Tailoring of alginate/gelatin microspheres properties for oral Ciprofloxacin-controlled release against Pseudomonas aeruginosa

ISLAN GA; CASTRO GR

DRUG DELIVERY

TAYLOR & FRANCIS INC

Lugar: Londres; Año: 2014 vol. 21 p. 615 - 662

1071-7544

AbstractContext: Ciprofloxacin (Cip) is a broad spectrum antibiotic frequently used in the treatmentof infectious diseases caused by Pseudomonas aeruginosa. Cip oral administration is commonlyassociated with poor drug biodisponibility, gastrointestinal tract irritation, and toxic undesirableside effects.Objective: The aim of this work is to provide an oral biopolymeric system for controlled releaseof Cip.Materials and methods: Alginate/gelatin blend microspheres were crosslinked in the presenceof 1,2-propylene glycol, calcium, and glutaraldehyde. Studies of Cip encapsulation and releasewere performed. Matrix characteristics were studied simultaneously by optical microscopyand Fourier transform infrared spectroscopy (FTIR) using synchrotron light, and bytexturometric analysis. Microsphere surface topologies were observed by scanning electronmicroscopy (SEM), atomic force microscopy (AFM), and epifluorescence microscopy.Results: Microspheres crosslinked with glutaraldehyde showed about 80% Cip encapsulationand less than 10% Cip release under simulated gastric conditions in 15 min, while a controlledrelease profile was observed at intestinal environment conditions. Antimicrobial activity againstP. aeruginosa showed an increasing bacterial growth inhibition in time. Finally, bovine serumalbumin (BSA) was used as model protein for binding of macromolecules onto active surfaceof microspheres, with a consequently modulation of Cip release.Discussion and conclusions: The results are indicating that alginate/gelatin matrix crosslinkedvia Ca2þ and glutaraldehyde can be tailored by decorating the microsphere surface withbiological active molecules useful for targeting, making a potential tool to improve Cip oraladministration for infection diseases.