Two preparation methods used to improve the bioavailability of quercetin nano-suspension
Objective:To compare the properties of quercetin nanocrystals(QNCs)prepared by microfluidic and antisolvent precipitation methods.Methods:QNCs were prepared by microfluidic and antisolvent precipitation methods,respectively.QNCs prepared by both methods were characterized by Beckman particle sizer,transmission electron microscopy,dissolution meter,differential scanning calorimetry(DSC)and X-ray powder diffractometer(XRPD).The pharmacokinetic differences of QNCs prepared by two methods in rats were studied by HPLC.Results:QNCs prepared by both methods were sphere-like and amorphous.The average particle size of QNCs prepared by the microfluidic method was(78.03±4.97)nm,and that prepared by antisolvent precipitation method was(554.25±84.75)nm.The cumulative dissolution rate of QNCs prepared by both methods exceeded 45%at 60 min,whereas QCT dissolved only 6.8%.AUC0-∞ of QNCs prepared by the microfluidic method was 185.711 mg·h·L-1,and that by antisolvent precipitation method was 86.331 mg·h·L-1.Conclusion:The preparation of QNCs by the two methods can significantly improve the dissolution and oral bioavailability of quercetin,while a better oral bioavailability was obtained by microfluidic method.The results showed that microfluidic technology had a potential in preparing insoluble drug nanocrystals and improving the bioavailability of insoluble drugs.
quercetinnanocrystalsanti-solvent precipitationmicrofluidic methodpharmacokinetics in vivo
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