Formulation and Evaluation of Bimatoprost and Sparfloxacin Nanosuspension for Ocular Use

Abstract

newline Background: Bimatoprost and Sparfloxacin are ophthalmic drugs used in the newlinetreatment of glaucoma and conjunctivitis respectively. The drugs are having poor newlinesolubility and poor bioavailability. newlineObjectives: The objective of the present study was to enhance the bioavailability of newlinethe drug by formulating it in the nanosuspension formulations. newlineMethodology: The ophthalmic nanosuspension were formulated and optimized with newlinerespect to percentage of polymer and surfactants to get optimum particle size and newlineentrapment efficiency. The nanosuspensions were characterized for particle size, newlineshape, zeta potential and entrapment efficiency. The in vitro release and ex vivo newlinepermeation of drug through formulation was checked by Franz diffusion cell. The newlinegoat corneal membrane were used for drug permeation experiment. The newlinenanosuspensions also evaluated for in vitro and in vivo ocular irritation studies, newlinecytotoxicity screening, ex vivo and in vivo microbiological studies (Sparfloxacin newlinenanosuspension), ex vivo corneal permeation study, isotonicity study, newlinePharmacokinetic study, anti- glaucoma study, (Bimatoprost Nanosuspension) and newlinesurface morphology (TEM) followed by stability study. The in vivo antimicrobial newlinestudy for Sparfloxacin and in vivo pharmacokinetic and anti-glaucoma studies were newlinecarried out in Newzeland albino rabbits. newlineResults: The particle size and entrapment efficiency of optimized formulations newlineBimatoprost and Sparfloxacin nanosuspension were found 374±8 nm and 400±10 nm newlineand 89±2 and 94±2% respectively. The both formulations nanoparticles were nearly newlinespherical in shape with zeta potential varied from -42±8 to -12±2 mV. The improved in newlinevitro and ex vivo drug permeation across the corneal membrane indicates the newlineimproved solubility of drugs. The irritation study, isotonicity study and cytotoxicity newlinestudy confirms both Sparfloxacin and Bimatoprost nanosuspension formulations are newlinenon-irritating, isotonic and safe. The optimized Sparfloxacin formulation SNF3 newlineshowed greater antimicrobial pote