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AAPS PharmSciTech

, Volume 19, Issue 8, pp 3631–3649 | Cite as

Nano-lipid Complex of Rutin: Development, Characterisation and In Vivo Investigation of Hepatoprotective, Antioxidant Activity and Bioavailability Study in Rats

  • G. S. Ravi
  • R. Narayana Charyulu
  • Akhilesh Dubey
  • Prabhakara Prabhu
  • Srinivas Hebbar
  • Avril Candida Mathias
Research Article Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery
  • 71 Downloads
Part of the following topical collections:
  1. Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery

Abstract

The current study was aimed to develop an amphiphilic drug-lipid nano-complex of rutin:egg phosphatidylcholine (EPC) to enhance its poor absorption and bioavailability, and investigated the impact of the complex on hepatoprotective and antioxidant activity. Rutin nano-complexes were prepared by solvent evaporation, salting out and lyophilisation methods and compared for the complex formation. For the selected lyophilisation method, principal solvent DMSO, co-solvent (t-butyl alcohol) and rutin:EPC ratios (1:1, 1:2 and 1:3) were selected after optimisation. The properties of the nano-complexes such as complexation, thermal behaviour, surface morphology, molecular crystallinity, particle size, zeta potential, drug content, solubility, in vitro stability study, in vitro drug release, in vitro and in vivo antioxidant study, in vivo hepatoprotective activity and oral bioavailability/pharmacokinetic studies were investigated. Rutin nano-complexes were developed successfully via the lyophilisation method and found to be in nanometric range. Rutin nano-complexes significantly improved the solubility and in vitro drug release, and kinetic studies confirmed the diffusion-controlled release of the drug from the formulation. The nano-complex showed better antioxidant activity in vitro and exhibited well in vitro stability in different pH media. The in vivo study showed better hepatoprotective activity of the formulation compared to pure rutin at the same dose levels with improved oral bioavailability. Carbon tetrachloride (CCl4)-treated animals (group II) failed to restore the normal levels of serum hepatic marker enzymes and liver antioxidant enzyme compared to the nano-complex-treated animals. The results obtained from solubility, hepatoprotective activity and oral bioavailability studies proved the better efficacy of the nano-complex compared to the pure drug.

KEY WORDS

antioxidant bioavailability hepatoprotective lyophilisation rutin 

Notes

Acknowledgments

The authors acknowledge Nitte (Deemed to be University), Mangaluru, Karnataka, India, for providing the facilities to carry out this work. The authors are also thankful to Lipoid®, GmbH, Germany, for providing the EPC (Lipoid® E 80 S) as a gift sample for this research work. Facilities provided towards the research work by Mangalore University, National Institute of Technology, Karnataka (NITK) and Manipal Academy of Higher Education are also gratefully acknowledged.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  1. 1.Department of Pharmaceutics, NGSM Institute of Pharmaceutical SciencesNitte (Deemed to be University)MangaluruIndia
  2. 2.Department of PharmaceuticsShree Devi College of PharmacyMangaluruIndia

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