Institute of Preventive Medicine, National Defense Medical Center, Sanhsia, Taipei 237, Taiwan, ROC.
Acta Biomater. 2011 Oct;7(10):3804-12. doi: 10.1016/j.actbio.2011.06.026. Epub 2011 Jun 24.
In this study, the potential of chondroitin sulfate (ChS)-chitosan (CS) nanoparticles (NPs) for the delivery of proteins was investigated. ChS-CS NPs were prepared by ionic cross-linking of CS solution with ChS. The aggregation line, particle size and zeta potential were investigated as a function of the pH, weight ratio and concentration. The water content and formation yield of the NPs were measured by gravimetry. Results indicated that ChS-CS NPs showed a higher degree of ionic cross-linking and formation yield than sodium tripolyphosphate-CS NPs. Fluorescein isothiocyanate conjugate bovine serum albumin (FITC-BSA), a model protein drug, was incorporated into the ChS-CS NPs. The encapsulation efficiency was obviously increased with the increase in initial FITC-BSA concentration and was as high as 90%. In vitro release studies of ChS-CS NPs showed a small burst effect following a continued and controlled release. Cytotoxicity tests with Caco-2 cells showed no toxic effects of ChS-CS NPs. The ex vivo cellular uptake studies using Caco-2 and HEK-293 cells indicated that NPs were found to be endocytosed into the cells. In conclusion, ChS-CS NPs are a potential new delivery system for the transport of hydrophilic compounds such as proteins.
在这项研究中，研究了硫酸软骨素（ChS）-壳聚糖（CS）纳米粒子（NPs）作为蛋白质传递载体的潜力。ChS-CS NPs 通过 CS 溶液与 ChS 的离子交联制备。考察了聚集线、粒径和zeta 电位随 pH 值、重量比和浓度的变化。通过重量法测量 NPs 的含水量和形成产率。结果表明，与三聚磷酸钠-CS NPs 相比，ChS-CS NPs 具有更高的离子交联程度和形成产率。荧光素异硫氰酸酯结合牛血清白蛋白（FITC-BSA），一种模型蛋白药物，被包裹到 ChS-CS NPs 中。随着初始 FITC-BSA 浓度的增加，包封效率明显增加，高达 90%。ChS-CS NPs 的体外释放研究表明，在持续控制释放后会出现小的突释效应。用 Caco-2 细胞进行的细胞毒性试验表明，ChS-CS NPs 没有毒性作用。用 Caco-2 和 HEK-293 细胞进行的体外细胞摄取研究表明，纳米颗粒被内吞到细胞中。总之，ChS-CS NPs 是一种潜在的新型亲水化合物（如蛋白质）输送系统。
