amphiphilic di-block and tri-block copolymers of poly(ethylene glycol) (PEG) and poly(ε-caprolactone) (PCL) with surface modified super-paramagnetite Fe3O4 nanoparticles (magnetic nanoparticles (MNPs)). The synthesized block copolymers (methoxy poly(ethylene glycol) (mPEG)–PCL and PCL–PEG–PCL) were characterized by Fourier transform infrared (FT-IR), 1H nuclear magnetic resonance (1HNMR), gel permeation chromatography (GPC), scanning electron microscopy (SEM), and differential scanning calorimetry (DSC), and their properties such as critical micelle concentration, hydrophilicity to lipophilicity balance, and hydrolytic degradation were investigated. The block copolymers were functionalized with terminal azide groups (mPEG–PCL(N3) and (N3)PCL–PEG–PCL(N3)), and magnetic Fe3O4 nanoparticles were surface modified with poly(acrylic acid) (PAA) and propargyl alcohol (MNP–PAA–C≡CH). Magnetic nanocarriers were synthesized by click reaction between azide-terminated block copolymers and MNP–PAA–C≡CH and characterized by FT-IR, thermogravimetric analysis (TGA), dynamic light scattering (DLS), vibrating sample magnetometer (VSM), and transmission electron microscopy (TEM), and cytotoxicity was investigated by methyl thiazolyl tetrazolium assay. In vitro drug loading and release and release kinetics were investigated.