Phenylboronic acid-functionalized glycopolymeric nanoparticles for biomacromolecules delivery across nasal respiratory.
The aim of this study was to explore the potential of the mucoadhesive and enzyme-inhibitory phenylboronic acid-functionalized glycopolymeric nanoparticles as carriers for the nasal delivery of biomacromolecules. The glycopolymers were prepared by the random copolymerization of 3-acrylamidophenylboronic acid and N-acetyl glucosamine. Insulin, as a model, was encapsulated within self-assembled glypolymeric nanoparticles. Nanoparticle size, insulin loading, and insulin release were characterized. In vitro cytotoxicity experiment showed the glycopolymers were cytocompatible (≥ 80% cell viability). Adhesiveness was determined from the absorption amount of mucin, reaching up to 1180 μg/mL. Moreover, the results obtained from in vivo administration of insulin-loaded p(AAPBA-r-MAGA) nanoparticles to rats evidenced that the nanoparticles enhanced insulin absorption across the nasal mucosal barrier and did not induce irritation of nasal mucosa. Thus, insulin-loaded nanoparticles were able to significantly decrease plasma glucose levels (more than 35% reduction). These results suggest that p(AAPBA-r-MAGA) nanoparticles have potential application for the nasal delivery of biomacromolecules.
Key Laboratory of Functional Polymer Materials of Ministry Education, Institute of Polymer Chemistry, Nankai University, Tianjin, China. zhangxinge@nankai.edu.cn
Xinge
X
Zhang
Yanxia
Y
Wang
Chao
C
Zheng
Chaoxing
C
Li
D000117:Acetylglucosamine / Q000737:chemistry*; D000268:Adhesiveness; D000281:Administration, Intranasal; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D001897:Boronic Acids / Q000737:chemistry*; D016503:Drug Delivery Systems; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D007328:Insulin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D046911:Macromolecular Substances; D008297:Male; D009077:Mucins / Q000378:metabolism; D053758:Nanoparticles; D009297:Nasal Mucosa / Q000187:drug effects / Q000378:metabolism; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar
C419826:3-acrylamidophenylboronic acid; D001786:Blood Glucose; D001897:Boronic Acids; D007004:Hypoglycemic Agents; D007328:Insulin; D046911:Macromolecular Substances; D009077:Mucins; D000117:Acetylglucosamine