Abstract
BACKGROUND: Polyglycerol is an attractive hydrophilic building block of amphiphilic copolymers for biomedical and pharmaceutical applications due to its biocompatibility, facile chemical modification, and anti-fouling activity. Herein we introduce theranostic nanoemulsions incorporating anti-cancer therapeutic and contrast agents using linear polyglycerol-poly(ε-caprolactone) diblock copolymers (PG-b-PCL). Lipiodol is used as a core oil that dissolves paclitaxel and serves as a contrast agent for computer tomography (CT). METHODS: PG-b-PCL is synthesized by three-step processes: polymerization of ethoxyethyl glycerol ether; ring-opening polymerization of ε-caprolactone; and deprotection of the PEEGE block. In vitro cytotoxicity of the polyglycerolated lipiodol nanoemulsions is demonstrated using HeLa ovarian cancer cells. The applicability of the prepared nanoemulsions as a contrast agent for CT imaging is also evaluated using micro-CT. RESULTS: Three compositions of PG-b-PCL with different block lengths are synthesized to prepare nanoemulsions. The polyglycerolated lipiodol nanoemulsions exhibit excellent anti-cancer activities, while placebo nanoemulsions have no significant cytotoxicity under the same condition. Micro-CT imaging of the nanoemulsions confirms the ability of nanoemulsions as a contrast agent. CONCLUSIONS: This study suggests that PG-b-PCL is a promising polymeric emulsifier for effective stabilization and surface functionalization of drug delivery nanocarriers for therapeutic and imaging agents.