Formulation, Optimization and Characterization of Acetazolamide-Loaded Solid Lipid Nanoparticles for Glaucoma...

The goal of the present study is to optimize acetazolamide-loaded solid lipid nanoparticles (AZM-loaded SLNs) using central composite design (CCD) for prolonged ocular delivery. The emulsion solvent evaporation process was used to develop AZM-loaded SLNs. The optimal formulation parameters influencing particle size, entrapment efficiency, and percentage drug release were determined using a CCD, and the effects of these variables on the formulation were examined. Furthermore, the particle size, entrapment effectiveness, and in-vitro drug release were carried out, along with FTIR, XRD, DSC, SEM, and TEM, which were used to determine structural and physicochemical properties. The ex-vivo corneal permeability investigations were used to assess drug penetration, and in-vivo experiments in rabbit eyes were conducted to assess the impact on reducing intraocular pressure. Moreover, hemocompatibility, sterility, and eye irritation were also used to evaluate the formulation's safety features. The optimized AZM-loaded SLNs had a drug entrapment efficiency of 89.45%, a particle size of 110.3 nm, and a prolonged drug release of 87.76% in a 24 h period. The drug's effective incorporation into the lipid carrier particles was verified by FTIR, XRD, DSC, SEM, and TEM. Ex-vivo corneal permeation showed that it was significantly higher than both the pure drug and the marketed formulation. Additionally, the in-vivo studies showed a reduction in the intraocular pressure (IOP) during 24 h. A promising nanocarrier system for prolonged ocular administration and better glaucoma patient management has been represented by the developed AZM-loaded SLNs.