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Development of quercetin nanoformulation and in vivo evaluation using streptozotocin induced diabetic rat model

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Abstract

Quercetin-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (Qu-NP) were prepared by emulsion–diffusion–evaporation method and characterized as 179.9 ± 11.2 nm in size with 0.128 as polydispersity index, more than 86% drug entrapment efficiency, and zeta potential was −6.06 ± 1.51 mV. d-Trehalose (5% w/v) was found to be a suitable cryoprotectant for lyophilization of Qu-NP, and antioxidant assays indicated that Qu-NP were able to retain the antioxidant property similar to that of free drug at equivalent concentration after formulation development. In vitro release study of Qu-NP showed a controlled release pattern of quercetin. An enhanced oral bioavailability (523% relative increase) was observed in pharmacokinetic study with a 6-day sustained release from Qu-NP as compared to quercetin suspension, which indicated the reduced dosing frequency. Efficacy in diabetic rats suggested that same dose of Qu-NP on every fifth day was sufficient to bring effect similar to daily dose of oral quercetin suspension, and the same effect was also observed for catalase and superoxide dismutase levels in pancreas and kidneys. Thus, the system offers an efficacious oral therapy with reduced dose and dosing frequency for treatment of diabetes and is hence patient compliant.

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Acknowledgments

DC and AM are thankful for their research associate ship award to Department of Biotechnology (DBT) and Council of Scientific and Industrial Research (CSIR) respectively to carry out this research. NK is thankful to NIPER for financial support through grant C-11 (Nanotechnology and drug delivery).

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Authors and Affiliations

  1. Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Mohali, 160 062, India

    Deepak Chitkara, Sanjay K. Nikalaje, Anupama Mittal, Mahesh Chand & Neeraj Kumar

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  1. Deepak Chitkara
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  2. Sanjay K. Nikalaje
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  3. Anupama Mittal
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Correspondence to Neeraj Kumar.

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Chitkara, D., Nikalaje, S.K., Mittal, A. et al. Development of quercetin nanoformulation and in vivo evaluation using streptozotocin induced diabetic rat model. Drug Deliv. and Transl. Res. 2, 112–123 (2012). https://doi.org/10.1007/s13346-012-0063-5

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