Synthesis of raloxifene–chitosan conjugate: A novel chitosan derivative as a potential targeting vehicle

Abstract

Chitosan is a biocompatible, non-toxic and biodegradable biopolymer. Due to the presence of functional groups on its surface, it can be modified and used as a carrier in targeted drug/gene delivery systems.In this study, raloxifene (a selective estrogen receptor ligand) was conjugated to chitosan using different methods. The conjugates were investigated by means of FTIR, TGA and physical properties assessments. Cell viability was evaluated by XTT assay. FTIR and TGA results confirmed that the conjugation between chitosan and raloxifene occurred more efficiently when trimethyl chitosan in the presence of triethylamine and excess amount of linker was used. XTT assay on MCF-7 cell line illustrated that more than 80% of cells were viable after 24h exposure to selected molecules. These findings confirm that the conjugation of raloxifene–chitosan can occur successfully using special synthesis condition and this novel chitosan derivative can be introduced as a potential drug/gene targeting agent.