Preparation And Biological Properties Of Raltitrexed-loaded HSA Nanoparticles

Raltitrexed is a kind of Folic-acids anti-cancer drug for colorectal treatment. To enhance water-solubility, prolong blood circulation half-life, reduce side effects and improve passive targeting performance, we prepared raltitrexed-loaded Human Serum Albumin (HSA) nanoparticles with different size and drug loading by using the desolvation method. The biological properties were evaluated by in vitro and in vivo experiment.Glutathione (GSH) was used to reduce the disulfide bond in HSA to sulfide group. Thereafter, a solution of Raltitrexed in ethanol was added dropwise to form the nanoparticle by using desolvation method. Finally, heat treatment was used to stabilize the nanoparticle. The particle size, drug loading and stability were assessed by DLS and UV spectrophotometry. The cell toxicity was evaluated by MTT method. The cell-uptake was measured by CLSM. Real-time near infrared fluorescence imaging system was used to trace the nanoparticles injected by tail vein in CT-26 tumor-bearing BALB/C mice. The biodistribution of Raltitrexed was quantified by HPLC after extracting the drug from tissue homogenates.The results show that size and drug loading of the nanoparticles can be well controlled. The nanoparticles can enter the cells of CT-26 through endocytosis system, and achieve delayed drug release, and accumulate in tumor tissue by EPR effect.