Design and development of lipid modified chitosan containing muco-adhesive self-emulsifying drug delivery systems for cefixime oral delivery.
Acyl-chitosan
Bioavailability
Cefixime
Muco-adhesive
Oral delivery
SNEDDS
Journal
Chemistry and physics of lipids
ISSN: 1873-2941
Titre abrégé: Chem Phys Lipids
Pays: Ireland
ID NLM: 0067206
Informations de publication
Date de publication:
03 2021
03 2021
Historique:
received:
01
10
2020
revised:
07
01
2021
accepted:
12
01
2021
pubmed:
23
1
2021
medline:
27
8
2021
entrez:
22
1
2021
Statut:
ppublish
Résumé
Current study was aimed to design and develop muco-adhesive self-nano emulsifying drug delivery system (SNEDDs) for improved pharmacokinetics of Cefixime (CFX) in rabbits. The components of SNEDDs formulation i.e., cinnamon oil, Tween® 80, and PEG 200 as oil, surfactant, and co-surfactant respectively were selected based on their high solubilizing capability of the drug. SNEDDs formulation was optimized using Design of experiments (D-optimal design) in terms of droplet size, poly dispersity index and zeta potential. The optimized SNEDDs formulation was studied for various parameters like droplet size, morphology, zeta potential, emulsification, optical clarity, thermodynamic stability, GIT stability, and robustness to dilution. CFX was loaded to optimized formulation to form CFX-SNEDDs. Furthermore, acyl-chitosan, a muco-adhesive agent, was added to CFX-SNEDDS to prepare CHT-CFX-SNEDDS. In vitro drug release showed the controlled release behavior reached a maximum value of 70 % at pH 6.8 within 24 h. The droplet size, atomic force microscopy, and optical clarity analysis revealed the formation of nanosized emulsion (156 ± 25 nm) with spherical morphology. Also in vivo pharmacokinetic studies on rabbits showed an increased drug plasma concentration for CHT-CFX-SNEDDs (15 ± 3 μg/mL) and CFX-SNEDDs (9 ± 2 μg/mL) in comparison with control CFX (4 ± 1 μg/mL). The results indicated that the developed CHT-CFX-SNEDDs with an increased degree of solubilization, permeation, and nanosized range emulsion enhance the oral performance of CFX.
Identifiants
pubmed: 33482099
pii: S0009-3084(21)00005-0
doi: 10.1016/j.chemphyslip.2021.105052
pii:
doi:
Substances chimiques
Adhesives
0
Emulsions
0
Lipids
0
Chitosan
9012-76-4
Cefixime
97I1C92E55
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
105052Informations de copyright
Copyright © 2021 Elsevier B.V. All rights reserved.