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Galactose-based polymer-containing phenylboronic acid as carriers for insulin delivery

机译：基于半乳糖的含聚合物的苯硼酸作为胰岛素递送的载体

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摘要

The galactose-based polymer is a promising drug delivery material. Herein, a new galactose-based block copolymer, termed as 6-O-vinyl sebacic acid-D-galactopyranosyl ester block 3-acrylamide phenylboric acid p(OVNG-b-AAPBA) was successfully synthesized by 'block copolymer' method. The structure of p(OVNG-b-AAPBA) was proved by nuclear magnetic hydrogen spectrum (1 HNMR) and infrared (IR), the thermal stability was observed by thermogravimetric analyzer, and the molecular weights (Mw and Mn) were demonstrated by Gel permeation chromatography (GPC). The above test results suggested that the polymer of p(OVNG-b-AAPBA) was successfully synthesized, and it had optimal molecular weight and thermal stability, which could be used for investigating the drug delivery system. Then, this block copolymer was prepared to the nanoparticle (NP), these NPs had a satisfactory morphology, and their safety was verified by MTT and chronic animal toxicology test. In addition, insulin was encapsulated by the p(OVNG-b-AAPBA) NPs, the drug loading rate and encapsulation efficiency increased with that of AAPBA in the polymer. Finally, this study confirmed that these NPs can effectively maintain the blood sugar of diabetic mice at 96 h. In conclusion, the current study suggested that the insulin-loaded galactose-based polymer-block-3-acrylamide phenylboric acid NPs had slow-release/glucose-responsive drug release performance, which might play an active role in the diabetes therapy.
机译：基于半乳糖基的聚合物是有希望的药物递送材料。这里，通过“嵌段共聚物”方法成功地合成了作为6-乙烯基癸二酸-D-半乳糖醇酯嵌段3-丙烯酰胺苯甲酸P（OVNG-B-AAPBA）的新的半乳糖基嵌段共聚物。通过核磁氢谱（1 hNMR）和红外（IR）证明了P（OVNG-B-AAPBA）的结构，通过热重分析仪观察热稳定性，并通过凝胶证明了分子量（MW和MN）渗透色谱法（GPC）。上述测试结果表明，P（OVNG-B-AAPBA）的聚合物成功合成，具有最佳的分子量和热稳定性，可用于研究药物递送系统。然后，将该嵌段共聚物制备给纳米颗粒（NP），这些NPS具有令人满意的形态，并通过MTT和慢性动物毒理学测试验证了它们的安全性。此外，通过P（OVNG-B-AAPBA）NPS包封胰岛素，药物负载率和封装效率随着聚合物中的AAPBA而增加。最后，本研究证实，这些NPS可以在96小时有效地维持糖尿病小鼠的血糖。总之，目前的研究表明，胰岛素加载的半乳糖基聚合物 - 嵌段-3-丙烯酰胺苯并酸NPS具有缓释/葡萄糖响应药物释放性能，这可能在糖尿病疗法中发挥积极作用。

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  • 来源
    《Nanotechnology》 |2020年第39期|共15页
  • 作者

    Zhong Yunhua; Song Bo; He Dan; Xia Zemei; Wang Peng; Wu Junzi; Li Yan;

  • 作者单位

    Kunming Univ Sci &

    Technol Dept Geratol Peoples Hosp Yunnan Prov 1 Kunming 650032 Yunnan Peoples R China;

    Yunnan Univ Chinese Med Sch Basic Med Kunming 650500 Yunnan Peoples R China;

    Yunnan Univ Chinese Med Sch Basic Med Kunming 650500 Yunnan Peoples R China;

    Yunnan Univ Chinese Med Sch Clin Med Kunming 650500 Yunnan Peoples R China;

    Yunnan Univ Chinese Med Sch Clin Med Kunming 650500 Yunnan Peoples R China;

    Kunming Univ Sci &

    Technol Dept Geratol Peoples Hosp Yunnan Prov 1 Kunming 650032 Yunnan Peoples R China;

    Kunming Univ Sci &

    Technol Dept Geratol Peoples Hosp Yunnan Prov 1 Kunming 650032 Yunnan Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 特种结构材料;
  • 关键词

    galactose-based polymer; p(OVNG-b-AAPBA); nanoparticle (NP); insulin delivery; glucose sensitivity;

    机译：基于半乳糖的聚合物;P（OVNG-B-AAPBA）;纳米粒子（NP）;胰岛素递送;葡萄糖敏感性;

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