Preparation, characterization and biodistribution of 10-hydroxycamptothecin loaded PEG-PHDCA nanoparticles

摘要

10-Hydroxycamptothecin (HCPT) is a promising anticancer agent against a broad spectrum of cancers. The clinical utilization is greatly limited by its instability and poor solubility in both water and organic solvents. In this paper, we synthesized poly (PEG cyanoacrylate-co-hexadecyl cyanoacrylate) PEG-PHDCA and prepared HCPT-loaded PEG-PHDCA nanoparticles by film-dispersion and hydration-sonication method. The result showed that the prepared nanoparticles demonstrated good stability and encapsulation efficiency was more than 80%, the average size was 141.6 ± 6.7 nm, the Zeta potential was −18.2 ± 2.2 mV and drug loading content was 2.92 ± 0.21%. In vitro drug release and in vivo pharmacokinetics of HCPT nanoparticles were compared with those of HCPT. The results demonstrated that the nanoparticles remarkably prolonged in vitro the release time and in vivo half life respectively. All studies in this paper demonstrated that PEG-PHDCA nanoparticles seem to be a appropriate delivery system for HCPT.