A novel gel based on an ionic complex from a dendronized polymer and ciprofloxacin: Evaluation of its use for controlled topical drug release

MONICA GARCIA; JULIO CUGGINO; CLARISA ROSSET; PAULINA PAEZ; MIRIAM STRUMIA; RUBEN MANZO; CECILIA ALVAREZ I.; ALVARO GIMENEZ KAIRUZ

MATERIALS SCIENCE & ENGINEERING. C, BIOMIMETIC MATERIALS, SENSORS AND SYSTEMS

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2016 p. 236 - 246

0928-4931

The development and characterization of a novel, gel-type material based on a dendronized polymer (DP) loadedwith ciprofloxacin (CIP), and the evaluation of its possible use for controlled drug release, are presented in thiswork. DP showed biocompatible and non-toxic behaviors in cultured cells, both ofwhich are considered optimalproperties for the design of a final material for biomedical applications. These results were encouraging for theuse of the polymer loaded with CIP (as a drug model), under gel form, in the development of a new controlled-release system to be evaluated for topical administration. First, DP-CIP ionic complexes were obtainedby an acid-base reaction using the high density of carboxylic acid groups of the DP and the amine groups ofthe CIP. The complexes obtained in the solid state were broadly characterized using FTIR spectroscopy, XRP diffraction,DSC-TG analysis and optical microscopy techniques. Gels based on the DP-CIP complexes were easilyprepared and presented excellent mechanical behaviors. In addition, optimal properties for application on mucosalmembranes and skinwere achieved due to their high biocompatibility and acute skin non-irritation. Slow andsustained release of CIP toward simulated physiological fluids was observed in the assays (in vitro), attributed toion exchange phenomenon and to the drug reservoir effect. An in vitro bacterial growth inhibition assay showedsignificant CIP activity, corresponding to 38 and 58% of that exhibited by a CIP hydrochloride solution at similarCIP concentrations, against Staphylococcus aureus and Pseudomonas aeruginosa, respectively. However, CIP deliverywas appropriate, both in terms of magnitude and velocity to allow for a bactericidal effect. In conclusion, thefinal product showed promising behavior, which could be exploited for the treatment of topical and mucosal opportunisticinfections in human or veterinary applications.