• A combined assembly strategy from hydrophobicity-driving and reversible borate bridges is proposed for high drug-loading efficiency and superior stability.

• Intestinal environment-triggered drug delivery system represents an effective treatment for local infection due to the site-specific targeting and shuttling of drugs.

• The reduced dosage brought by the drug-loading micelles could solve the problem of drug residue in breeding industry.

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 was 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 anti-coccidial 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.

• 提出了疏水驱动和可逆硼酸盐桥的组合组装策略，以实现高载药效率和优异的稳定性。

• 肠道环境触发的药物输送系统代表了针对部位的靶向和穿梭药物，因此可以有效地治疗局部感染。

• 载药胶束带来的剂量减少可以解决养殖业的药物残留问题。

刺激触发的药物输送系统在局部感染治疗中具有针对特定部位靶向和穿梭药物的广阔前景。本文合成了装有唾液酸（SA）和苯基硼酸（PBA）的壳聚糖共轭物（SPCS），其中SA用作球菌的靶向配体和PBA的可逆结合桥。SPCS胶束的载药能力增强归因于疏水性驱动和可逆硼酸盐桥的组合组装。载有药物的SPCS胶束在上消化道中具有出色的生物稳定性。到达病变部位后，硼酸盐桥在较高pH下被碳水化合物切断，然后加速药物释放，而胶束表面的SA暴露促进了药物细胞的内在化，从而消除了体内的寄生虫。与商业制剂相比，药物胶束显示出更高的抗球虫能力，指数为185.72。理化组装的双重响应组合可以为开发稳定，安全和灵活的抗感染药物输送系统提供有效策略。