Development optimization and characterization of besifloxacin hydrochloride nanoformulations for ocular drug delivery

Abstract

The aim of present research is to design and development of solid lipid nanoparticle, nanosuspension, nanoemulsion and niosome as an in-situ gel for ocular drug delivery of Besifloxacin hydrochloride, a fourth generation fluoroquinolone antibiotic. newlineAnalytical method of Besifloxacin Hydrochloride was developed by HPLC-UV technique. Various characterization studies like FTIR, DSC, XRD were performed to check the compatibility study with drug and excipients. SLN is prepared by Hot Homogenization Process using glyceryl monostearate and polysorbate 80 along with poloxamer 188 and purified water. Nanosuspension of Besifloxacin HCl was prepared by high speed homogenization process using eudragit RS100, ethyl acetate, polysorbate 80, poloxamer 188 and purified water. Nanoemulsion of Besifloxacin HCl was prepared by high speed homogenization process using egg lechithin, soybean oil, glycerin, polysorbate 80, poloxamer 188 and purified water. Niosome of Besifloxacin HCl was prepared by coacervation phase separation method using cholesterol, span 60, ethanol and purified water. The preliminary formulation of solid lipid nanoparticle, nanosuspension, nanoemulsion and niosome were tested for zeta potential, polydispersity index, and particle size. The formulations were optimized following 32 factorial design. Particle size, polydispersity index, zeta potential and entrapment efficiency were evaluated for the confirmation of nanoformulations. The final optimized formulations of solid lipid nanoparticle, nanosuspension, nanoemulsion and niosome were mixed with optimized gelrite solution to form in-situ gel. Surface morphology of final ophthalmic formulations were confirmed with SEM and TEM studies. In-vitro releases were studies of above nanoformulations. Stability studies of final ophthalmic nanoformulations were checked for 6 months as per the ICH guidelines. Finally In-vivo studies of these solid lipid nanoparticles, nanosuspension, nanoemulsion and niosome ophthalmic formulations were carried out with eye irritancy test a