Novel microemulsion in situ electrolyte-triggered gelling system for ophthalmic delivery of lipophilic cyclosporine A: in vitro and in vivo results.
Int J Pharm
; 365(1-2): 143-9, 2009 Jan 05.
Article
em En
| MEDLINE
| ID: mdl-18773948
ABSTRACT
The objective of the present study was to design a novel microemulsion in situ electrolyte-triggered gelling system for ophthalmic delivery of a lipophilic drug, cyclosporine A (CsA). A CsA-loaded microemulsion was prepared using castor oil, Solutol HS 15 (surfactant), glycerol and water. This microemulsion was then dispersed in a Kelcogel solution to form the final microemulsion in situ electrolyte-triggered gelling system. In vitro, the viscosity of the CsA microemulsion Kelcogel system increased dramatically on dilution with artificial tear fluid and exhibited pseudo-plastic rheology. In vivo results revealed that the AUC(0-->32 h) of corneal CsA for the microemulsion Kelcogel system was approximately three-fold greater than for a CsA emulsion. Moreover, at 32 h after administration, CsA concentrations delivered by the microemulsion Kelcogel system remained at therapeutic levels in the cornea. This CsA microemulsion in situ electrolyte-triggered gelling system might provide an alternative approach to deliver prolonged precorneal residence time of CsA for preventing cornea allograft rejection.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Ciclosporina
/
Eletrólitos
/
Excipientes
/
Imunossupressores
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Revista:
Int J Pharm
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
China