Preparation of Tacrolimus-loaded polyion complex micelles and their release characteristics in vitro
JIAO Yan
LI Lingbing
MU Yan
XU Wei
Abstract：Objective To prepare the Tacrolimus-loaded polyion complex micelles and observe their release charac-teristics in vitro.Methods Tacrolimus-loaded polyion complex micelles were prepared by film-ultrasonic method with Plu-ronic F127-chitosan (F127-CS)polymer and sodium deoxycholate (DCA).Preparation technique and optimal formulation were selected via single factor investigation and uniform design.Morphology of polyion micelles was observed by transmis-sion electron microscope.Diameter distribution and zeta potential of polyion micelles were measured by using laser size scattering determinator.Drug loading capacity (DL%)was determined with the high performance liquid chromatography (HPLC).Pyrene as a fluorescence probe was used to detect critical micelle concentration (CMC).In vitro release was e-valuated with dynamic membrane dialysis.Results The electron microscope showed spherical micelles were round and u-niform.The average diameter was (55.77 ±2.23)nm,zeta potential was (-6.38 ±0.47)mV,drug loading capacity (DL%)was 8.93% ±0.20%,and the Critical Micelle Concentration (CMC)was 2.65 ×10 -3 mol/L.In vitro release study suggested that Tacrolimus-loaded F127-CS /DCA micelles showed a pH-dependent release,the release rate in artifi-cial intestinal juice was higher than that in artificial gastric juice.Conclusion F127-CS /DCA polyion micelles have high drug-loading capacity and pH-dependent release characteristics,and are suitable for oral administration of Tacrolimus.
Keywords：Tacrolimuspolyion complex micellesPluronic F127-chitosanpreparation techniquein vitro experi-ment
Publication Date：2016-01-01
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：4( 28-31 )