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

Author(s):

1. Jiejia Ge: College of Pharmaceutical Sciences, Southwest University, Chongqing, China

2. Miao Wang: College of Pharmaceutical Sciences, Southwest University, Chongqing, China

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

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

5. 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.

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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