Abstract
HighlightsA 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.
Highlights
Livestock infectious diseases caused by various microorganisms are widespread and economically significant, the outbreak of which may induce serious food safety and animal food storage issues [1,2,3]
Compared with CS copolymer which possessed an obvious peak at 899 cm−1 from β-(1,4) glucosidic bond and characteristic absorption peaks of CS at 1000–1150 cm−1, PCS conjugates displayed additional absorption peaks at 1720 cm−1 corresponding to stretching vibration of amide (C=O), 810 and 708 cm−1 corresponding to in-plane bending vibration of benzene (Ar–H) and 1442 cm−1 corresponding to stretching vibration of boric acid ester (B-O)
The graft degree increased along with the feeding amount of Carboxyphenylboronic acid (CPBA) moieties (Table S1) and reached its maximum when CPBA reacted with CS at a molar ratio of 1.5: 1. Polymers of P1.0CS and P1.5CS were applied for further conjugation with various amount of sialic acid (SA) (Tables S2 and S3)
Summary
Livestock infectious diseases caused by various microorganisms are widespread and economically significant, the outbreak of which may induce serious food safety and animal food storage issues [1,2,3]. The coccidiosis is of high sensitivity to chemotherapy during the schizozoite period of oral–fecal life cycle [5] Aiming at this key period, numerous active ingredients are introduced for coccidiostats, among which triazine benzacetonitril anti-coccidial drugs are of broad spectrum and high efficacy [6]. The DIC-loaded micelles were expected to remain stable before reaching the infected cecum site, while the in-core borate bridges were snipped by high-concentrated glucose under high pH value of cecum, generating a loose nanostructure and accelerated payload release. The nature bacteriostatic activity of chitosan can prevent occurrence of secondary infection and promote wound healing This dual-stimuli responsive micellar system offers an efficient nanocarrier platform with great potential for site-specific delivery of anti-infectious agents
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
