Background: Abstract: The objective of the present work was to prepare and optimize the
loteprednoletabonate (LE) loaded poly (D,L-lactide co-glycolide) (PLGA) polymer based nanoparticle
carrier. The review on recent patents (US9006241, US20130224302A1, US2012/0028947A1) assisted
in the selection of drug and polymer for designing nanoparticles for ocular delivery applications.
Methods: The nanoparticles were prepared by solvent evaporation followed by high speed homogenization.
Biodegradable polymer PLGA (50:50) grade was utilized to develop various formulations with
different drug:polymer ratio. A Box-Behnken design with 33 factorial design was selected for the present
study and 17 runs were carried out in totality. The influence of various process variables (viz.,
polymer concentration, homogenization speed and sonication time) on the characteristics of nanoparticles
including the in vitro drug release profile were studied.
Results: The nanoparticulate formulations were evaluated for mean spherical diameter, polydispersity
index (PDI), zeta potential, surface morphology, drug entrapment and in-vitro drug release profile. The
entrapment efficiency, drug loading and mean particle size were found to be 96.31±1.68 %, 35.46±0.35
% and 167.6±2.1 nm respectively.
Conclusion: The investigated process and formulation variables were found to have significant effect
on the particle size, drug loading (DL), entrapment efficiency (EE), and in vitro drug release profile. A
biphasic in vitro drug release profile was apparent from the optimized nanoparticles (NPs) for 24 hours.