Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery. (1st February 2014)

• Record Type: Journal Article
• Authors: Gaur, Praveen Kumar; Purohit, Suresh; Kumar, Yatendra; Mishra, Shikha; Bhandari, Anil
• Is Part Of: Pharmaceutical development and technology. Volume 19:Number 1(2014)
• Page Start: 48
• Page End: 54
• Publication Date: 2014-02-01
• Subjects: Ceramide -- diclofenac -- entrapment efficiency -- ex vivo; Drug delivery systems -- Periodicals; Pharmaceutical technology -- Periodicals; Drugs -- Administration -- Research -- Periodicals; Drug Delivery Systems -- Periodicals; Pharmaceutical Preparations -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615
• DOI: 10.3109/10837450.2012.751406
• Languages: English
• ISSNs: 1083-7450

Abstract

Abstract: Context: Transdermal formulations contain permeation enhancer which causes skin damage. Ceramide 2 is natural lipid found in stratum corneum (SC). Objective : Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, cholesteryl sulfate were formulated and analyzed for physical and biological properties. Diclofenac was used as a model drug. Materials and method : The vesicles were prepared using the film hydration method and characterized for physical parameters, in vitro drug release, accelerated stability studies and formulated into gel. Respective gels were compared with a commercial formulation (CEG) and plain carbopol gel (CG) containing drug for ex vivo, in vivo drug permeation and anti-inflammatory activity. Results : The vesicles were stable with optimum physical parameters. DCG-1 showed 92.89% in vitro drug release. Ceramide vesicles showed drug release between 18 and 25 μg/cm 2 whereas CG and CEG released 0.33 and 1.35 μg/cm 2 drug, respectively. DCG-1 and CEG showed corresponding C max at 6 and 4 h, respectively. DCG-1 showed six times AUC than CEG. DCG-1 inhibited edema by 86.37% by 4th hour of application. Discussion : The presence of ceramide 2 specifically promotes the drug permeation through SC and dermis and also contribute towards stability and non-irritancy. Conclusion : The composition of the nanovesicle played an important role in physical properties and drug permeation.