FORMULATION AND IN VITRO EVALUTION OF DIACEREIN LOADED NIOSOMES

摘要

Objective: Diacerein is poorly water soluble non steroidal anti-inflammatory drug belongs to BCS class II with low oral bioavailability. This research aimed towards formulation and evaluation of successful diacerein loaded niosomes in order to improve dissolution and hence it s oral bioavailability. Methods: Eight formulations (N1-N8) were prepared by thin film hydration method using different ratios of cholesterol to non ionic surfactant (Span 20 and 60) 1:2 and 1:3. The effect of the composition change of surfactant and cholesterol on the properties such as encapsulation efficiency, particle size and drug release were studied. Also the effect of the presence of 0.5% (w/w) sodium deoxycholate as co surfactant was evaluated. Results: The prepared niosomes were in the size range of 0.5-2.6 um. The order of encapsulation efficiency increases with increase in concentration of Span 60. In vitro release study on diacerein niosomes indicates better release profile compared to free diacerein and 93.24% release at 60 min for formulation N8 prepared with cholesterol: Span 20 (1:3) and 0.5% (w/w) sodium deoxycholate. Conclusion: It was concluded that it is possible to enhance solubility and ultimately improve bioavailability of the drug by this promising approach.