Formulation, Optimization and Evaluation of Nano Based Novel Ophthalmic Drug Delivery System for Glaucoma

Abstract

Drugs delivered topically using traditional administration methods have a low bioavailability. Therefore, the goal of the current study was to create and refine the in-situ gel of carteolol-loaded chitosan nanoparticles (CHNPs), which were made using the ionotropic gelation method. Using formulation variables such as CH (A), STPP concentration (B), and stirring speed (C), the formulation was optimised by the application of box-Behnken design. Their impacts on the independent variables, such as entrapment efficiency (Y2) and particle size (Y1), were assessed. Additionally, the physicochemical properties, in-vitro drug release, ex-vivo permeability, bioadhesive studies, corneal hydration, histopathology, and HET-CAM of Carteolol-CHNPs were assessed. Nanoparticles loaded in-situ gel were also analysed. The tiny particle size (153 ± 6 nm) of the optimised formulation (Carteolol-CHNP opt) is ideal for ocular administration. In addition, it had a spherical form, a high encapsulation rate (71.06%), and a positive zeta potential (+36.3 mV). A sustained drug release profile (83.99 ± 3.6% over 12 hours) was found in the drug release research. Hydration, histology, and the HET-CAM test all reveal that the excised goat cornea in the CHNPs loaded in-situ gel did not show any signs of injury. The outcomes shown that glaucoma patients with a longer precorneal residency length and better patient compliance could benefit from the use of Carteolol-CHNPs loaded in-situ gel by reducing the dosage frequency.