Improvement of solubility and dissolution of ebastine by fabricating phosphatidylcholine/ bile salt bilosomes.
Administration, Oral
Bile Acids and Salts
/ chemistry
Biological Availability
Butyrophenones
/ administration & dosage
Drug Compounding
Drug Liberation
Histamine H1 Antagonists
/ administration & dosage
Liposomes
Nanoparticles
Phosphatidylcholines
/ chemistry
Piperidines
/ administration & dosage
Solubility
Journal
Pakistan journal of pharmaceutical sciences
ISSN: 1011-601X
Titre abrégé: Pak J Pharm Sci
Pays: Pakistan
ID NLM: 9426356
Informations de publication
Date de publication:
Sep 2020
Sep 2020
Historique:
entrez:
9
4
2021
pubmed:
10
4
2021
medline:
19
11
2021
Statut:
ppublish
Résumé
Although ebastine (EBT) can impede histamine-induced skin allergic reaction and persuade long acting selective H1 receptor antagonistic effects but its poor water solubility circumscribed its clinical application. The main objective of this research work was to improve the aqueous solubility and oral bioavailability of EBT by preparing EBT-loaded bilosomes (EBT-PC-SDC-BS). A thin film hydration method was used to prepare ebastine loaded bilosomes. The prepared-formulations were optimized considering size, morphology and entrapment efficiency. The SEM images revealed regular and spherical shape of bilosomes. Average size of the prepared EBT-PC-SDC-BS was 665.8 nm and zeta potential was around-32.9 mV with 89.05 % average entrapment efficiency (EE).Importantly, the solubility of EBT in water was amplified up to 17.9 μg/ml compared to pure drug (2 μg/mL) reflecting a highest solubility increase of 751 %. In vitro drug release results of prepared EBT-PC-SDC-BS exhibited improved release behavior. Finally, it is established from the results that the EBT-PC-SDC-BS could function as a favorable nano-carrier system to improve the solubility as well as dissolution of EBT.
Substances chimiques
Bile Acids and Salts
0
Butyrophenones
0
Histamine H1 Antagonists
0
Liposomes
0
Phosphatidylcholines
0
Piperidines
0
ebastine
TQD7Q784P1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM