Citation: Zuzheng He, Hui Liu. Application of Macrocyclic Compounds as Drug Solubilizers[J]. Chemistry, ;2021, 84(5): 426-432, 425. shu

Application of Macrocyclic Compounds as Drug Solubilizers

  • Corresponding author: Hui Liu, 2806358119@qq.com
  • Received Date: 7 September 2020
    Accepted Date: 22 December 2020

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  • In the process of drug research and development, the number of compounds with low solubility has increased, and it is urgent to solve the problem of drug solubility in the pharmaceutical industry. Macrocyclic compounds such as cyclodextrin, calixarene and cucurbituril can form host-guest inclusion complex, thus acting as solubilizers for poorly soluble drugs. This paper introduces the application of macrocyclic compounds in improving the solubility of drugs by host-guest interaction. Firstly, due to the differences of macrocyclic compounds in structure and properties, the types of encapsulated drugs are overviewed. Secondly, the host-guest complex by dynamic reversible inclusion can enhance the stability and dissolution rate, thereby further improving the bioavailability of drugs. In addition, the toxicological data of macrocyclic compounds are presented, thus allowing the marketability of macrocyclic compounds as excipients. Lastly, the limitations of macrocyclic compounds as drug solubilizers, such as the restricted dimension of the cavity and the more comprehensive safety assessment are summarized.
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