Department of Geratology, The First People's Hospital of Yunnan Province, Kunming University of Science and Technology, Kunming 650032, People's Republic of China.
School of Basic Medical, Yunnan University of Chinese Medicine, Kunming, Yunnan 650500, People's Republic of China.
Nanotechnology. 2020 Sep 25;31(39):395601. doi: 10.1088/1361-6528/ab9e26. Epub 2020 Jun 18.
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.
基于半乳糖的聚合物是一种很有前途的药物输送材料。在此，通过“嵌段共聚物”法成功合成了一种新型的基于半乳糖的嵌段共聚物，称为 6-O-乙烯基癸二酸-D-吡喃半乳糖酯嵌段 3-丙烯酰胺苯硼酸 p(OVNG-b-AAPBA)。通过核磁共振氢谱(1 HNMR)和红外光谱(IR)证明了 p(OVNG-b-AAPBA)的结构，通过热重分析仪观察了其热稳定性，通过凝胶渗透色谱(GPC)证明了其分子量(Mw 和 Mn)。以上测试结果表明，成功合成了 p(OVNG-b-AAPBA)聚合物，其具有最佳的分子量和热稳定性，可用于研究药物输送系统。然后，将该嵌段共聚物制备成纳米颗粒（NP），这些 NP 具有令人满意的形态，并通过 MTT 和慢性动物毒理学试验验证了其安全性。此外，胰岛素被 p(OVNG-b-AAPBA)NP 包封，药物载药量和包封效率随聚合物中 AAPBA 的增加而增加。最后，本研究证实这些 NP 可有效维持糖尿病小鼠的血糖 96 h。总之，本研究表明，载胰岛素的基于半乳糖的聚合物-嵌段-3-丙烯酰胺苯硼酸 NP 具有缓释/葡萄糖响应的药物释放性能，可能在糖尿病治疗中发挥积极作用。
