Abstract
Levofloxacin (LVF) is an antibacterial drug approved for the treatment of ocular infections. However, due to the low ocular bioavailability, high doses are needed, causing bacterial resistance. Polymeric nanospheres (NPs) loading antibiotic drugs represent the most promising approach to eradicate ocular infections and to treat pathogen resistance. In this study, we have developed chitosan NPs based on sulfobutyl-ether-β-cyclodextrin (CH/SBE-β-CD NPs) for ocular delivery of LVF. CH/SBE-β-CD NPs loading LVF were characterized in terms of encapsulation parameters, morphology, and sizes, in comparison to NPs produced without the macrocycle. Nuclear magnetic resonance and UV–vis spectroscopy studies demonstrated that SBE-β-CD is able to complex LVF and to influence encapsulation parameters of NPs, producing high encapsulation efficiency and LVF loading. The NPs were homogenous in size, with a hydrodynamic radius between 80 and 170 nm and positive zeta potential (ζ) values. This surface property could promote the interaction of NPs with the negatively charged ocular tissue, increasing their residence time and, consequently, LVF efficacy. In vitro, antibacterial activity against Gram-positive and Gram-negative bacteria showed a double higher activity of CH/SBE-β-CD NPs loading LVF compared to the free drug, suggesting that chitosan NPs based on SBE-β-CD could be a useful system for the treatment of ocular infections.
Highlights
Introduction published maps and institutional affilLevofloxacin (LVF) ((3S)-9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3dihydro-7H-[1,4]oxazino [2,3,4-ij]quinoline-6-carboxylic acid) is an antibacterial chemotherapy belonging to the family of third-generation tricyclic quinolones [1,2], the fluroquinolones.It is the synthetic L-isomer of the racemic ofloxacin, with an atom of fluorine in ninth position (Figure 1).LVF shows activity widely extended compared to the racemic mixture and the Risomer against positive, negative, and atypical bacteria [3]
We evaluated the stability of LVF at the pH value used for the preparation of NPs and in the medium used for in vitro release studies (PBS, pH 7.4), in the absence and presence of SBE-β-CD
No significant degradation of LVF was observed at the experimental conditions, as evidenced by HPLC analysis for the free drug and complexed with SBE-β-CD
Summary
Introduction published maps and institutional affilLevofloxacin (LVF) ((3S)-9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3dihydro-7H-[1,4]oxazino [2,3,4-ij]quinoline-6-carboxylic acid) is an antibacterial chemotherapy belonging to the family of third-generation tricyclic quinolones [1,2], the fluroquinolones.It is the synthetic L-isomer of the racemic ofloxacin, with an atom of fluorine in ninth position (Figure 1).LVF shows activity widely extended compared to the racemic mixture and the Risomer against positive, negative, and atypical bacteria (aerobic and anaerobic) [3]. Levofloxacin (LVF) ((3S)-9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3dihydro-7H-[1,4]oxazino [2,3,4-ij]quinoline-6-carboxylic acid) is an antibacterial chemotherapy belonging to the family of third-generation tricyclic quinolones [1,2], the fluroquinolones. It is the synthetic L-isomer of the racemic ofloxacin, with an atom of fluorine in ninth position (Figure 1). LVF shows activity widely extended compared to the racemic mixture and the Risomer against positive, negative, and atypical bacteria (aerobic and anaerobic) [3]. Its activity is selective against bacterial topoisomerases, saving human cells. LVF has been approved for the treatment of infections involving different organs, iations
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