meanwhile, the factors relevant to the transport of drug nanocrystals were also elaborated in detail.

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Funding

This work was supported by the National Natural Science Foundations of China (81860628), and Ningxia Key Research and Development Projects (No. 2019BEG03038).

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  1. Zonghua Tian and Yaping Mai contributed equally to this work.

Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, China

    Zonghua Tian, Tingting Meng, Shijie Ma & Jianhong Yang

  2. Department of Medical Science and Technology Research Center, Ningxia Medical University, Yinchuan, China

    Yaping Mai

  3. Department of Medical Chemistry, School of Basic Medicine, Ningxia Medical University, Yinchuan, China

    Guojing Gou

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  1. Zonghua Tian
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  2. Yaping Mai
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Correspondence to Guojing Gou or Jianhong Yang.

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Tian, Z., Mai, Y., Meng, T. et al. Nanocrystals for Improving Oral Bioavailability of Drugs: Intestinal Transport Mechanisms and Influencing Factors. AAPS PharmSciTech 22, 179 (2021). https://doi.org/10.1208/s12249-021-02041-7

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