Biodegradable phenylboronic acid-modified ε-polylysine for glucose-responsive insulin delivery via transdermal microneedles. Issue 30 (13th July 2021)

• Record Type: Journal Article
• Authors: Shen, Di; Yu, Haojie; Wang, Li; Chen, Xiang; Feng, Jingyi; Zhang, Qian; Xiong, Wei; Pan, Jin; Han, Yin; Liu, Xiaowei
• Is Part Of: Journal of materials chemistry. Volume 9:Issue 30(2021)
• Page Start: 6017
• Page End: 6028
• Publication Date: 2021-07-13
• Subjects: Materials -- Periodicals; Chemistry, Analytic -- Periodicals; Biomedical materials -- Research -- Periodicals; 543.0284
• DOI: 10.1039/d1tb00880c
• Languages: English
• ISSNs: 2050-750X

Abstract

Abstract : Microneedles with insulin-loaded glucose-responsive particles are promising to control the blood glucose levels of diabetic patients. 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.