Morphological effect of lipid carriers on permeation of lidocaine hydrochloride through lipid membranes.
Int J Pharm
; 388(1-2): 251-6, 2010 Mar 30.
Article
em En
| MEDLINE
| ID: mdl-20060459
ABSTRACT
We have studied how the transdermal delivery of lidocaine hydrochloride (LHC) is affected by the morphology of lipid carriers, liposomes and micelles, having the same lipid composition of 1-stearoyl-sn-glycero-3-phosphocholine (LPC) and cholesteryl hemisuccinate (CHEMS). In vitro drug permeation study, carried out on guinea pig skin, has revealed that the liposomes made of LPC and CHEMS significantly enhance the permeation rate of entrapped LHC; by contrast, the mixed micelles with the same composition decrease the degree of delivering co-existing LHC. Basically, we have also investigated the release kinetics of LHC through the cellulose membrane and found that both liposomes and micelles have a similar releasing profile. To experimentally demonstrate this unique behavior, we have observed the fluidity of stratum corneum liposomal membranes in the presence of either our liposomes or micelles. From this study, we have found that LPC/CHEMS liposomes fluidize the lipid membrane of stratum corneum lipids; however, lipid micelles rather make the membrane rigid. These findings highlight that controlling the morphology of drug carriers provides us with a means to modulate the permeability of encapsulated drug molecules.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Absorção Cutânea
/
Portadores de Fármacos
/
Lidocaína
Limite:
Animals
Idioma:
En
Revista:
Int J Pharm
Ano de publicação:
2010
Tipo de documento:
Article