Preparation of dried nanoemulsion formulation by electrospinning

Dry eye disease is a multifactorial condition characterized by a loss of homeostasis of the tear film. Among the various treatment approaches, the application of ophthalmic oil-in-water nanoemulsions with incorporated anti-inflammatory drugs represents one of the most advanced approaches. However, the liquid nature of nanoemulsions limits their retention time at the ocular surface. Transforming the nanoemulsions into a dry form that would disperse rapidly in the tear fluid would improve the retention of the drug at the ocular surface. The aim of this study was to investigate electrospinning as a method for the preparation of a solid eye preparation based on nanoemulsion loaded with the anti-inflammatory drug loteprednol etabonate. Four nanoemulsions differing in oil-to-surfactant ratios were incorporated in hydrophilic nanofibers based on polyethylene oxide, poloxamer 188, and Soluplus®. The dried nanoemulsions in the form of nanofibers dispersed readily on contact with aqueous medium, resulting in a dispersion of nanometre-sized droplets with average size comparable to the average droplet size of the initial nanoemulsions. A rheological study revealed the predominant elastic behavior of the dispersed nanofibers, which indicates the formation of a weak gel after the dispersion of the dried nanoemulsion in tear fluid at the ocular surface. The biocompatibility of the dried nanoemulsions in the form of nanofibers after a single and multiple-dose application was confirmed using the 3D HCE-T model of the stratified epithelium of the human cornea, suggesting that this innovative solid eye preparation could represent a new approach to the treatment of dry eye disease.