Development and Evaluation of Liposomes for Topical Delivery of Tacrolimus (Fk-506)

Abstract

In the present work Tacrolimus loaded liposomal systems were developed and evaluated for their topical delivery. Neutral multilamellar liposomes (MLVs) were prepared by thin film hydration method. The amount of drug loaded into vesicles ranged from 4.4 mg per 115mg to 8.2mg per 140mg of total lipid. Entrapment efficiency of tacrolimus in liposomes was studied by altering the amount of cholesterol ratio to lipid ratio. After performing stability study at different temperatures (4, 25, and 37°C) was affirms that drug leakage increased at higher temperature. The in-vitro permeation study shows significant reduced permeation with tacrolimus liposomes compared with free tacrolimus in propylene glycol. The animal study carried out on allergic contact dermatitis (ACD) model in rats showed that 0.03% tacrolimus liposomal gel exhibited similar activity when compared with 0.03% marketed tacrolimus ointment. It is also likely that tacrolimus liposomal gel which leads no visible or palpable residue when applied on skin would be more appealing to patients than conventional ointment. Overall study suggests that tacrolimus can be effectively incorporated in liposomes and can be used for the treatment of atopic dermatitis.

Keywords: Tacrolimus; Multilamellar vesicle; Allergic contact dermatitis.  

© 2010 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.

 DOI: 10.3329/jsr.v2i3.3258               J. Sci. Res. 2 (3), 587-598  (2010)