Influence of nanoprecipitation method parameters on nanoparticles loaded with gatifloxacin for ocular drug delivery

Poor ocular bioavailability of drugs (<1%) from conventional eye drops (i.e., solution, suspension, and ointments) is mainly due to the physiologic barriers of the eye. In general, ocular efficacy is closely related to ocular drug bioavailability, which may be enhanced by increasing corneal drug penetration and prolonging precorneal drug residence time. In our current work, we developed a colloidal system that is polycaprolactone (PCL) nanoparticles for Gatifloxacin ophthalmic delivery, to improve precorneal residence time and ocular penetration for enhanced drug bioavailability. In this research, we studied nanoparticles preparation procedures and the effect of process variables on its characters. Nanoparticles were prepared by nanoprecipitation technique and characterized for various properties such as particle size, polydispersity index PdI, zeta potential and Entrapment efficiency EE%. The developed nanosuspension showed a mean particle size in the range of 184 to 207nm, suitable for ophthalmic application with zeta potential range of -30 to -32 mV and Entrapment Efficiency EE% of 40%. These results demonstrated that, the developed nanosuspension was found to be applicable for sustained ocular drug delivery allowing minimizing dose repetition to reduce systemic side effects and enhance patient compliance.