15August2020

Nano-Micro Letters

A Combinative Assembly Strategy Inspired Reversibly Borate-Bridged Polymeric Micelles for Lesion-Specific Rapid Release of Anti-Coccidial Drugs

Hao Cheng1,#, Huaqing Zhang1, #, Gujun Xu1, Jin Peng1, Zhen Wang1, Bo Sun2, Djamila Aouameur1, Zhechen Fan1, Wenxin Jiang1, Jianping Zhou1, *, Yang Ding1, *

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Nano-Micro Lett. (2020) 12: 155

First Online: 25 July 2020 (Article)

DOI:10.1007/s40820-020-00495-1

*Corresponding author. E-mail: zhoujianp60@163.com (J. Zhou); dydszyzf@163.com (Y. Ding)

 

Abstract

 


Toc

Stimuli-triggered drug delivery systems hold vast promise in local infection treatment for the site-specific targeting and shuttling of drugs. Herein, chitosan conjugates (SPCS) installed with sialic acid (SA) and phenylboronic acid (PBA) were synthesized, of which SA served as targeting ligand for coccidium and reversible-binding bridge for PBA. The enhanced drug-loading capacity of SPCS micelles were attributed to a combination assembly from hydrophobicity-driving and reversible borate-bridges. The drug-loaded SPCS micelles shared superior biostability in upper gastrointestinal tract. After reaching the lesions, the borate-bridges were snipped by carbohydrates under a higher pH followed by accelerated drug release; while SA exposure on micellar surface facilitated drug cellular internalization to eliminate parasites inside. The drug-micelles revealed an enhanced anticoccidial capacity with a higher index of 185.72 compared with commercial preparation. The dual-responsive combination of physicochemical assembly could provide an efficient strategy for the exploitation of stable, safe and flexible anti-infectious drug delivery systems.


 

Keywords

Combinative assembly strategy, Borate-bridged micelles, Dual-stimuli triggered release, Lesion-specific location, Coccidiosis control

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