Lomustine loaded chitosan nanoparticles: Characterization and in-vitro cytotoxicity on human lung cancer cell line L132

Abstract

The aim of this work was to prepare chitosan nanoparticles loaded with antineoplastic drug Lomustine (LCNPs), by ionic-gelation method with homogenization. The nanoparticles were characterized for particle size, polydispersity index (PDI), surface morphology, encapsulation efficiency, in-vitro drug release and cytotoxicity on human lung cancer cell line L132 by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The particle size, zeta potential and encapsulation efficiency of prepared nanoparticles ranged from 75±1.1 to 637±1.6 nm (PDI from 0.05±0.001 to 0.18±0.007), 37.2±0.21 to 53.8±0.18 mV and 66.74±1.4 to 98.0±1.8% respectively. The particles were spherical in shape with smooth surface in scanning electron microscopy (SEM) and transmission electron microscopy (TEM) images. Mechanical shearing by homogenization treatment significantly changed the nanoparticle size. The drug release rate was biphasic and diffusion controlled over the 8 h. LCNPs greatly inhibited the growth of the L132 cancer cell line used in this study in comparison to the native Lomustine (LMT). © 2011 Pharmaceutical Society of Japan.