Chitosan-Based Ciprofloxacin Extended Release Systems: Combined Synthetic and Pharmacological (In Vitro and In Vivo) Studies

Ciprofloxacin is one of the most effective antibiotics, but it is characterized by a range of side effects. Elaboration of drug-releasing systems which allow to diminish toxicity of ciprofloxacin is a challenging task in medicinal chemistry. The current study is focused on development of new ciprofl...

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Published in:Molecules (Basel, Switzerland) Switzerland), 2022-12, Vol.27 (24), p.8865
Main Authors: Egorov, Anton R, Kurliuk, Aleh V, Rubanik, Vasili V, Kirichuk, Anatoly A, Khubiev, Omar, Golubev, Roman, Lobanov, Nikolai N, Tskhovrebov, Alexander G, Kritchenkov, Andreii S
Format: Article
Language:English
Subjects:
Acoustics
Animals
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial activity
Antibiotics
Antiinfectives and antibacterials
Aqueous solutions
Biocompatibility
Biopolymers
Carbodiimide
Chemistry, Pharmaceutical
Chitosan
Chitosan - chemistry
Chitosan - pharmacology
Ciprofloxacin
Ciprofloxacin - chemistry
Ciprofloxacin - pharmacology
Conjugation
Drug Liberation
In vivo methods and tests
Infectious diseases
Molecular weight
Nanoparticles
Nanoparticles - chemistry
Polymers
Rats
Self-assembly
Side effects
Subacute toxicity
Ultrasonic imaging
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Summary:Ciprofloxacin is one of the most effective antibiotics, but it is characterized by a range of side effects. Elaboration of drug-releasing systems which allow to diminish toxicity of ciprofloxacin is a challenging task in medicinal chemistry. The current study is focused on development of new ciprofloxacin releasing systems (CRS). We found that ultrasound efficiently promotes -dicyclohexyl carbodiimide-mediated coupling between COOH and NH functionalities in water. This was used for conjugation of ciprofloxacin to chitosan. The obtained ciprofloxacin/chitosan conjugates are capable of forming their self-assembled nanoparticles (SANPs) in aqueous medium. The SANPs can be additionally loaded by ciprofloxacin to form new CRS. The CRS demonstrated high loading and encapsulation efficiency and they are characterized by extended release profile (20 h). The elaborated CRS were tested in vivo in rats. The in vivo antibacterial effect of the CRS exceeded that of the starting ciprofloxacin. Moreover, the in vivo acute and subacute toxicity of the nanoparticles was almost identical to that of the chitosan, which is considered as the non-toxic biopolymer.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules27248865