Development of a new nanovesicle formulation as transdermal carrier: formulation, physicochemical characterization, permeation studies and anti-inflammatory activity.
Artif Cells Nanomed Biotechnol
; 42(5): 323-30, 2014 Oct.
Article
en En
| MEDLINE
| ID: mdl-23944163
CONTEXT: Ibuprofen is an important NSAID, however, it can cause GI disturbances when given orally, and employment of transdermal route will require permeation enhancer causing skin injury. OBJECTIVE: Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, and cholesteryl sulfate (ICVG) were formulated and analyzed for physicochemical and permeation properties. MATERIALS AND METHOD: Vesicles were formulated using film hydration method and physicochemical parameters, in vitro drug release, and stability were assessed. Further, nanovesicle gels were evaluated against plain gel containing drug (CG) for ex vivo/in vivo drug permeation and anti-inflammatory activity. RESULTS: The developed formulations showed optimal physicochemical profile and ICV-1 gave 97.24% drug release. Drug permeation was between 17.32 and 33.12 µg/cm(2) for ICVG formulations and 0.27 µg/cm(2) for CG. ICVG-1 and CG showed Cmax of 9.6 and 0.7 µg/ml at 8 and 4 h. ICVG-1 showed 19.9 times higher AUC than CG. Edema inhibition was 57.98% during initial hours by ICVG-1. DISCUSSION: Ratio of ceramide 2 and palmitic acid plays a critical role in drug permeation through stratum corneum. The stability and protective effect of the formulations were due to ceramide content. CONCLUSION: The composition has an important role in physicochemical properties and drug permeation thereby generating an optimum formulation.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ceramidas
/
Antiinflamatorios no Esteroideos
/
Ibuprofeno
/
Nanoestructuras
/
Fenómenos Químicos
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Artif Cells Nanomed Biotechnol
Año:
2014
Tipo del documento:
Article
País de afiliación:
India
Pais de publicación:
Reino Unido