Silymarin (SIL) contains a various flavonolignans extracted from Silybum marianum and has an anti-cancer properties against a variety of cancers. In this study, two types of improved nanocarriers based on iron oxide magnetic nanoparticles (MNPs) including chitosan anchored onto silica coated and uncoated Fe 3 O 4 MNPs (Cs-f-SiO 2 @Fe 3 O 4 MNPs and Cs-f-Fe 3 O 4 MNPs) were successfully fabricated and characterized. Next, silymarin was loaded into the nanocarriers (SIL-Cs-f-SiO 2 @Fe 3 O 4 MNPs and SIL-Cs-f-Fe 3 O 4 MNPs). These systems were characterized and silymarin content, antioxidant activity and intrinsic cytotoxicity were assessed. The functionalization degree of silymarin was assessed by the Folin-Ciocalteu method, finding 120 mg of SIL/g of Cs-f-SiO 2 @Fe 3 O 4 MNPs and 99 mg of SIL/g of Cs-MNPs. The antioxidant activity of the silymarin after loading into Cs-f-SiO 2 @Fe 3 O 4 MNPs and Cs-f-Fe 3 O 4 MNPs was proved by DPPH method. These compounds have high antioxidant effect and their radical scavenging activity increased with increasing these concentrations. SIL-Cs-f-SiO 2 @Fe 3 O 4 MNPs showed higher antioxidant activity than the SIL-Cs-f-Fe 3 O 4 MNPs in same concentrations. The cytotoxicity of Cs-f-SiO 2 @Fe 3 O 4 MNPs and SIL-Cs-f-SiO 2 @Fe 3 O 4 MNPs against MCF-7 was investigated by MTT assay and IC50 values were 110.03 and 73.56 μgml À1 respectively. In conclusion, SIL-loaded MNPs can be used as drug delivery system on target in the treatment of cancer cells.