To improve the efficiency of niosomal drug delivery, here we employed two tactics. First, niosomes were magnetized using FeO@SiO mangnetic nanoparticles, and second, their surface was modified by PEGylation. PEGylation was intended for increasing the bioavailability of niosomes, and magnetization was used for rendering them capable of targeting specific tissues. These PEGylated magnetic niosomes were also loaded with Carboplatin, an antitumor drug. Next, these niosomes were studied in terms of size, morphology, zeta potential, and drug entrapment efficiency. Then, the in vitro drug release from these modified niosomes was compared to that of both naked and nonmagnetized niosomes. Interestingly, although loading of naked-niosomes with magnetic particles lead to an increase in the rate of drug release, PEGylation of these magnetized niosomes caused a more sustained drug release. Thus, PEGylation of magnetic niosomes, besides improving their bioavailability, caused a slower and sustained release of the drug over time. Finally, studying the in vitro effectives of niosomal formulations towards MCF-7, a breast cancer cell line, showed that PEGylated magnetic niosomes had a satisfactory toxicity towards these cells in the presence of an external magnetic field. In conclusion, PEGylated magnetic niosomes showed enhanced qualities regarding the controlled release and delivery of drug. Graphical abstract ᅟ.