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Drug Res (Stuttg) 2017; 67(10): 564-575
DOI: 10.1055/s-0043-109564
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Enhancement of Quercetin Oral Bioavailability by Self-Nanoemulsifying Drug Delivery System and their Quantification Through Ultra High Performance Liquid Chromatography and Mass Spectrometry in Cerebral Ischemia

Niyaz Ahmad
1   Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University (Formerly University of Dammam), Dammam, Kingdom of Saudi Arabia
,
Rizwan Ahmad
2   Department of Natural Products and Alternative Medicine, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University (Formerly University of Dammam), Dammam, Kingdom of Saudi Arabia
,
Atta Abbas Naqvi
3   Department of Pharmacy Practice, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University (Formerly University of Dammam), Dammam, Kingdom of Saudi Arabia
,
Md Aftab Alam
4   Department of Pharmaceutics, School of Medical and Allied Sciences, Galgotias University, Gautam Budh Nagar, Greater Noida, India
,
Rehan Abdur Rub
5   Nanomedicine Lab, Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India
,
Farhan Jalees Ahmad
5   Nanomedicine Lab, Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India
› Author Affiliations
Further Information

Publication History

received 18 January 2017

accepted 21 April 2017

Publication Date:
23 May 2017 (online)

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Abstract

Background Quercetin (Qur) and its major in vivo bioactive metabolites i. e., 3′-O-methyl quercetin, 4′-O-methyl quercetin and quercetin 7-O-β-D-glucuronide, may be used to treat cerebral ischemia however the poor aqueous solubility and less intestinal absorption of Qur results low bioavailability.

Purpose To improve Qur bioavailability through preparation of nanoformulation and to develop and validate a sensitive quantification method for Qur detection in brain homogenate.

Methods Qur-containing self-nanoemulsifying drug delivery system (Qur-SNEDDS) was developed to form oil-in-water nanoemulsions in situ. Ultra-high performance liquid chromatography electrospray ionization-synapt mass spectrometric method (UHPLC/ESI-QTOF-MS/MS) was developed and validated for quantification whereas for optimal recovery of analyte, a liquid-liquid extraction method (LLE) was used.

Results A droplet size of 94.63±3.17 nm and zeta potential of −17.91±1.02 mV for nanoemuslion, elution time for Qur and internal standard (IS) Rutin as 1.21 and 1.50 min alongwith a transition at m/z 301.04/151.03 and 609.21/299.21, were observed respectively. Similarly, linear dynamic range (1.00 ng/mL–2 000.0 ng/mL), intra and inter-assay i. e., %CV of 0.26–2.04, lower limit of detection (LOD) 0.08 ng/mL as well as lower limit of quantitation (LOQ) as 0.131 ng/mL were also observed.

Conclusion The developed method have advantage over previous all methods i. e., less time consuming (<3.0), low consumption of solvents (flow rate 0.20 mL/min.) via small size column, more accuracy and specificity as well as use of acetonitrile as compared to hazardous solvents. This certainly adds advantages for green chromatography technique and supports application of current developed method for quantification and evaluation of Qur-SNEDDS.

 

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