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Preparation, Characterization and Drug Release in Vitro of Galactosylated Chitosan-Graft-PEG Nanoparticles

机译:半乳糖基化壳聚糖-接枝-PEG纳米粒子的制备,表征和体外释药

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Abstract-Galactose group was coupled with chitosan for liver specificity, and Poly(ethylene glycol) was selected to modify galactosylated chitosan (GC) for stability in water and enhanced cell permeability. The chemical structure of galactosylated chitosan-graft-PEG (GCP) was characterized by FT-IR and 1H-NMR techniques. Norcantharidin was chosen as model drug and encapsulated within GCP nanoparticles through ionic gelification. Transmission electron microscope (TEM) and dynamic light scattering (DLS) were employed to characterize the nanoparticles fabricated for morphology, size with polydispersity index. Encapsulation efficiency (EE) and the release of norcantharidin in nanoparticles in vitro were measured by HPLC. Norcantharidin release from the nanoparticles exhibited a biphasic pattern, initial burst release and consequently sustained release. The experimental results show that the novel GCP nanoparticles may be used as a potential drug delivery system with passive and active hepatic targeting properties.
机译:摘要半乳糖基团与壳聚糖偶联可提高肝脏的特异性,并选择聚乙二醇修饰半乳糖基化壳聚糖(GC),以提高其在水中的稳定性并增强细胞通透性。通过FT-IR和1H-NMR技术对半乳糖基化壳聚糖-接枝PEG(GCP)的化学结构进行了表征。选择降冰片素作为模型药物,并通过离子凝胶化将其封装在GCP纳米颗粒中。采用透射电子显微镜(TEM)和动态光散射(DLS)表征制备的纳米颗粒的形态,尺寸和多分散指数。通过HPLC测量包封效率(EE)和降冰片素在纳米颗粒中的体外释放。从纳米颗粒释放的降冰片烷素显示出双相模式,最初的爆发释放和因此的持续释放。实验结果表明,新型GCP纳米颗粒可以用作具有被动和主动肝靶向特性的潜在药物递送系统。

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