Issue 30, 2021

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

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.

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

Supplementary files

Article information

Article type
Paper
Submitted
19 Apr 2021
Accepted
24 Jun 2021
First published
13 Jul 2021

J. Mater. Chem. B, 2021,9, 6017-6028

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

D. Shen, H. Yu, L. Wang, X. Chen, J. Feng, Q. Zhang, W. Xiong, J. Pan, Y. Han and X. Liu, J. Mater. Chem. B, 2021, 9, 6017 DOI: 10.1039/D1TB00880C

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