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Naringenin-Loaded Nanoparticles Improve the Physicochemical Properties and the Hepatoprotective Effects of Naringenin in Orally-Administered Rats with CCl4-Induced Acute Liver Failure

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Abstract

Purpose

A novel naringenin-loaded nanoparticles system (NARN) was developed to resolve the restricted bioavailability of naringenin (NAR) and to enhance its hepatoprotective effects in vivo on oral administration.

Materials and methods

Physicochemical characterizations of NARN included assessment of particle size and morphology, powder X-ray diffraction, fourier transform infrared spectroscopy, and dissolution study. In addition, to evaluate its bioactivities and its oral treatment potential against liver injuries, we compared the hepatoprotective, antioxidant, and antiapoptotic effects of NARN and NAR on carbon tetrachloride (CCl4)-induced hepatotoxicity in rats.

Results

NARN had a significantly higher release rate than NAR and improved its solubility. NARN also exhibited more liver-protective effects compared to NAR with considerable reduction in liver function index and lipid peroxidation, in conjunction to a substantial increase in the levels of the antioxidant enzymes (P < 0.05). Moreover, NARN was able to significantly inhibit the activation of caspase-3, -8, and -9 signaling, whereas NAR only markedly inhibited caspase-3 and -9 (P < 0.05).

Conclusion

NARN effectively improved the release of NAR which resulted in more hepatoprotective effects mediated by its antioxidant and antiapoptotic properties. These observations also suggest that nanoformulation can improve the free drug’s bioactivity on oral administration.

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Acknowledgements

The authors would like to thank Mrs. Shui-Chin Lu (Department of Medical Research, Kaohsiung Medical University) for technical support with the TEM. This study was supported by a research grant from the National Science Council of Taiwan (NSC 97-2313-B-037-001-MY3).

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Authors and Affiliations

  1. Faculty of Pharmacy, College of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 807, Taiwan

    Feng-Lin Yen, Tzu-Hui Wu, Thau-Ming Cham & Chun-Ching Lin

  2. Department of Microbiology and Immunology, Dalhousie University, Halifax, Nova Scotia, Canada

    Liang-Tzung Lin

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  1. Feng-Lin Yen
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  2. Tzu-Hui Wu
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Correspondence to Thau-Ming Cham or Chun-Ching Lin.

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Feng-Lin Yen and Tzu-Hui Wu contributed equally to this work.

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Yen, FL., Wu, TH., Lin, LT. et al. Naringenin-Loaded Nanoparticles Improve the Physicochemical Properties and the Hepatoprotective Effects of Naringenin in Orally-Administered Rats with CCl4-Induced Acute Liver Failure. Pharm Res 26, 893–902 (2009). https://doi.org/10.1007/s11095-008-9791-0

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