Oral bioavailability and pharmacodynamic activity of hesperetin nanocrystals generated using a novel bottom-up technology

Molecular Pharmaceutics
Ganesh SheteArvind Kumar Bansal

Abstract

In the present study, nanocrystalline solid dispersion (NSD) was developed to enhance the release rate and oral bioavailability of hesperetin (HRN). NSD of HRN was prepared using a novel bottom-up technology platform. It is a spray drying based technology to generate solid particles, containing drug nanocrystals dispersed in small molecule excipients. HRN and mannitol were used in a 5:5 ratio, and an average crystallite size of HRN in NSD with mannitol was found to be 137.3 ± 90.0 nm. An in vitro release study revealed a statistically significant release rate enhancement for HRN nanocrystals (46.3 μg/mL/min) as compared to that of the control (29.5 μg/mL/min). Further, a comparative oral bioavailability study of NSD and control in Sprague-Dawley rats established significant improvement in Cmax and oral bioavailability (AUC0-∞) by 1.79- and 2.25-fold, respectively, for HRN nanocrystals. The findings of oral bioavailability were corroborated by intestinal uptake and Caco-2 cell uptake studies, wherein HRN, when administered in nanocrystalline form, showed higher penetration in intestinal mucosa and higher uptake in Caco-2 cells. Finally, the therapeutic efficacy of HRN nanocrystals was tested by a reactive oxygen species (ROS) ge...Continue Reading

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Citations

Dec 17, 2015·Archives of Pharmacal Research·Pravin Nalawade, Anuradha Gajjar
Sep 4, 2015·International Journal of Pharmaceutics·Varun BhattArvind Kumar Bansal
May 1, 2017·Journal of Pharmaceutical Sciences·Kunal ChadhaKaran Vasisht
Apr 24, 2019·The Journal of Pharmacology and Experimental Therapeutics·G KaurM N V Ravi Kumar
Dec 14, 2018·Current Medicinal Chemistry·Francesco LaiChiara Sinico
Feb 14, 2020·Drug and Chemical Toxicology·Pragyan ParamitaAmbigapathi Moorthi
Feb 26, 2016·Drug Delivery and Translational Research·Ganesh Shete, Arvind Kumar Bansal
Oct 19, 2019·Drug Development and Industrial Pharmacy·Shreya ThakkarManju Misra
Jul 16, 2021·Drug Discovery Today·Prashantkumar K ParmarArvind K Bansal

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