POLYMER DERIVATIVES OF GLUCOCORTICOID HORMONES

The activated derivatives of hydrocortisone, prednisolone, and dexamet hasone, crotonates, methacrylates, and haloacetates were synthesized b y acylating native hormones with chloroanhydrides or the corresponding acids. Water-soluble conjugates of steroids which bear a positive sig n were obtained by reactions in chains of copolymers of vinylpyrrolido ne and vinyl-, allylamine, diethylaminoethyl methacrylate and diethyla minoethyl crotonate with steroid haloacetates. Water-soluble derivativ es bearing a negative sign were obtained by the acylation of steroids using vinylpyrrolidone copolymer with maleic anhydride. Non-ionogenic water-soluble polymers were synthesized by the copolymerization of vin ylpyrrolidone with steroid methacrylates and crotonates. Cationic and anionic polyelectrolytes bearing steroid units were also obtained by t he ternary copolymerization of vinylpyrrolidone with steroid crotonate s, diethylaminoethyl crotonate and crotonic acid. The polymer steroids exhibit high specificity In the interaction with trans-cortine and an tybodies to cortisol and to target cells, thymocytes. The in vivo expe riments revealed anti-inflammatory activity on the level of native hor mones. The antishock activity of polymer conjugates exeeds that of nat ive hormones. It was detected that negative side effects characteristi c of native hormones decrease markedly after they are: bonded to a mol ecule of water-soluble polymer. No effect of the sign of the macromole cule on the biological activity of modified hormones was detected.