Evaluation of gatifloxacin pluronic micelles and development of its formulation for ocular delivery.

The purpose of the present study was to enhance the solubility of gatifloxacin by developing self-assembling pluronic micelles of gatifloxacin for ocular delivery, to overcome the problem of poor bioavailability and therefore lesser therapeutic response exhibited by conventional ophthalmic solutions of the drug. Gatifloxacin was loaded in micelles by solid dispersion method using Pluronic F127 and evaluated for particle size, drug loading, loading efficiency, in vitro transcorneal permeation study, in vitro drug release, solubility studies, microbiological studies, ex vivo mucoadhesive strength, and ocular safety studies. The drug loading and drug loading efficiency studies revealed that gatifloxacin/Pluronic F127 ratio of 0.25/2.52 g offered good drug loading (9.96 %), high loading efficiency (90 %), and acceptable particle size of 176 nm (polydispersity index 0.345). Hen's egg test chorioallantoic membrane (HET-CAM) assay with 0 score in 8 h and ocular safety test with score of 2 indicate the nonirritant property of the developed pluronic micelles. In vitro transcorneal permeation studies through excised goat cornea indicated increase in ocular availability with no corneal damage. In vitro drug release data of optimized formulation provided sustained release over a period of 8 h. Optimized formulation was found to possess acceptable transcorneal permeation and antimicrobial efficacy when compared to marketed eye drops. The solubility studies of gatifloxacin from these lyophilized pluronic micelles revealed 18.67-fold increase in comparison to gatifloxacin suspension in water. The pluronic micelles could enhance ocular bioavailability of gatifloxacin, prolong its residence time in the eyes, and may lead to reduced instillation frequency, thereby resulting in better patient compliance.