可生物降解的苯硼酸修饰的 ε-聚赖氨酸，用于通过经皮微针递送葡萄糖响应性胰岛素,Journal of Materials Chemistry B

当前位置： X-MOL 学术 › J. Mater. Chem. B › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

可生物降解的苯硼酸修饰的 ε-聚赖氨酸，用于通过经皮微针递送葡萄糖响应性胰岛素
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2021-07-13 , DOI: 10.1039/d1tb00880c
Di Shen ₁ , Haojie Yu ₁ , Li Wang ₁ , Xiang Chen ₁ , Jingyi Feng ₂ , Qian Zhang ₂ , Wei Xiong ₂ , Jin Pan ₂ , Yin Han ₃ , Xiaowei Liu ₁

Affiliation

带有载有胰岛素的葡萄糖反应颗粒的微针有望控制糖尿病患者的血糖水平。特别是这些微针的长期使用需要可生物降解且具有成本效益的颗粒，这仍然是很大的挑战。在本文中，合成了葡萄糖响应性 4-羧基-3-氟苯基硼酸接枝的 ε-聚赖氨酸 (CFPBA- g -PL ) 以满足这些要求。CFPBA- g - PL细胞毒性低，血液相容性好，无组织反应。还研究了 CFPBA- g -PL 的药代动力学。CFPBA- g -PL的自组装颗粒是通过简单的超声处理制备的。载有胰岛素的 CFPBA- g颗粒-PL（命名为 INS/GRP-12.8）基于体外分解相关机制呈现了葡萄糖反应性胰岛素递送性能。通过成型策略制备了形态均匀、皮肤渗透性能适中的 INS/GRP-12.8 封装微针贴片。INS/GRP-12.8通过皮下注射对STZ诱导的糖尿病SD大鼠持续超过8小时的正常血糖，并且INS/GRP-12.8包封的微针贴剂在体内也表现出透皮给药的降血糖性能.

"点击查看英文标题和摘要"

Biodegradable phenylboronic acid-modified ε-polylysine for glucose-responsive insulin delivery via transdermal microneedles

Microneedles with insulin-loaded glucose-responsive particles are promising to control the blood glucose levels of diabetic patients. In particular, the long-term usage of these microneedles calls for biodegradable and cost-effective particles, which are still large challenges. In this paper, glucose-responsive 4-carboxy-3-fluorophenylboronic acid-grafted ε-polylysine (CFPBA-g-PL) was synthesized to meet these requirements. CFPBA-g-PL had low cytotoxicity, good hemocompatibility and no tissue reaction. The pharmacokinetics of CFPBA-g-PL were also studied. The self-assembled particles of CFPBA-g-PL were prepared via simple ultrasonic treatment. The insulin-loaded particles of CFPBA-g-PL (named INS/GRP-12.8) presented a glucose-responsive insulin delivery performance based on the disassembly-related mechanism in vitro. The INS/GRP-12.8-encapsulated microneedle patch with a uniform morphology and moderate skin penetration performance was prepared via a molding strategy. INS/GRP-12.8 lasted for more than 8 hours of normoglycemia on STZ-induced diabetic SD rats via subcutaneous injection and the INS/GRP-12.8-encapsulated microneedle patch also showed a blood-glucose-level-lowering performance in vivo via transdermal administration.

更新日期：2021-07-13

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南