title: Synthesis and characterization of folic acid modified water-soluble chitosan derivatives for folate-receptor-mediated targeting.
abstract: Three chemical modification methods of carboxymethylation, quaternization and hydroxypropylation were used to synthesize water-soluble chitosan derivatives. In order to study the feasibility of these chitosan derivatives as backbones of nuclear imaging agents, folic acid (FA) and Technetium-99m were introduced onto the water-soluble chitosan chains. The bifunctional chelating agent 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was conjugated to the folate grafted chitosan derivatives for chelating with radionuclides such as (64)Cu and (68)Ga. The structures of these new ligands were characterized with multiple methods. The solubility and stability of the (99m)Tc-complexes were both favorable. Further study of their radiochemical and biological properties will be performed to evaluate the usefulness of these water-soluble chitosan derivatives for nuclear imaging agent design.
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Huihui
authors.initials: H
authors.lastname: Jing
authors.forename: Zhide
authors.initials: Z
authors.lastname: Guo
authors.forename: Wenyan
authors.initials: W
authors.lastname: Guo
authors.forename: Wenjiang
authors.initials: W
authors.lastname: Yang
authors.forename: Peng
authors.initials: P
authors.lastname: Xu
authors.forename: Xianzhong
authors.initials: X
authors.lastname: Zhang
mesh_terms: D048271:Chitosan / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005240:Feasibility Studies; D005492:Folic Acid / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D011956:Receptors, Cell Surface / Q000187:drug effects*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet
chemical_list: D011956:Receptors, Cell Surface; D048271:Chitosan; D005492:Folic Acid