Ghelardi Emilia, Tavanti Arianna, Davini Paola, Celandroni Francesco, Salvetti Sara, Parisio Eva, Boldrini Enrico, Senesi Sonia, Campa Mario
Dipartimento di Patologia Sperimentale, Biotecnologie Mediche, Infettivologia ed Epidemiologia, Università di Pisa, Via S. Zeno 37, 56127 Pisa, Italy.
Antimicrob Agents Chemother. 2004 Sep;48(9):3396-401. doi: 10.1128/AAC.48.9.3396-3401.2004.
Bacterial keratitis is a serious infectious ocular disease requiring prompt treatment to prevent frequent and severe visual disabilities. Standard treatment of bacterial keratitis includes topical administration of concentrated antibiotic solutions repeated at frequent intervals in order to reach sufficiently high drug levels in the corneal tissue to inhibit bacterial growth. However, this regimen has been associated with toxicity to the corneal epithelium and requires patient hospitalization. In the present study, a mucoadhesive polymer extracted from tamarind seeds was used for ocular delivery of 0.3% rufloxacin in the treatment of experimental Pseudomonas aeruginosa and Staphylococcus aureus keratitis in rabbits. The polysaccharide significantly increased the intra-aqueous penetration of rufloxacin in both infected and uninfected eyes. Rufloxacin delivered by the polysaccharide reduced P. aeruginosa and S. aureus in the cornea at a higher rate than that obtained by rufloxacin alone. In particular, use of the polysaccharide allowed a substantial reduction of S. aureus in the cornea to be achieved even when the time interval between drug administrations was extended. These results suggest that the tamarind seed polysaccharide prolongs the precorneal residence times of antibiotics and enhances drug accumulation in the cornea, probably by reducing the washout of topically administered drugs. The tamarind seed polysaccharide appears to be a promising candidate as a vehicle for the topical treatment of bacterial keratitis.
细菌性角膜炎是一种严重的感染性眼病,需要及时治疗以防止频繁出现严重视力残疾。细菌性角膜炎的标准治疗方法包括频繁局部应用浓缩抗生素溶液,以便在角膜组织中达到足够高的药物水平来抑制细菌生长。然而,这种治疗方案已被证明对角膜上皮有毒性,且需要患者住院治疗。在本研究中,从罗望子种子中提取的一种粘膜粘附聚合物被用于眼部递送0.3%的芦氟沙星,以治疗兔实验性铜绿假单胞菌和金黄色葡萄球菌角膜炎。该多糖显著增加了芦氟沙星在感染和未感染眼中的房水渗透。通过多糖递送的芦氟沙星比单独使用芦氟沙星能更有效地降低角膜中的铜绿假单胞菌和金黄色葡萄球菌。特别是,即使延长给药时间间隔,使用该多糖也能使角膜中的金黄色葡萄球菌大幅减少。这些结果表明,罗望子种子多糖可能通过减少局部给药药物的冲洗,延长了抗生素在角膜前的停留时间,并增强了药物在角膜中的蓄积。罗望子种子多糖似乎是细菌性角膜炎局部治疗的一种有前景的载体。