Preparations based on silybin are used as hepatoprotectors in the treatment of liver lesions of various etiologies. The main disadvantage limiting their use is low bioavailability associated with the low solubility of silybin in water. To solve this problem, numerous delivery systems are created that increase its solubility, including those based on biodegradable polymers. This study presents a method for producing a polymer composition containing silybin (PCS) based on copolymers of lactic and glycolic acids. The content of the active ingredient in the product is 5%, its entrapment efficiency in particles is more than 90%; the Z-average particle size in an aqueous suspension is about 200 nm, the polydispersity index is less than 0.2, and the zeta potential is from ‒1 to ‒5 mV. The high antioxidant activity of silybin in the polymer composition by galvanostatic coulometry, as well as in the reaction of the nonenzymatic autoxidation of adrenaline, is shown. In an in vivo study on a model of acute toxic hepatitis induced by carbon tetrachloride, the more pronounced hepatoprotective effect of PCS is found compared with free silybin.