Oil-water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system.
Central composite design-response surface methodology
Dihydroartemisinin
Oil–water partition coefficient
SEDDS
Ternary phase diagram
Journal
BMC biotechnology
ISSN: 1472-6750
Titre abrégé: BMC Biotechnol
Pays: England
ID NLM: 101088663
Informations de publication
Date de publication:
27 05 2022
27 05 2022
Historique:
received:
21
03
2022
accepted:
11
05
2022
entrez:
27
5
2022
pubmed:
28
5
2022
medline:
1
6
2022
Statut:
epublish
Résumé
The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS). We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying agent, the design mixture method was selected in the design expert software. Next, optimal prescription validation and preliminary formulation evaluation were conducted. By comparing the oil-water partition coefficient in vitro, the improvement of the in vivo osmotic absorption of DHA via self-emulsification was evaluated. The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the DHA self-emulsifying preparation = 0.511:0.2:0.289 (w/w/w), with a drug-loading capacity of 26.3634 mg/g, solubility of 2.5448 mg/ml, and self-emulsification time of 230 s. The solubility self-emulsification was approximately 20.52 × higher in DHA than in the crude drug. The self-emulsification could improve DHA permeability and promoting in vivo DHA absorption. The DHA SEDDS could significantly improve DHA solubility and in vivo absorption.
Sections du résumé
BACKGROUND
The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS).
METHODS
We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying agent, the design mixture method was selected in the design expert software. Next, optimal prescription validation and preliminary formulation evaluation were conducted. By comparing the oil-water partition coefficient in vitro, the improvement of the in vivo osmotic absorption of DHA via self-emulsification was evaluated.
RESULTS
The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the DHA self-emulsifying preparation = 0.511:0.2:0.289 (w/w/w), with a drug-loading capacity of 26.3634 mg/g, solubility of 2.5448 mg/ml, and self-emulsification time of 230 s. The solubility self-emulsification was approximately 20.52 × higher in DHA than in the crude drug. The self-emulsification could improve DHA permeability and promoting in vivo DHA absorption.
CONCLUSION
The DHA SEDDS could significantly improve DHA solubility and in vivo absorption.
Identifiants
pubmed: 35624465
doi: 10.1186/s12896-022-00746-6
pii: 10.1186/s12896-022-00746-6
pmc: PMC9137071
doi:
Substances chimiques
Artemisinins
0
Water
059QF0KO0R
Polyethylene Glycols
3WJQ0SDW1A
artenimol
6A9O50735X
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
16Informations de copyright
© 2022. The Author(s).
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