Title:Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity
VOLUME: 24 ISSUE: 3
Author(s):Gülsel Yurtdaş Kırımlıoğlu*, Sinan Özer, Gülay Büyükköroğlu and Yasemin Yazan
Affiliation:Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskisehir, Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskisehir, Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Anadolu University, Eskisehir, Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskisehir
Keywords:Moxifloxacin hydrochloride, nanoparticle, Eudragit® RL 100, Kollidon® SR, modified release, ocular delivery.
Abstract:
Background: Considering the low ocular bioavailability of conventional formulations
used for ocular bacterial infection treatment, there is a need to design efficient novel drug delivery
systems that may enhance 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 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 a spray-drying process. Particle size, zeta potential, entrapment efficiency,
particle morphology, thermal, FTIR, 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 the Korsmeyer-Peppas kinetic model. Following the successful incorporation of
MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was
selected for further studies because of its better characteristics like cationic zeta potential, smaller
particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERLMOX
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
ERL-MOX 2 formulation has the potential of enhancing ocular bioavailability.
