The preparation and characterization of folate-conjugated human serum albumin magnetic cisplatin nanoparticles

摘要

Objective:Nanoparticles are becoming an important method of targeted drug delivery.To evaluate the importance of folate-conjugated human serum albumin(HSA)magnetic nanoparticles(Folate-CDDP/HSA MNP),we prepared drug-loaded Folate-CDDP/HSA MNPs and characterized their features.Methods:First, folate was conjugated with HSA under the effect of a condensing agent,and the conjugating rate was evaluated by a colorimetric method using 2,4,6-trinitrobenzene sulfonic acid.Second,under N 2 gas,Fe 3 O 4 magnetic nanomaterials were prepared and characterized by using transmission electron microscopy(TEM),SEM-EDS and X-ray diffraction(XRD).Finally,Folate-CDDP/HSA MNP was prepared by using a solvent evaporation technique. TEM was used to observe particle morphology.The particle size and distribution of the prepared complexes were determined by a Laser particle size analyzer.Drug loading volume and drug release were investigated by a high performance liquid chromatography method(HPLC)in vitro.Results:We successfully prepared folate-conjugated HSA and its conjugating rate was 27.26μg/mg.Under TEM,Fe 3 O 4 magnetic nanoparticles were highly electron density and had an even size distribution in the range of 10-20 nm.It was confirmed by SEM-EDS and XRD that Fe 3 O 4 magnetic nanoparticles had been successfully prepared.Under TEM,drug-loaded magnetic nanoparticles were observed,which had a round shape,similar uniform size and smooth surface.Their average size was 79 nm which was determined by laser scattering,and they exhibited magnetic responsiveness.Encapsulation efficiency was 89.75%and effective drug loading was calculated to be 15.25%.The release results in vitro showed that the half release time(t1/ 2 )of cisplatin in cisplatin Solution and Folate-CDDP/HSA MNP was 65 min and 24 h respectively, which indicated that microspheres had an obvious effect of sustained-release.Conclusion:Folate-CDDP/HSA MNPs were prepared successfully.The preparation process and related characteristics data provided a foundation for further study,including the mechanism of the nanoparticles distribution in vivo and their intake by tumor cells.