Abstract
Topical ocular delivery of therapeutics are always a challenging arena in order to achieve high ocular bioavailability with safe administration. Ideal ocular delivery of drug required 4 P's that is Patient compliance, Prolong retention, Penetration to cornea and Prolong release of drug. In an attempt to achieve desired characteristics for ocular delivery, Ketorolac loaded PLGA nanoparticles were fabricated by double emulsification solvent evaporation method and optimized by employing response surface methodology (RSM) followed by statistical analysis. Results obtained by RSM were further validated for fitness in model by different checkpoint formulations. Vitamin E TPGS was selected as emulsifier, which acquires high emulsifying capability and high permeability character. Zeta-size study revealed that optimized formulation has mean particle size 142.8 ± 11.7 nm, which was in agreement of TEM study and zeta potential was found −24.2 ± 1.2 mV. Encapsulation efficiency was achieved 63.5 ± 8.4%. Release profile was established by different mathematical modelling. It was observed that optimized formulation showed sustained release and followed by Korsmeyer-Peppas model. Corneal transport study showed enhanced drug permeation as compared to drug solution. HET-CAM test and histopathology studies revealed that optimized PLGA NPs was non-irritant and safe for ocular application.
[Display omitted]
•Ketorolac loaded PLGA nanoparticles were optimized in terms of ocular constraints by mathematical modelling.•Vitamin E TPGS was employed as emulsifier to improve the encapsulation of hydrophilic drug (Ketorolac Tromethamine).•Enhanced transcorneal permeation was achieved as compare to drug solution.•HET-CAM and Histopathology studies were carried out to determine the safety profile of developed KT-PLGA NPs.