Mehrotra Archana, Nagarwal Ramesh Chand, Pandit Jayanta Kumar
NRI Institute of Pharmaceutical Sciences, Bhopal (MP), India.
Chem Pharm Bull (Tokyo). 2011;59(3):315-20. doi: 10.1248/cpb.59.315.
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).
本研究旨在通过离子凝胶法结合均质化制备负载抗肿瘤药物洛莫司汀的壳聚糖纳米粒（LCNPs）。通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法对纳米粒的粒径、多分散指数（PDI）、表面形态、包封率、体外药物释放以及对人肺癌细胞系L132的细胞毒性进行表征。制备的纳米粒的粒径、zeta电位和包封率分别为75±1.1至637±1.6 nm（PDI为0.05±0.001至0.18±0.007）、37.2±0.21至53.8±0.18 mV以及66.74±1.4至98.0±1.8%。在扫描电子显微镜（SEM）和透射电子显微镜（TEM）图像中，颗粒呈球形，表面光滑。通过均质化处理进行机械剪切显著改变了纳米粒的尺寸。药物释放速率呈双相，在8小时内受扩散控制。与天然洛莫司汀（LMT）相比，LCNPs极大地抑制了本研究中使用的L132癌细胞系的生长。
