Paclitaxel-loaded PLA/PEG/fluorescein anticancer agent prepared by Ugi reaction

ABSTRACTTwo different fluorescent block copolymers of poly(lactic acid) (PLA) and polyethylene glycol (PEG) containing fluorescein grafted to the polymer chain were synthesized by Ugi four-component condensation (UFCC). The structure of these PEG–PLA copolymers was confirmed by 1H-NMR and fluorescence spectroscopy. Paclitaxel-loaded fluorescent microspheres (PCT-FMS1 and PCT-FMS2) were prepared from them by the single-emulsion solvent evaporation method. A kinetic study of drug release in vitro using high-performance liquid chromatography showed a prolonged and controlled release of paclitaxel. Anticancer activity of release medium against colorectal cancer cell line (Caco-2) was determined using the cell viability assay. Paclitaxel-loaded microspheres were able to inhibit cancer cell growth and colony formation. The main contribution of this work is to propose a new application for UFCC in the preparation of biomasked fluorescent drug delivery systems able to improve cancer treatment.