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目的：为得到稳定有效的口服胰岛素制剂，对氰基丙烯酸异丁酯包裹胰岛素的机制进行了一系列的体外研究。方法：用凝胶层析法分离纳米包裹颗粒和游离的胰岛素，结合ＲＩＡ法、放射标记示踪以及作者设计的“抗体捕捉”实验，以阐明氰基丙烯酸异丁酯包裹胰岛素纳米颗粒的结构。结果：大部分胰岛素分子（８０％）与形成的纳米包裹颗粒紧密相连，处于包裹颗粒的表面，可以用ＲＩＡ法测到，而且对蛋白酶降解有一定抵抗作用。用乙腈溶解包裹颗粒，大部分胰岛素分子（８４％）并不在溶液中，而与聚合物相连。用抗胰岛素抗体与包裹胰岛素的颗粒反应，可以在电镜下观察到包裹颗粒被抗体捕获。结论：这些结果表明胰岛素分子并未被包裹于颗粒内部，也不是以简单吸附的方式与包裹颗粒相连，而可能通过共价结合的方式与氰基丙烯酸酯聚合物相结合
OBJECTIVE: To obtain a stable and effective oral insulin preparation, a series of in vitro studies were carried out on the mechanism of insulin encapsulation with isobutyl cyanoacrylate. METHODS: Nano-encapsulated particles and free insulin were separated by gel chromatography. The RIA method, radiolabeled tracer and the “Antibody Capture” experiment were designed to elucidate the structure of isobutyl cyanoacrylate encapsulated insulin nanoparticles. Results: Most of the insulin molecules (80%) were closely linked with the formed nano-encapsulated particles, which were located on the surface of the encapsulated particles and could be detected by RIA method and had some resistance to protease degradation. Dissolving the encapsulated particles with acetonitrile, most of the insulin molecules (84%) are not in solution but are attached to the polymer. Anti-insulin antibodies and insulin-coated particles react, you can observe under electron microscopy wrapped particles captured by the antibody. CONCLUSIONS: These results indicate that insulin molecules are not encapsulated in the interior of the particles, nor are they attached to the encapsulated particles in a simple adsorption fashion, but may be incorporated with cyanoacrylate polymers by covalent bonding