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Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different

Sultan M Alshehri1, Faiyaz Shakeel1, Mohamed A Ibrahim1

  • 1Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.

Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society
|February 16, 2019
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Summary

This study developed apigenin (APG) solid dispersions (SDs) to improve oral bioavailability. Microwave and melted techniques significantly enhanced APG dissolution and absorption, offering a promising oral drug delivery system.

Keywords:
ApigeninBioavailabilityMicrowave technologyPluronic-F127Solid dispersion

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Bioavailability Enhancement

Background:

  • Apigenin (APG) is a bioactive nutraceutical with poor solubility and low oral bioavailability.
  • Developing effective oral drug delivery systems for APG is crucial for therapeutic efficacy.

Purpose of the Study:

  • To develop apigenin solid dispersions (SDs) using microwave, melted, and kneaded technologies with pluronic-F127 (PL).
  • To enhance the in vitro dissolution rate and in vivo bioavailability of apigenin upon oral administration.

Main Methods:

  • Solid dispersions (SDs) of APG were prepared using microwave, melted, and kneaded techniques with pluronic-F127 (PL).
  • Characterization involved TGA, DSC, FTIR, PXRD, and SEM.
  • In vitro drug release and in vivo pharmacokinetic studies were conducted in rats.

Main Results:

  • Characterization confirmed the successful formation of APG SDs.
  • In vitro dissolution showed significant APG release from SDs (67.39-84.13%) compared to the control (32.74%).
  • Optimized SDs, particularly from microwave and melted methods, demonstrated significantly improved oral absorption and a 3.19-fold increase in oral bioavailability compared to the commercial capsule.

Conclusions:

  • Developed APG solid dispersion systems effectively enhance dissolution rate and oral absorption.
  • Microwave and melted techniques are suitable for creating advanced oral drug delivery systems for apigenin.
  • These SD systems hold potential for improved therapeutic outcomes of apigenin.