Abstract In this paper, the β-cyclodextrin (β-CD) and biotin (Bi) were successfully grafted onto carboxymethyl chitosan (CMCS). And then the β-CD-Bi-CMCS nanoparticles (NPs) were prepared as oral nano-delivery carrier of protein drugs by ionic gelation method. The morphological feature of fabricated drug carrier was determined by dynamic light scattering and transmission electron microscopy. The result showed that the prepared NPs presented spherical structure with an average diameter of 138 nm. Bovine serum albumin (BSA) was selected as model protein drug that was entrapped in prepared drug carrier with satisfactory entrapment efficiency (79.18%) and loading content (3.96%). The drug release profiles of BSA/β-CD-Bi-CMCS NPs were studied at different pH environment for simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF). It was found that the BSA/β-CD-Bi-CMCS NPs displayed a pH dependent drug release profiles. After 72 h, the cumulative release amount of BSA in SGF, SIF, and SCF was about 20.57, 74.46, and 91%, respectively. Furthermore, the enzymatic degradation and cytotoxicity studies showed the synthesized β-CD-Bi-CMCS NPs had high chemical stability and biocompatibility. This work indicated that the β-CD-Bi-CMCS NPs had the potentiality as promising nanocarriers for oral delivery of protein drugs.

中文翻译：

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离子凝胶化β-环糊精-生物素-羧甲基壳聚糖纳米粒子作为蛋白质药物口服给药载体的制备

摘要 本文成功地将β-环糊精（β-CD）和生物素（Bi）接枝到羧甲基壳聚糖（CMCS）上。然后通过离子凝胶法制备β-CD-Bi-CMCS纳米颗粒（NPs）作为蛋白质药物的口服纳米递送载体。通过动态光散射和透射电子显微镜确定制备的药物载体的形态特征。结果表明，制备的纳米颗粒呈球形结构，平均直径为 138 nm。选择牛血清白蛋白（BSA）作为模型蛋白药物，将其包埋在制备好的药物载体中，包封率（79.18%）和负载量（3.96%）令人满意。研究了 BSA/β-CD-Bi-CMCS NPs 在不同 pH 环境下模拟胃液 (SGF) 的药物释放曲线，模拟肠液（SIF）和模拟结肠液（SCF）。发现 BSA/β-CD-Bi-CMCS NPs 显示出 pH 依赖性药物释放曲线。72 h 后，BSA 在 SGF、SIF 和 SCF 中的累积释放量分别约为 20.57、74.46 和 91%。此外，酶促降解和细胞毒性研究表明合成的 β-CD-Bi-CMCS NPs 具有较高的化学稳定性和生物相容性。这项工作表明 β-CD-Bi-CMCS NPs 具有作为口服蛋白质药物的有前途的纳米载体的潜力。酶促降解和细胞毒性研究表明合成的 β-CD-Bi-CMCS NPs 具有较高的化学稳定性和生物相容性。这项工作表明 β-CD-Bi-CMCS NPs 具有作为口服蛋白质药物的有前途的纳米载体的潜力。酶促降解和细胞毒性研究表明合成的 β-CD-Bi-CMCS NPs 具有较高的化学稳定性和生物相容性。这项工作表明 β-CD-Bi-CMCS NPs 具有作为口服蛋白质药物的有前途的纳米载体的潜力。