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Research Article

Insulin- and quercetin-loaded liquid crystalline nanoparticles: implications on oral bioavailability, antidiabetic and antioxidant efficacy

    Swapnil Singh

    Center for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, SAS Nagar, Punjab 160062, India

    ,
    Varun Kushwah

    Center for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, SAS Nagar, Punjab 160062, India

    ,
    Ashish Kumar Agrawal

    Center for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, SAS Nagar, Punjab 160062, India

    James Graham Brown Cancer Center, University of Louisville, Louisville, KY 40202, USA

    &
    Sanyog Jain

    *Author for correspondence: Tel.: +91 172 229 2055; Fax: +91 172 221 4692;

    E-mail Address: sanyogjain@niper.ac.in

    Center for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, SAS Nagar, Punjab 160062, India

    Published Online:https://doi.org/10.2217/nnm-2017-0278

    Aim: The present study reports insulin (INS)- and quercetin (QT)-lyotropic liquid crystalline nanoparticles (LCNPs) with improved bioavailability, antidiabetic and antioxidant efficacy following oral administration. Materials & methods: The developed INS-QT-LCNPs were evaluated for simulated gastric fluid stability. In vitro Caco-2 uptake studies were also performed. Furthermore, in vivo pharmacokinetics and pharmacodynamics of INS-QT-LCNPs were evaluated. Results & conclusion: INS entrapped within LCNPs demonstrated excellent stability in simulated gastric fluid. Higher uptake of fluorescein isothiocyanate-INS-LCNPs were observed in Caco-2 cells. INS-LCNPs demonstrated approximately 20% relative bioavailability compared with subcutaneously administered INS. Significant decrease in oxidative stress was confirmed by reduction in malondialdehyde level. Overall, combination strategy not only overcomes poor oral bioavailability of INS and QT, but also prevents the generation of reactive oxygen species, responsible for diabetes-mediated complications.

    Graphical abstract

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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