Levofloxacin: formulation and in-vitro evaluation of alginate and chitosan nanospheres

Abstract

Background and objectives Levofloxacin, the active l-isomer of ofloxacin, is a widely used fluoroquinolone, with activity against bacteria that causes respiratory, skin, and genitourinary tract infections, (-)-(S)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido benzoxazine-6-carboxylic acid hemihydrates. It is a new quinolone antimicrobial agent that exhibits broad-spectrum in-vitro bactericidal activities against gram-positive and gram-negative aerobes. The aim of this study was to formulate sodium alginate nanospheres containing levofloxacin and evaluate its physiochemical properties, exploring alternative routes of administration, such as nanoparticle to develop a targeted drug delivery system and to act locally on the organ of infection with enriched therapeutic efficacy. Materials and methods Sodium alginate and calcium chloride solutions were prepared. A constant volume (20 μl) of levofloxacin solution was incorporated into the sodium alginate solution, and then the same method was followed for the preparation of hybrid chitosan-alginate nanoparticles. In-vitro release study was carried out by dialysis membrane for 7 h in the physiological fluid (pH 7.4 phosphate buffer solution). Morphology and structure characterization of nanoparticles were investigated by field emission scanning electron microscope and Fourier transform infrared spectra, zeta potential, X-ray diffraction, particle size analysis, respectively. Results and conclusion This paper reports the possibility to entrap lipophilic levofloxacin within chitosan/alginate (CS/ALG) nanoparticles using a very simple ionotropic pregelation technique; strong electrostatic interactions exist in the nanoparticles. The nanoparticles with a diameter of 25-55 nm were obtained at the optimal mass range of sodium alginate: calcium chloride:chitosan in the meta acid environment. The delivery behavior of levofloxacin from nanoparticles was studied. Levofloxacin released from chitosan-alginate nanoparticles was 71% at pH 7.4 within 7 h. The release profile was characterized by an initial burst effect in phosphate buffer solution, followed by a continuous and controlled release phase. The drug release mechanism from polymer also offers an interesting potential for the delivery of lipophilic compound.