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

Abstract

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.