Comparative studies for ciprofloxacin hydrochloride pre-formed gels and thermally triggered (in situ) gels: in vitro and in vivo appraisal using a bacterial keratitis model in rabbits. (June 2015)

• Record Type: Journal Article
• Authors: Abdelkader, Hamdy; Mansour, Heba F.
• Is Part Of: Pharmaceutical development and technology. Volume 20:Number 4(2015)
• Page Start: 410
• Page End: 416
• Publication Date: 2015-06
• Subjects: Drug delivery systems -- Periodicals; Pharmaceutical technology -- Periodicals; Drugs -- Administration -- Research -- Periodicals; Drug Delivery Systems -- Periodicals; Pharmaceutical Preparations -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615
• DOI: 10.3109/10837450.2013.871034
• Languages: English
• ISSNs: 1083-7450

Abstract

<abstract> <title>Abstract</title> <p>This article reports on comparative <italic>in vitro</italic> characterization and <italic>in vivo</italic> evaluation of pre-formed cellulose-based gels, methylcellulose (MC) and carboxymethylcellulose sodium (CMC) and <italic>in situ</italic> gel-forming Pluronic F127 (PL) for ocular delivery of ciprofloxacin hydrochloride (Cipro) by using a bacterial keratitis model and histological corneal examination. Drug–polymer interactions were studied employing thermal analysis. Further, different concentrations (1–3% w/w or 10–30% w/w) of gels depending on the nature of the polymer used were prepared, characterized for clarity, pH, rheology and <italic>in vitro</italic> release. Selected gel formulations were evaluated for ocular delivery to <italic>Staphylococcus aureus</italic>-infected rabbit corneas; and ocular toxicity through histological examination of the cornea. The results demonstrated no Cipro-polymers physicochemical interactions and pseudoplastic flow for all gels used at 35 °C. Both polymer concentrations and drug solubility in the gels are dominantly the rate-determining factors for <italic>in vitro</italic> drug release. The corneal healing rate for all gel-based formulations was significantly faster (<italic>p</italic> < 0.05) than that for Cipro solution-treated rabbits. PL-based gel induced significant swelling/edema of the corneal stroma, compared with MC- and CMC-based gels. In conclusion, cellulose-based polymers have superior ocular tolerability/dramatically less irritant; and superior efficacy with more convenient administration compared with PL and Cipro solution, respectively.</p> </abstract>