Zhang Xinge, Zhang Huijie, Wu Zhongming, Wang Zhen, Niu Haimei, Li Chaoxing
The Key Laboratory of Functional Polymer Materials of Ministry Education, Institute of Polymer Chemistry, Nankai University, Tianjin, China.
Eur J Pharm Biopharm. 2008 Mar;68(3):526-34. doi: 10.1016/j.ejpb.2007.08.009. Epub 2007 Aug 16.
The objective of this work was to explore the potential of polyethylene glycol-grafted chitosan (PEG-g-chitosan) nanoparticles as a system for improving the systemic absorption of insulin following nasal administration. Insulin-loaded PEG-g-chitosan nanoparticles were prepared by the ionotropic gelation of PEG-g-chitosan solution using tripolyphosphate ions as the crosslinking agent. The nanoparticles were in the size range 150-300 nm, had a positive electrical charge (+16 to +30 mV) and were associated with insulin (loading efficiency 20-39%). The physicochemical properties of nanoparticles were affected by the composition of the copolymer. In vitro insulin release studies showed an initial burst followed by a slow release of insulin. Intranasal administration of PEG-g-chitosan nanoparticles in rabbits enhanced the absorption of insulin by the nasal mucosa to a greater extent than a suspension of insulin-PEG-g-chitosan and control insulin solution. PEG-g-chitosan nanoparticles are promising vehicles for insulin transport through the nasal mucosa.
这项工作的目的是探索聚乙二醇接枝壳聚糖(PEG-g-壳聚糖)纳米颗粒作为一种改善胰岛素经鼻给药后全身吸收的系统的潜力。通过使用三聚磷酸根离子作为交联剂,使PEG-g-壳聚糖溶液发生离子凝胶化反应,制备了载胰岛素的PEG-g-壳聚糖纳米颗粒。纳米颗粒的尺寸范围为150-300 nm,带有正电荷(+16至+30 mV),并与胰岛素结合(载药效率为20-39%)。纳米颗粒的物理化学性质受共聚物组成的影响。体外胰岛素释放研究显示,胰岛素最初会有一个突释,随后是缓慢释放。在兔体内经鼻给药PEG-g-壳聚糖纳米颗粒比胰岛素-PEG-g-壳聚糖混悬液和对照胰岛素溶液更能增强鼻黏膜对胰岛素的吸收。PEG-g-壳聚糖纳米颗粒是胰岛素经鼻黏膜转运的有前景的载体。