Nano-emulsomes for back of the eye delivery of Ganciclovir: formulation optimization, characterization & in vitro/in vivo evaluation

In this work, novel carriers- nanoemulsomes (NE) of ganciclovir (GCV) and a fluorescent marker sodium fluorescein (SF) were developed and evaluated for posterior ocular delivery via topical route. GCV loaded emulsomes (GCV NE) were optimized by a factorial design and various characterization parameters were performed on the optimized batch. The optimized batch had particle size of 131.04 +/- 1.87 nm, % entrapment efficiency of 36.42 +/- 3.09% and its TEM image showed discrete spherical structures below 200 nm. Ocular irritation potential of excipients and formulation were evaluated by cell line based in vitro tests on SIRC cell line, results confirmed the safety of excipients for ocular use. Precorneal retention and pharmacokinetic studies of GCV NE were performed in rabbit eyes which showed significant retention of GCV NE in the cul-de-sac. The ocular distribution study of SF-loaded nanoemulsomes (SF NE) were performed in mice eyes by confocal microscopy, images showed fluorescence in the various internal layers of retina, suggesting efficacy of emulsomes in delivering agents to the back of eye via topical administration.

Automated summary

Novel carriers, nanoemulsomes (NE), of ganciclovir (GCV) and a fluorescent marker, sodium fluorescein (SF), were developed and evaluated for posterior ocular delivery via topical route. The optimized GCV NE had a particle size of 131.04 +/- 1.87 nm, % entrapment efficiency of 36.42 +/- 3.09%, and showed discrete spherical structures below 200 nm. Safety of excipients for ocular use was confirmed through in vitro tests on SIRC cell line. Confocal microscopy images of SF-loaded nanoemulsomes (SF NE) showed fluorescence in the various internal layers of retina, indicating the efficacy of emulsomes in delivering agents to the back of the eye via topical administration.