Silymarin (SIL) is a component extracted from Silybum marianum herb and is studied in medicine due to its protective activities on certain organs (liver, kidney, heart, brain). The review discusses some methods that increase silymarin bioavailability such as development of complexes with cyclodextrins, phospholipids, liposome and nanostructured material (hydroxyapatite-HAP). The interactions between SIL and alpha-lipoic acid, metallic nanoparticles (gold nanoparticles-GNP, and silver nanoparticles – SNP), some carotenoids (β-carotene and lycopene) and curcumin were debated too. Some combined treatments (e.g. SIL + curcumin) highlighted anticancer activity against colon cancer cells (DLD-1, HCT116 and LoVo) and protective effect against chemicals toxicity.