Design and characterization of Tacrolimus monohydrate loaded core shell lipid polymer hybrid nanoparticle

Tacrolimus monohydrate (TAC) loaded core shell lipid polymer hybrid nanoparticle (CS-LPHNs) composed of polymer core (PLGA) surrounded by lipid shell (lecithin). DSPE-PEG(2000) was used as stabilize the nanoparticles. TAC-CS-LPHNs were prepared by single step modified nanoprecipitation method. Field emission electron microscope and Transmission Electron Microscope reveals a spherical shape nano-sized particle coated with a lipid layer. The nanoparticles ranged in size from 82nm +/- 0.2-195 +/- 0.143nm which increase with increase the polymer quantity. The entrapment efficiency also affected by the polymer quantity that ranges from 55 +/- 1.23%-76 +/- 1.93%. XRD and DSC studies show conversion of TAC from crystalline into amorphous when imbedded inside the CS-LPHNs and FTIR study shows no chemical interaction between TAC and other components. The Cytotoxicity study of TAC and TAC-CS-LPHNs show a decrease in cytotoxicity of loaded TAC (IC50=1.18067 +/- 0.045 mu g/ml) in compare with free TAC(IC50=0.697 +/- 0.02 mu g/ml). Finally, the uptake study shows complete internalization of nanoparticle by Vero cell and accumulation of nanoparticles inside nucleus and cytoplasm. The results suggested CS-LPHNs is a good drug delivery system for TAC which is safe, effective and promising a better clinicals outcome.