SYNTHESIS OF STARCH-BASED DRUG CARRIER FOR THE CONTROL RELEASE OF ESTRONE HORMONE/

The objective of this study was to provide new synthetic route to prep are starch as a potential carrier for controlled release of drugs. a s tarch was modified with bromoacetyl bromide in order to provide more r eactive sites for coupling of bioactive estrone and a suitable spacer between the drug carrier and the hormone. The degree of substitution ( D.S.) per anhydroglucose (AHG) unit was calculated from the bromine co ntent and ranged from 0.11 to 2.29, depending on the ratio of bromoace tyl bromide to starch. The starch-estrone conjugate was then synthesiz ed by reacting bromoacetylated starch with the sodium salt of estrone. The structures of bromoacerylated starch and starch-estrone conjugate were determined by means of FTIR, H-1 NMR, C-13 NMR and UV. Additiona lly, X-ray diffraction patterns showed the amorphous character of the bromoacetylated starches. (C) 1997 Elsevier Science Ltd.