Comparative evaluation of nano ocular delivery systems loaded pH and thermosensitive in situ gels for Acanthamoeba keratitis treatment.

对负载 pH 和热敏原位凝胶的纳米眼部递送系统在棘阿米巴角膜炎治疗中的应用进行比较评价

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作者:Abou-Taleb Basant A, Abdelwahab Ibrahim A
Acanthamoeba keratitis is the most dangerous ocular-infection that can cause blindness. The propamidine-isethionate (PI) 0.1% eye-drops are used in the treatment, but they have low-bioavailability due to precorneal loss parameters. In-situ-gels are administered as drops into the eye and changed into gel in the cul-de-sac, which may be able to solve these issues. In this study, we demonstrate different nano-ocular delivery-systems formulations of 0.1%PI loaded in-situ-gels using the ideas of pH & temperature-stimulated in-situ-gelation. Pluronic F-127 a thermosensitive-polymer with chitosan as a pH-sensitive polymer that also enhances permeability was utilized as a gelling-agent. Several in-vitro pharmaceutical and antiprotozoal assessments on Acanthamoeba keratitis were assessed for the developed formulations. It was observed that the created PI-chitosan nanoparticles in-situ-gel formulation showed smaller particle-size, higher zeta with a higher %inhibition of amoebae after 24-h incubation compared to other formulations with continuous drug release for 24-h. The PI-CSNPs in-situ-gel formulation offers an effective substitute for traditional BROLENE eye-drops in the management of Acanthamebae, around double the effect based on % amebae inhibition, reached 92%. It can reach the clinical-stage & is appropriate for sustained-ocular-administration for the treatment of Acanthamoeba keratitis.

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