Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto 862-0973, Japan.
J Pharm Sci. 2012 Aug;101(8):2891-9. doi: 10.1002/jps.23232. Epub 2012 Jun 7.
In this study, to clarify the utility of polypseudorotaxane (PPRX) hydrogels composed of poly(ethylene glycol) (PEG) and α- or γ-cyclodextrin (α- or γ-CyD) as a sustained-release system for protein drugs, we prepared CyD PPRX hydrogels including lysozyme, and then the release profiles of lysozyme from these hydrogels and the release mechanisms were investigated. The α- and γ-CyD formed PPRX hydrogels by threading onto one PEG chain and two PEG chains, respectively. The formation of α- and γ-CyD PPRX hydrogels including lysozyme was based on physical cross-linking arisen from their columnar structures. The in vitro release rates of lysozyme were markedly decreased by the encapsulation into CyD PPRX hydrogels. In addition, when release data were plotted according to Korsmeyer-Peppas model, the exponent values (n) in the α- and γ-CyD systems had no statistically significant difference, suggesting that these release mechanisms were almost same. In conclusion, these results suggest that α- and γ-CyD PPRX hydrogels possess the potential as a sustained-release system for lysozyme.
在这项研究中,为了阐明由聚乙二醇(PEG)和α-或γ-环糊精(α-或γ-CyD)组成的聚轮烷水凝胶作为蛋白质药物的缓释系统的效用,我们制备了包括溶菌酶在内的 CyD 聚轮烷水凝胶,然后研究了溶菌酶从这些水凝胶中的释放情况和释放机制。α-和γ-CyD 通过分别将一个 PEG 链和两个 PEG 链穿入形成 PPRX 水凝胶。α-和γ-CyD 聚轮烷水凝胶的形成是基于其柱状结构产生的物理交联。溶菌酶被包封在 CyD PPRX 水凝胶中,其体外释放速率显著降低。此外,当根据 Korsmeyer-Peppas 模型绘制释放数据时,α-和γ-CyD 系统中的指数值(n)没有统计学上的显著差异,表明这些释放机制几乎相同。总之,这些结果表明,α-和γ-CyD 聚轮烷水凝胶具有作为溶菌酶的缓释系统的潜力。