Construction and Characterization of Tacrolimus Niosomes / 中国药房

ABSTRACT

OBJECTIVE:To prepare Tacrolimus niosomes (Tac-NS) and evaluate their characteristics in vitro. METHODS:Tac-NS were prepared by a film hydration-ultrasonic method. Using the comprehensive score of encapsulation efficiency (EE%), drug-loading amount,mean particle size and PDI as the evaluation index,orthogonal design was used to optimize the concentration of sorbitan monostearate(Span-60),mole ratio of Span-60 to cholesterol,mole ratio of Span-60 to SDC. The morphology,mean particle size,PDI,Zeta-potential and EE%of Tac-NS were investigated. Accumulative percutaneous penetration(Q)and accumula-tive retention amount(Qs)of Tac-NS and physical mixture of Tac and NS were compared by percutaneous penetration test in vitro. RESULTS:The optimal formulation was as follows as Span-60 0.025 mol/L,mole ratio of Span-60 to cholesterol 10∶1,mole ratio of Span-60 to SDC 15∶1,drug-loading amount of 5%. Tac-NS was spherical and distributed evenly,but hardly congregated.The mean particle size,PDI,Zeta-potential and EE% were (233.0 ± 6.48) nm,0.266 ± 0.021,(-41.7 ± 0.32) mV and (76.83 ± 4.61)%,respectively. The results of in vitro permeability study showed that Qs of Tac-NS was 2.4 times of physical mixture;in ad-dition,Q of the two were similar. CONCLUSIONS:Tac-NS,owning high EE%,small particle size,uniform distribution and ide-al permeation effect,is prepared successfully.