pH-Responsive Cellulose-Based Microspheres Designed as an Effective Oral Delivery System for Insulin,ACS Omega

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pH-Responsive Cellulose-Based Microspheres Designed as an Effective Oral Delivery System for Insulin
ACS Omega ( IF 3.7 ) Pub Date : 2021-01-24 , DOI: 10.1021/acsomega.0c04946
Yaqi Gong ₁ , Shabbir Mohd ₁ , Simei Wu ₁ , Shilin Liu _{2,

3} , Ying Pei ₃ , Xiaogang Luo _{1,

3}

Affiliation

Functional modified cellulose microsphere (CMs) materials exhibit great application potential in drug various fields. Here, we designed pH-responsive carboxylated cellulose microspheres (CCMs) by the citric/hydrochloric acid hydrolysis method to enhance oral bioavailability of insulin by a green route. The CMs were high purity cellulose that dissolved and regenerated from a green solvent by the green sol–gel method. The prepared microspheres were characterized by spectroscopic techniques, such as field emission scanning electron microscopy (FE-SEM), Fourier transform infrared spectrum (FT-IR), X-ray diffraction (XPS), etc. The spherical porous structure and carboxylation of cellulose were confirmed by FESEM and FT-IR, respectively. Insulin was loaded into the CCMs by electrostatic interactions, and the insulin release was controlled through ionization of carboxyl groups and proton balance. In vitro insulin release profiles demonstrated the suppression of insulin release in artificial gastric fluid (AGF), while a significant increase at artificial intestinal fluid (AIF) was observed. The insulin release profile was fitted in Korsmeyer–Peppas kinetic model, and insulin release was governed by the Fickian diffusion mechanism. The stability of the secondary structure of insulin was studied by dichroism circular. Excellent biocompatibility and no cytotoxicity of designed CCMs cast them as a potential oral insulin carrier.

中文翻译：

基于pH响应的纤维素微球被设计为胰岛素的有效口服输送系统

功能性改性纤维素微球（CMs）材料在药物各个领域具有巨大的应用潜力。在这里，我们通过柠檬酸/盐酸水解方法设计了pH响应的羧化纤维素微球（CCM），以通过绿色途径增强胰岛素的口服生物利用度。CM是通过绿色溶胶-凝胶法从绿色溶剂中溶解并再生的高纯度纤维素。制备的微球通过光谱技术进行表征，例如场发射扫描电子显微镜（FE-SEM），傅立叶变换红外光谱（FT-IR），X射线衍射（XPS）等。纤维素的球形多孔结构和羧化分别由FESEM和FT-IR确认。通过静电相互作用将胰岛素加载到CCM中，通过羧基离子化和质子平衡来控制胰岛素的释放。体外胰岛素释放曲线表明，在人工胃液（AGF）中胰岛素释放受到抑制，而在人工肠液（AIF）中则显着增加。胰岛素释放曲线符合Korsmeyer-Peppas动力学模型，胰岛素释放受Fickian扩散机制控制。通过二色性图研究了胰岛素二级结构的稳定性。设计的CCM具有出色的生物相容性和无细胞毒性，使它们成为潜在的口服胰岛素载体。而观察到人工肠液（AIF）明显增加。胰岛素释放曲线符合Korsmeyer-Peppas动力学模型，胰岛素释放受Fickian扩散机制控制。通过二色性图研究了胰岛素二级结构的稳定性。设计的CCM具有出色的生物相容性和无细胞毒性，使它们成为潜在的口服胰岛素载体。而观察到人工肠液（AIF）明显增加。胰岛素释放曲线符合Korsmeyer-Peppas动力学模型，胰岛素释放受Fickian扩散机制控制。通过二色性图研究了胰岛素二级结构的稳定性。设计的CCM具有出色的生物相容性和无细胞毒性，使它们成为潜在的口服胰岛素载体。

更新日期：2021-02-02

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