15-hydroxystearate micelles for the delivery of aprepitant: Preparation, characterization, pharmacokinetics and tissue distribution in mice | Pakistan Journal of Pharmaceutical Sciences 2021

Author(s)

Jiejia Ge College of Pharmaceutical Sciences, Southwest University, Chongqing, China

Miao Wang College of Pharmaceutical Sciences, Southwest University, Chongqing, China

Haiting Kong Chongqing Engineering Research Center for Pharmaceutical Process and Quality Control, Chongqing, China

Hong Liu College of Pharmaceutical Sciences, Southwest University, Chongqing, China; Chongqing Engineering Research Center for Pharmaceutical Process and Quality Control, Chongqing, China

Hongchun Pan College of Pharmaceutical Sciences, Southwest University, Chongqing, China; Chongqing Engineering Research Center for Pharmaceutical Process and Quality Control, Chongqing, China

Abstract

This study developed a novel Aprepitant micells (APPT-Ms) formulation that uses a mixture of 15hydroxystearate (HS15) as surfactant to solubilize AAPT. This article determines the content of APPT by HPLC. The in vitro test results show that the optimized APPT-Ms has small particle size, excellent stability and long-lasting release. At a test dose of 20mg/kg, the pharmacokinetic study of APPT-Ms showed that it accorded with first-order kinetics in mice, and its AUC value was higher than the pure AAPT about 6 times. The tissue distribution study of mice showed that the APPT-Ms had higher tissue binding ability than pure AAPT. The APPT-Ms could be rapidly distributed to various tissues and it was easier to pass through the blood-brain barrier than APPT. In this study, the APPT-Ms has high antiemetic activity and improves the compliance of patient. The pharmacokinetics and tissue distribution of APPT-Ms after injection administration were studied, which may be of guiding significance for further research.

Publication Details

Page(s) 635-639

DOI DOI not available

Published Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 34, Issue: 2, Year: 2021

Keywords

Pharmacokinetics distribution Micelles Aprepitant tissue

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