1. Formation of inclusion complex of enrofloxacin with 2-hydroxypropyl- β -cyclodextrin.
- Author
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Ding Y, Pang Y, Vara Prasad CVNS, and Wang B
- Subjects
- Animals, Anti-Bacterial Agents chemistry, Anti-Bacterial Agents pharmacokinetics, Biological Availability, Enrofloxacin chemistry, Enrofloxacin pharmacokinetics, Rats, Solubility, 2-Hydroxypropyl-beta-cyclodextrin chemistry, Anti-Bacterial Agents administration & dosage, Drug Carriers chemistry, Enrofloxacin administration & dosage
- Abstract
Enrofloxacin, a third-generation fluoroquinolone, is a broad-spectrum antimicrobial drug against a lot of veterinary bacterial diseases. However, bactericidal activity of enrofloxacin is concentration-dependent and its poor aqueous solubility and bitter taste limit its development and application. Meanwhile, 2-hydroxypropyl- β -cyclodextrin (HP-β-CD), a widely used cyclodextrin analog, is a safe and an effective drug carrier. It forms inclusion complexes with its drug substrates and improves their physiochemical and pharmacokinetic properties. Enrofloxacin was also found to form a stable inclusion complex with HP-β-CD and different research groups have shown improved solubility for enrofloxacin by 32.5%, 9.25 and 165-fold. Our own efforts in this direction resulted in manifold improvement (916-fold) in its solubility compared to the previous studies. It was further shown that pharmaceutical properties, absorption and bioavailability, of enrofloxacin have also been significantly improved by complexation with HP-β-CD.
- Published
- 2020
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