Preparation,characterization and in vitro anti-inflammatory activity of tetrandrine-loaded chitosan-stearic acid nano micelles modified with folic acid
OBJECTIVE To prepare tetrandrine(TET)-loaded chitosan(CS)-stearic acid(SA)nano micelles modified with folic acid(FA)(FA-CS-SA/TET nano micelles),characterize them and study the anti-inflammatory effect in vitro.METHODS FA-CS-SA/TET nano micelles were prepared by ultrasonic method;the preparation technology was optimized by orthogonal test and validation test was also performed with the mass ratio of FA-CS-SA to TET,ultrasound power and ultrasound times as the factors,using the comprehensive score of entrapment efficiency(EE),drug loading(DL)and particle size as evaluation index.FA-CS-SA/TET nano micelles prepared by the optimal technology were characterized,and their release performance in vitro was investigated.RAW264.7 cells were used as subjects to investigate their anti-inflammatory activity in vitro.RESULTS The optimal preparation technology included that the mass ratio of FA-CS-SA to TET was 2∶1,ultrasonic power was 200 W,and the ultrasonic frequency was 200 times.The parameters of FA-CS-SA/TET nano micelles prepared by optimized technology included that EE was(98.86±0.30)%,DL was(28.57±0.34)%,the average particle size was(227.0±9.4)nm,polydispersity index was 0.42±0.04,and the Zeta potential was(12.6±2.3)mV,respectively.The nano micelles were uniform in appearance and round in shape.The nano micelles were released quickly in 0.5%sodium dodecyl sulfate solution,with a cumulative release rate of(79.49±3.43)%within 72 hours,and its anti-inflammatory effect was stronger than that of TET raw materials.CONCLUSIONS FA-CS-SA/TET nano micelles are prepared successfully in the study,with good drug loading performance,uniform particle size,and good in vitro anti-inflammatory activity.
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