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

IF 6.1 3区 医学 Q1 MATERIALS SCIENCE, BIOMATERIALS
Di Shen, Haojie Yu, Li Wang, Xiang Chen, Jingyi Feng, Qian Zhang, Wei Xiong, Jin Pan, Yin Han and Xiaowei Liu
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引用次数: 10

Abstract

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.

Abstract Image

可生物降解苯硼酸修饰的ε-聚赖氨酸用于经透皮微针给药葡萄糖反应胰岛素†
带有胰岛素负载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和具有成本效益的颗粒,这仍然是一个很大的挑战。为此,本文合成了葡萄糖响应型4-羧基-3-氟苯硼酸接枝ε-聚赖氨酸(CFPBA-g-PL)。CFPBA-g-PL细胞毒性低,血液相容性好,无组织反应。研究了CFPBA-g-PL的药代动力学。通过简单的超声处理制备了cfppa -g- pl自组装颗粒。在体外实验中,CFPBA-g-PL的胰岛素负载颗粒(命名为INS/GRP-12.8)表现出基于拆解相关机制的葡萄糖响应性胰岛素递送性能。采用模压法制备了形貌均匀、透皮性能适中的INS/ grp -12.8包封微针贴片。INS/GRP-12.8经皮下注射可使stz诱导的糖尿病SD大鼠维持8小时以上的血糖正常,INS/GRP-12.8包封微针贴片经皮给药在体内也有降血糖作用。
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来源期刊
Journal of Materials Chemistry B
Journal of Materials Chemistry B MATERIALS SCIENCE, BIOMATERIALS-
CiteScore
11.50
自引率
4.30%
发文量
866
期刊介绍: Journal of Materials Chemistry A, B & C cover high quality studies across all fields of materials chemistry. The journals focus on those theoretical or experimental studies that report new understanding, applications, properties and synthesis of materials. Journal of Materials Chemistry A, B & C are separated by the intended application of the material studied. Broadly, applications in energy and sustainability are of interest to Journal of Materials Chemistry A, applications in biology and medicine are of interest to Journal of Materials Chemistry B, and applications in optical, magnetic and electronic devices are of interest to Journal of Materials Chemistry C.Journal of Materials Chemistry B is a Transformative Journal and Plan S compliant. Example topic areas within the scope of Journal of Materials Chemistry B are listed below. This list is neither exhaustive nor exclusive: Antifouling coatings Biocompatible materials Bioelectronics Bioimaging Biomimetics Biomineralisation Bionics Biosensors Diagnostics Drug delivery Gene delivery Immunobiology Nanomedicine Regenerative medicine & Tissue engineering Scaffolds Soft robotics Stem cells Therapeutic devices
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