Patel Ashaben, Gaudana Ripal, Mitra Ashim K
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City , Kansas City, MO , USA.
J Microencapsul. 2014;31(6):542-50. doi: 10.3109/02652048.2014.885606. Epub 2014 Apr 3.
IgG-Fab fragment, a model antibody protein was hydrophobically modified by a novel approach of ion-pairing complexation. Three different sulphated ion-pairing agents were utilised including sodium dodecyl sulphate, taurocholic acid and dextran sulphate (DS). The formations of hydrophobic ion-pairing (HIP) complexes were dependant on pH and molar ratio of ion-pairing agent to Fab. Aqueous solubilities of HIP complexes were very low compared to Fab alone. In particular, when dextran sulphate was added as ion-pairing agent, formed Fab:DS HIP complexes were least soluble in water. Further, nanoparticles (NPs) loaded with drug and Fab:DS HIP complex were prepared and characterised with respect to encapsulation efficiency and size. We observed significant improvement in encapsulation efficiency for Fab:DS HIP complex-loaded nanoparticles. This study demonstrates a novel approach of formulating antibody-loaded nanoparticles which can also be employed for delivery of large antibodies.
免疫球蛋白G（IgG）-Fab片段是一种模型抗体蛋白，采用一种新型的离子对络合方法对其进行疏水修饰。使用了三种不同的硫酸化离子对试剂，包括十二烷基硫酸钠、牛磺胆酸和硫酸葡聚糖（DS）。疏水离子对（HIP）络合物的形成取决于pH值以及离子对试剂与Fab的摩尔比。与单独的Fab相比，HIP络合物的水溶性非常低。特别是，当加入硫酸葡聚糖作为离子对试剂时，形成的Fab:DS HIP络合物在水中的溶解度最低。此外，制备了负载药物和Fab:DS HIP络合物的纳米颗粒（NPs），并对其包封效率和尺寸进行了表征。我们观察到负载Fab:DS HIP络合物的纳米颗粒的包封效率有显著提高。本研究展示了一种制备负载抗体纳米颗粒的新方法，该方法也可用于递送大分子抗体。
