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Nanocochleate-based delivery of quercetin with enhanced therapeutic potential: formulation, cytotoxicity and pharmacokinetics study

  • Harshad S. Kapare,
  • Nagesh Patil,
  • Mayuri Bhosale,
  • Deepak Kulkarni,
  • Ritesh Bhole

摘要

Background

Quercetin has well-proven anticancer potential through various mechanisms, but its applications in drug delivery are limited due to poor biopharmaceutical properties. The present study was aimed to formulate quercetin nanocochleates (QNC) in order to overcome these limitations. QNC formulation was fabricated by a trapping method, optimized and evaluated for various formulation aspects, in vitro cytotoxicity and pharmacokinetic parameters.

Result

Developed nanocochleates possess particle size and encapsulation efficiency of 205.6 ± 2.55 nm and 76.36 ± 0.88%, respectively. In vitro cytotoxicity study performed using MCF-7 cell lines revealed the comparative efficiency of QNC over pure quercetin. Total growth inhibition concentration (TGI) for pure quercetin was 96.73 μg/ml, while for QNC it was 83.29 μg/ml. Pharmacokinetic study results showed improvement in Cmax and AUC after QNC formulation with increased Tmax showing sustained release.

Conclusion

Overall, the developed QNC formulation markedly improved cytotoxic potential and biopharmaceutical aspects.