Preparation and Evaluation of a Xanthan Gum-Containing Linezolid Ophthalmic Solution for Topical Treatment of Experimental Bacterial Keratitis.
Administration, Ophthalmic
Animals
Biological Availability
Cornea
/ drug effects
Disease Models, Animal
Drug Carriers
/ chemistry
Humans
Keratitis
/ diagnosis
Linezolid
/ administration & dosage
Microbial Sensitivity Tests
Ophthalmic Solutions
/ administration & dosage
Permeability
Polysaccharides, Bacterial
/ chemistry
Rabbits
Slit Lamp Microscopy
Staphylococcal Infections
/ drug therapy
Staphylococcus aureus
/ drug effects
bacterial keratitis
in vivo antibacterial
linezolid
ocular tolerance
xanthan gum
Journal
Pharmaceutical research
ISSN: 1573-904X
Titre abrégé: Pharm Res
Pays: United States
ID NLM: 8406521
Informations de publication
Date de publication:
Feb 2021
Feb 2021
Historique:
received:
12
10
2020
accepted:
22
12
2020
pubmed:
21
1
2021
medline:
21
10
2021
entrez:
20
1
2021
Statut:
ppublish
Résumé
To formulate a xanthan gum-containing linezolid ophthalmic solution (LZD-XG) as a new antibiotic treatment against ocular bacterial infection. LZD-XG was prepared and evaluated for its in vitro/in vivo ocular tolerance, in vitro/in vivo antibacterial activity, and in vivo ocular penetration. The optimized LZD-XG exhibited good in vitro/in vivo eye tolerance. A prolonged ocular surface residence time of LZD-XG was observed after topical instillation, and the ocular permeation was significantly better for LZD-XG than fora linezolid (LZD) ophthalmic solution. The in vitro antimicrobial activity was significantly better with LZD-XG than with LZD. In vivo evaluation also confirmed a strong therapeutic treatment effect of LZD-XG, as it significantly improved the clinical symptoms, ameliorated the damage of Staphylococcus aureus to ocular tissues, lowered the colony forming unit counts in the cornea, and decreased the myeloperoxidase activity in the cornea. LZD-XG was deemed a viable ophthalmic solution against ocular bacterial infection due to its excellent in vitro and in vivo characterizations.
Identifiants
pubmed: 33469875
doi: 10.1007/s11095-020-02982-x
pii: 10.1007/s11095-020-02982-x
doi:
Substances chimiques
Drug Carriers
0
Ophthalmic Solutions
0
Polysaccharides, Bacterial
0
Linezolid
ISQ9I6J12J
xanthan gum
TTV12P4NEE
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
347-359Subventions
Organisme : National Natural Science Foundation of China
ID : 81770895
Organisme : China Shandong Provincial Key Research and Development Program
ID : 2019GSF108027
Organisme : the Talent Fund of Shandong Collaborative Innovation Center of Eco-Chemical Engineering
ID : XTCXQN19
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