Poly(lactide-co-glycolide) nanoparticles as carriers for norcantharidin

Norcantharidin (NCTD) is one of the new chemotherapy agents that have anti-tumor activity. However, the clinical potential of NCTD is limited by its high systemic toxicity, poor solubility in physiological environment and short half-life. In this paper, NCTD loaded poly(lactide-co-glycolide) (PLGA) nanoparticles for controlled delivery were prepared by using an interfacial deposition method. The resulting particles were characterized for their size, morphology, drug loading capacity, entrapment efficiency and in vitro drug release over an extended period of 12 days. The interfacial deposition technique succeeded in building a spherical, monodisperse nanoparticulate delivery system with high entrapment efficiency. The in vitro release lasts for more than 10 days showed a biphasic profile with an initial burst. The in vitro anti-tumor activity of NCTD-PLGA nanocapsules was assessed using the Human Hepatocellular Carcinoma cells SMMC-7721 by the MTT test. Ascites hepatoma (H-22H) and pulmonary adenocarcinoma (LA795) mice models were used to study the in vivo tumoricidal efficacy of NCTD delivery from the PLGA nanoparticles. The results demonstrate that i. v. or i.p. administration of this controlled release system could be of high clinical significance in cancer chemotherapy. (C) 2009 Elsevier B.V. All rights reserved,