Yao Qian, Hou Shi-Xiang, Zhang Xuan, Zhao Gang, Gou Xiao-Jun, You Jin-Zong
Laboratory of Chemistry of Traditional Chinese Medicine, School of Biological Industry, Chengdu University, Chengdu 610106, China.
Yao Xue Xue Bao. 2007 May;42(5):557-61.
Biotinylated chitosan nanoparticles (Bio-CS-NP) were prepared for the active delivery to cancer cells and its characterization was investigated in this study. The preparation process included two steps. First, biotinylated chitosan ( Bio-CS ) was obtained through a reaction between sulfosuccinimidobiotin and chitosan (CS). Second, Bio-CS-NP were prepared by the precipitation of Bio-CS with sodium chloride solution. With a biotin reagent box, the conjugation densities of biotin on the surface of Bio-CS-NP were determined. The morphology and diameter of the nanoparticles were assayed by transmission electron microscope (TEM) and laser light scattering particle analyzer, respectively. The uptake of nanoparticles by human hepotacarcinoma HepG2 cells, for example, Bio-CS-NP and chitosan nanoparticles (CS-NP) without any modification, was quantitatively examined. The results indicated that the conjugation densities of biotin on the surface of Bio-CS-NP were 2.2 biotin CS. Bio-CS-NP were spherical, smooth on the surface. The average diameter was 296.8 nm. The polydispersion index was 0.155. The uptake of Bio-CS-NP by HepG2 cells was much higher than that of CS-NP (P < 0.05). It demonstrated that Bio-CS-NP can be applied as a new vehicle to actively deliver anticancer drugs to tumor cells. The method for the determination of biotin was simple and practical.
本研究制备了生物素化壳聚糖纳米颗粒(Bio-CS-NP)用于向癌细胞的主动递送,并对其进行了表征。制备过程包括两个步骤。首先,通过磺基琥珀酰亚胺生物素与壳聚糖(CS)反应获得生物素化壳聚糖(Bio-CS)。其次,用氯化钠溶液沉淀Bio-CS制备Bio-CS-NP。使用生物素试剂盒测定Bio-CS-NP表面生物素的结合密度。分别通过透射电子显微镜(TEM)和激光散射粒子分析仪测定纳米颗粒的形态和直径。定量检测了纳米颗粒被人肝癌HepG2细胞的摄取情况,例如Bio-CS-NP和未进行任何修饰的壳聚糖纳米颗粒(CS-NP)。结果表明,Bio-CS-NP表面生物素的结合密度为2.2个生物素/壳聚糖。Bio-CS-NP呈球形,表面光滑。平均直径为296.8 nm。多分散指数为0.155。HepG2细胞对Bio-CS-NP的摄取远高于CS-NP(P < 0.05)。这表明Bio-CS-NP可作为一种新型载体,用于向肿瘤细胞主动递送抗癌药物。生物素的测定方法简单实用。