Department of Chemical Engineering, Aragon Institute of Nanoscience (INA), University of Zaragoza, Campus Río Ebro-Edificio I + D, C/ Poeta Mariano Esquillor S/N, 50018 Zaragoza, Spain; Networking Research Center on Bioengineering, Biomaterials and Nanomedicine, CIBER-BBN, 28029 Madrid, Spain.
Instituto Aragonés de Ciencias de la Salud (IACS), Zaragoza 50009, Spain; Aragon Institute for Health Research (IIS Aragon), Zaragoza 50009, Spain; Institute of Biocomputation and Physics of Complex Systems (BIFI), Joint Unit IQFR-CSIC-BIFI, Universidad de Zaragoza (UZ), Zaragoza, Spain; Centro de Investigación Biomédica en Red en el Área Temática de Enfermedades Hepáticas y Digestivas (CIBERehd), Barcelona, Spain.
Int J Biol Macromol. 2018 Nov;119:413-422. doi: 10.1016/j.ijbiomac.2018.07.143. Epub 2018 Jul 23.
Bovine Serum Albumin (BSA) and Horseradish Peroxidase (HRP) have been encapsulated within microparticulated matrices composed of Eudragit RS100 by the water-in-oil-in-water double emulsion solvent evaporation method. Good encapsulation efficiencies were achieved for BSA and HRP, 88.4 and 95.8%, respectively. The stability of the loaded proteins was confirmed by using circular dichroism and fluorescence. The gastroresistance of the protein-loaded microparticles was evaluated under simulated gastric conditions demonstrating the preservation of the structural integrity of the proteins loaded inside the particles. The enzymatic activity of HRP after being released from the enteric microparticles was evaluated by using the peroxidase substrate, revealing that the released enzyme preserved its 100% function. The high drug loadings achieved, reduced cytotoxicity and efficient gastric protection point out towards the potential use of those carriers as oral delivery vectors of therapeutic proteins offering a more controlled targeted release in specific sites of the intestine and an enhanced gastrointestinal absorption.
牛血清白蛋白（BSA）和辣根过氧化物酶（HRP）已被包封在由 Eudragit RS100 组成的微粒基质中，采用水包油包水双乳液溶剂蒸发法。BSA 和 HRP 的包封效率分别达到了 88.4%和 95.8%。通过圆二色性和荧光证实了负载蛋白质的稳定性。在模拟胃条件下评估了载蛋白微球的胃耐受性，证明了载于颗粒内部的蛋白质的结构完整性得到了保留。用过氧化物酶底物评估从肠溶微球中释放的 HRP 的酶活性，表明释放的酶保持其 100%的功能。实现的高药物载药量、降低的细胞毒性和有效的胃保护表明，这些载体可用作治疗性蛋白质的口服递药载体，在肠道的特定部位提供更受控的靶向释放，并增强胃肠道吸收。
