Surface Coated Lipidic Nanoparticles for Ophthalmic Drug Delivery

Abstract

Topical ophthalmic drug delivery has two major drawbacks: Poor permeability and poor residence time in the eye. To address these issues, a formulation containing novel surface coated lipidic nanoparticles were devised. The NLC of Voriconazole were prepared by high-speed homogenization method using Stearic acid as a solid lipid and newlineCapmul MCM as liquid lipid and Poloxamer 188 as surfactant. The amount of solid lipid, solid lipid to total lipid ratio and surfactant concentration were varied using Central Composite design to obtain the optimized NLC with respect to particle size, PDI and % Entrapment efficiency as dependent variable. The optimised Voriconazole containing NLC was found to have particle size in nano-range with narrow particle size distribution and good %entrapment efficiency. NLC were coated by mucoadhesive chitosan newlinehydrochloride solution. The prepared formulation was characterized for various newlinepharmaceutical parameters like particle size, % EE, PDI, zeta potential, in vitro drug newlinerelease behaviour, morphology, ex vivo permeation, mucin interaction, in vivo ocular newlineirritation, and stability. Voriconazole containing surface coated nanostructured lipid carriers were found to be 114.16±7.919 nm in size with PDI of 0.125±0.014 and newline%Entrapment efficiency of 77.94±1.929 % with positive zeta potential of + 16.866±1.36 newlinemV. Formulation showed sustained release profile, spherical morphology and proved to newlinebe non-irritant with stability of 6 months. Brinzolamide, indicated for treatment of elevated intraocular pressure, has poor newlineaqueous solubility and permeability. A formulation of Brinzolamide entrapped newlinemucoadhesive lipidic nanoparticles and the process for its preparation have been newlinedisclosed in this study. First the lipidic nanoparticles of Brinzolamide were prepared by high-speed homogenization method using Glyceryl monostearate and Oleic acid as solidlipid and liquid-lipid respectively, newlinewhile Poloxamer 188 as a surfactant.