Hyperbranched poly (amine-ester)-poly(ε-caprolactone) copolymer and their nanoparticles as camptothecin delivery system

Abstract

A new amphiphilic hyperbranched poly (amine-ester)-poly(e-caprolactone) copolymer (HPAE-co-PCL) was synthesized by ring-opening polymerization of e-caprolactone and branched poly (amine-ester) (HPAE-OHs) with Sn(Oct)2 as catalyst. The chemical structures of copolymers were determined by FT-IR, 1H-NMR (13C-NMR), thermo gravimetric analysis apparatus (TGA) and differential scanning calorimetry (DSC). Camptothecin (CPT)-loaded copolymer nanoparticles were prepared by the oil-in water (o/w) emulsion technique method. Their physicochemical characteristics, e.g. morphology and nanoparticles size distribution were then evaluated by means of fluorescence spectroscopy, environmental scanning electron microscopy (ESEM), and dynamic light scattering (DLS). CPT-loaded nanoparticles assumed a spherical shape and have unimodal size distribution. It was found that the chemical composition of the nanoparticles was a key factor in controlling nanoparticles size, drug-loading content, and drug release behavior. As the molar ratio of e-caprolactone to HPAE increased, the nanoparticles size and drug-loading content increased, and the drug release rate decreased. The antitumor activity of the CPT-loaded HPAE-co-PCL nanoparticles against human hepatoma HEPG2 cells was evaluated by 3-(4, 5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The CPT-loaded HPAE-co-PCL nanoparticles showed comparable anticancer efficacy with the free drug.