Sarmento B, Ferreira D C, Jorgensen L, van de Weert M
Department of Pharmaceutical Technology, Faculty of Pharmacy of the University of Porto, Porto, Portugal.
Eur J Pharm Biopharm. 2007 Jan;65(1):10-7. doi: 10.1016/j.ejpb.2006.09.005. Epub 2006 Sep 24.
The aim of the present study was to probe the structural integrity of insulin after being entrapped into chitosan/alginate nanoparticles produced by ionotropic polyelectrolyte pre-gelation. By manipulating the alginate:chitosan mass ratio and the pH during nanoparticle production, desired nanoparticles with a mean size of 850 (+/-88)nm and insulin association efficiency of 81 (+/-2)% were obtained. Insulin secondary structure was assessed by Fourier transform infrared (FTIR) and circular dichroism (CD) after entrapment into nanoparticles and after release from the particles under gastrointestinal simulated conditions. FTIR second-derivative spectra and area-overlap compared to an insulin standard confirmed that no significant conformational changes of insulin occurred in terms of alpha-helix and beta-sheet content. Far-UV-CD spectra corroborated the preservation of insulin structure during the nanoparticle production procedure. The presented nanoparticulate system is a promising carrier for insulin oral delivery since it preserves insulin structure and therefore also, potentially, its bioactivity.
本研究的目的是探究胰岛素包封于离子型聚电解质预凝胶化制备的壳聚糖/海藻酸钠纳米颗粒后其结构的完整性。通过在纳米颗粒制备过程中调控海藻酸钠与壳聚糖的质量比及pH值,获得了平均粒径为850(±88)nm且胰岛素包封效率为81(±2)%的理想纳米颗粒。在胰岛素包封于纳米颗粒后以及在胃肠道模拟条件下从颗粒中释放后,通过傅里叶变换红外光谱(FTIR)和圆二色光谱(CD)对胰岛素的二级结构进行了评估。与胰岛素标准品相比,FTIR二阶导数光谱和面积重叠结果证实,就α-螺旋和β-折叠含量而言,胰岛素未发生显著的构象变化。远紫外-CD光谱证实了在纳米颗粒制备过程中胰岛素结构得以保留。所呈现的纳米颗粒系统是一种有前景的胰岛素口服递送载体,因为它保留了胰岛素的结构,因此也可能保留其生物活性。