Background: Considering the low ocular bioavailability of conventional formulations used
for ocular bacterial infection treatment, there’s a need for designing efficient novel drug delivery
systems that may enhance of precorneal retention time and corneal permeability.
Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit®
RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its
prolonged release to be promising for effective ocular delivery.
Methods: In this study, MOX was incorporation was carried out by spray drying method aiming
ocular delivery. In vitro characteristics were evaluated in detail with different methods.
Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric
nanoparticles by spray-drying process. Particle size, zeta potential, entrapment efficiency, particle
morphology, thermal, FTIR, XRD and NMR analyses and MOX quantification using HPLC method
were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated
nanosized and spherical shape while in vitro release studies demonstrated modified release pattern
which followed Korsmeyer-Peppas kinetic model. Following successful incorporation of MOX into
the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for
further studies by the reason of its better characteristics like cationic zeta potential, smaller particle
size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERL-MOX 2
formulation remained stable for 3 months and demonstrated higher cell viability values for MOX.
Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERLMOX 2 formulation has the potential of enhancing ocular bioavailability.