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Updated: Oct 6, 2025

Modeling and Simulations of Olfactory Drug Delivery with Passive and Active Controls of Nasally Inhaled Pharmaceutical Aerosols
Published on: May 20, 2016
Internalization Mechanism of Phenylboronic-Acid-Decorated Nanoplatform for Enhanced Nasal Insulin Delivery
Xiaosong Wei1, Xiaozhuang Duan1, Yufei Zhang1
1Key Laboratory of Functional Polymer Materials of Ministry of Education, Institute of Polymer Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China.
Abstract:
Insulin injection causes great pain to the patient, and nasal mucosal administration of insulin is a novel route for the treatment of diabetes. This strategy could protect insulin from either extensive first-pass metabolism or enzyme degradation in the gastrointestinal tract. With the dynamic boronate esters reversibly formed by phenylboronic acid and diols on nasal mucosal epithelial cell surfaces, we herein developed phenylboronic-acid-functionalized dextran nanoplatforms to enhance the permeability of cargos and boost penetration. The nanoplatforms with excellent loading capacity exhibited significant endocytosis compared with naked insulin. The mechanism of endocytosis was involved in clathrin- and lipid raft/caveolae-dependent endocytic pathways. The in vivo nasal delivery of insulin suggested that these nanoplatforms did not trigger nasal epithelial inflammation and greatly decreased blood sugar levels and improved insulin bioavailability. Collectively, this proof-of-concept study demonstrates a novel carrier of phenylboronic-acid-decorated polymer for insulin delivery and provides a promising approach for the development of a diabetes therapeutic strategy.
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