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Liquiritin-Hydroxypropyl-Beta-Cyclodextrin Inclusion Complex: Preparation, Characterization, Bioavailability and

Qilong Wang1, Kangyi Zhang1, Wen Weng1

  • 1Department of Pharmaceutics, School of Pharmacy, Centre for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.

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|April 3, 2022
PubMed
Summary

This study developed a liquiritin-hydroxypropyl-beta-cyclodextrin (LT-HP-β-CD) complex to improve liquiritin

Keywords:
Anti-tumorBioavailabilityHP-β-CDLiquiritinPharmacokinetics

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Natural Product Chemistry

Background:

  • Liquiritin (LT) exhibits valuable pharmacological activities.
  • However, its therapeutic potential is hindered by poor water solubility and low oral absorption.
  • Developing strategies to enhance LT's bioavailability is crucial for its clinical application.

Purpose of the Study:

  • To prepare and characterize a liquiritin-hydroxypropyl-beta-cyclodextrin inclusion complex (LT-HP-β-CD).
  • To evaluate the impact of this complexation on LT's water solubility, oral bioavailability, and antitumor efficacy.
  • To establish LT-HP-β-CD as a promising drug delivery system for liquiritin.

Main Methods:

  • Preparation of LT-HP-β-CD using the saturated aqueous solution method.
  • Characterization of the complex using SEM, IR, XRD, and DSC.
  • In vitro drug release studies, in vivo pharmacokinetic analysis, and in vitro antitumor assays using A549 lung cancer cells.

Main Results:

  • Successful formulation of LT-HP-β-CD confirmed by physicochemical characterization.
  • Significantly enhanced in vitro drug release and oral bioavailability of LT from the complex compared to free LT.
  • Remarkable potentiation of the antitumor effect of LT against A549 lung cancer cells when formulated as LT-HP-β-CD.

Conclusions:

  • LT-HP-β-CD inclusion complex formation effectively improves liquiritin's water solubility and oral bioavailability.
  • The developed complex demonstrates enhanced antitumor activity, suggesting improved therapeutic efficacy.
  • LT-HP-β-CD serves as a viable carrier for enhancing liquiritin's pharmaceutical properties and therapeutic outcomes.