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Polysaccharides have been widely used for the development of drug delivery systems. These systems can be physicochemically modified to enhance their stabilities and control their drug release profiles. However, such modifications cannot alter their biocompatibility or toxicity. Herein, four structurally modified sodium alginate/carboxymethylcellulose blends are synthesized and loaded with prednisone, and the effects of the modifications on their hydrolytic degradation rates, biocompatibilities, toxicities, and drug release profiles are investigated. All the blends are ionically cross‐linked with Ca2+ and Fe3+. Blend 1 is not modified further, blend 2 is additionally reinforced with 8% w/w of cellulose nanocrystals, blend 3 is treated with epoxidized linseed oil to develop a hydrophobic layer, and blend 4 is chemically cross‐linked with epichlorohydrin. Blends 2 and 4 exhibit similar physicochemical characteristics, appropriate hydrolytic degradation rates and drug release patterns, as well as biocompatibility and non‐toxicity. In‐vitro studies using the osteoblasts and CAM assay demonstrate that blends 2 and 4 are also biocompatible and non‐toxic. In contrast, blend 1 exhibits the highest drug release rate, followed by blend 3. [ABSTRACT FROM AUTHOR]

Bacterial keratitis is an ocular infection that can lead to severe visual disability. Staphylococcus aureus is a major pathogen of the eye. We recently demonstrated the strong antimicrobial activity of LyeTxI-b, a synthetic peptide derived from a Lycosa erithrognatha toxin. Herein, we evaluated a topical formulation (eye drops) containing LyeTxI-b to treat resistant bacterial keratitis. Keratitis was induced with intrastromal injection of 4 × 105 cells (4 µL) in New Zealand female white rabbits. Minimum inhibitory concentration (MIC) and biofilm viability were determined. LyeTxI-b ocular toxicity was evaluated through chorioallantoic membrane and Draize tests. One drop of the formulation (LyeTxI-b 28.9 µmol/L +0.5% CMC in 0.9% NaCl) was instilled into each eye four times a day, for a week. Slit-lamp biomicroscopy analysis, corneal histopathological studies and cellular infiltrate quantification through myeloperoxidase (MPO) and N-acetylglucosaminidase (NAG) detection were performed. LyeTxI-b was very effective in the treatment of keratitis, with no signs of ocular toxicity. Planktonic bacteria MIC was 3.6 µmol/L and LyeTxI-b treatment reduced biofilm viability in 90%. LyeTxI-b eliminated bacteria and reduced inflammatory cellular activity in the eyes. Healthy and treated animals showed similar NAG and MPO levels. LyeTxI-b is a potent new drug to treat resistant bacterial keratitis, showing effective antimicrobial and anti-inflammatory activity. [ABSTRACT FROM AUTHOR]