Preparation, characterization and biological evaluation of chitosanmoxifloxacin prodrugs for pharmaceuticals
OBJECTIVE: In recent years, excipient development has become major area of research in
pharmaceutical drug delivery because it influences the formulation development and drug
delivery process in various ways. In modern pharmaceutical science biopolymers are choice
of research as excipient because of their low toxicity, biocompatibility, biodegrability, stability
and renewable nature. Chitosan, a biodegradable polysaccharide derived from chitin and
found widely in nature, possesses properties making it particularly suitable as a carrier, including
its high viscosity, charge distribution and release mechanisms. Our present research
work includes preparation and characterization of chitosan-moxifloxacin conjugates designed
in accordance with specific biomedical requirements.
METHODS: In this research work chitosan based chitosan-moxifloxacin conjugates have
been successfully formulated by using distilled water and glacial acetic acid mixture and the
film was made by solution casting method. Formulated films were characterized by various
analytical methods such as UV, IR and DSC as well as biological methods.
RESULTS: The antibacterial activity of chitosan-moxifloxacin conjugates was tested against
various microorganisms viz, gram positive bacteria’s Streptococcus pneumoniae and Staphylococcus
aureus and the results indicated that the antibacterial activity of chitosan-moxifloxacin
conjugates was several time greater than that of parent drug moxifloxacin. This may
be due to the favorable pharmacokinetics, pharmacodynamics, excellent bacterial susceptibility
and good stability of the drug conjugates.
CONCLUSION: This proposed combination may result in the enhancement of the separate
activities of chitosan and moxifloxacin.
KEYWORDS: MFX (Moxifloxacin), CH (Chitosan), conjugate, prodrug, electrostaticinteraction,
Bayer. Avelox (moxifloxacin hydrochloride) Tablets Avelox I.V (moxifloxacin hydrochloride in sodium chloride injection). Food and Drug Administration, 2008; 19.