Enhanced oral bioavailability of Bisdemethoxycurcumin-loaded self-microemulsifying drug delivery system: Formulation design, in vitro and in vivo evaluation.
Bioavailability
Bisdemethoxycurcumin
Experimental design
Formulation evaluation
Self micro-emulsifying system
Journal
International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127
Informations de publication
Date de publication:
30 Nov 2020
30 Nov 2020
Historique:
received:
25
05
2020
revised:
02
09
2020
accepted:
13
09
2020
pubmed:
21
9
2020
medline:
22
6
2021
entrez:
20
9
2020
Statut:
ppublish
Résumé
In this study, we sought to overcome the poor solubility and bioavailability of bismethoxycurcumin (BDMC) by fabricating a BDMC-loaded self micro-emulsifying system (BDMC-SMEDDS). Solubility and compatibility tests, pseudo-ternary phase diagrams (PTPDs) as well as d-optimal concept was applied to design the formulation. The assessment of the prepared BDMC-SMEDDS in-vitro mainly included droplet size (DS) and entrapment efficiency (EE) determination, morphology, drug release and stability testing. Besides, the in vivo behavior was also evaluated after oral administration of BDMC-SMEDDS to rats. The optimal formulation was found to compose of Kolliphor EL (K-EL, emulsifier, 645.3 mg), PEG 400 (co-emulsifier, 147.2 mg), ethyl oleate (EO, oil, 207.5 mg) and BDMC (50 mg). The BDMC-SMEDDS with satisfactory stability had a mean size of 21.25 ± 3.23 nm and EE of 98.31 ± 0.32%. Roughly 70% of BDMC was released from BDMC-SMEDDS within 84 h compared with <20% from the free BDMC. More importantly, the in-vivo behavior of BDMC-SMEDDS showed that the AUC
Identifiants
pubmed: 32950666
pii: S0378-5173(20)30872-3
doi: 10.1016/j.ijpharm.2020.119887
pii:
doi:
Substances chimiques
Diarylheptanoids
0
Emulsions
0
bisdemethoxycurcumin
2EFO1BP34R
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
119887Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.