Improvement of Oral Bioavailability and Anti-Tumor Effect of Zingerone Self-Microemulsion Drug Delivery System.
Bioavailability apoptosis
Oral drug delivery
Pharmacokinetic
Self-emulsifying
Zingerone
Journal
Journal of pharmaceutical sciences
ISSN: 1520-6017
Titre abrégé: J Pharm Sci
Pays: United States
ID NLM: 2985195R
Informations de publication
Date de publication:
07 2021
07 2021
Historique:
received:
17
11
2020
revised:
14
01
2021
accepted:
21
01
2021
pubmed:
22
2
2021
medline:
5
8
2021
entrez:
21
2
2021
Statut:
ppublish
Résumé
This study sought to prepare a self-microemulsion drug delivery system containing zingerone (Z-SMEDDS) to improve the low oral bioavailability of zingerone and anti-tumor effect. Z-SMEDDS was characterized by particle size, zeta potential and encapsulation efficiency, while its pharmacokinetics and anti-tumor effects were also evaluated. Z-SMEDDS had stable physicochemical properties, including average particle size of 17.29 ± 0.07 nm, the zeta potential of -22.81 ± 0.29 mV, and the encapsulation efficiency of 97.96% ± 0.02%. In vitro release studies have shown the release of zingerone released by Z-SMEDDS was significantly higher than free zingerone in different release media. The relative oral bioavailability of Z-SMEDDS was 7.63 times compared with free drug. Meanwhile, the half inhibitory concentration （IC50）of Z-SMEDDS and free zingerone was 8.45 μg/mL and 13.30 μg/mL, respectively on HepG2. This study may provide a preliminary basis for further clinical research and application of Z-SMEDDS.
Identifiants
pubmed: 33610568
pii: S0022-3549(21)00099-X
doi: 10.1016/j.xphs.2021.01.037
pii:
doi:
Substances chimiques
Emulsions
0
zingerone
4MMW850892
Guaiacol
6JKA7MAH9C
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
2718-2727Informations de copyright
Copyright © 2021. Published by Elsevier Inc.