Preparation and characterization of novel, mucoadhesive ofloxacin nanoparticles for ocular drug delivery

• Published in: Brazilian Journal of Pharmaceutical Sciences Vol. 55
• Main Authors: Taghe, Shiva, Mirzaeei, Shahla
• Format: Journal Article
• Language: English
• Published: Sao Paulo Universidade de Sao Paulo Faculdade de Ciencias 2019; Universidade de São Paulo, Faculdade de Ciências Farmacêuticas; Universidade de São Paulo
• Subjects: Antibiotics; Antimicrobial agents; Chitosan; Cornea; Corneal penetration; Efficiency; Gram-negative bacteria; Infections; Nanoparticles; Ocular drug delivery; Ofloxacin; Particle size; Permeability; PHARMACOLOGY & PHARMACY; Polymers; Prescription drugs; Sodium; Viscosity; United States > US; Germany; Nanoparticles; Chitosan; Corneal penetration; Ofloxacin; Ocular drug delivery
• ISSN: 2175-9790; 1984-8250; 2175-9790
• DOI: 10.1590/s2175-97902019000117105

The efficacy of conventional ocular formulations is limited by poor corneal retention and permeation, resulting in low ocular bioavailability. Mucoadhesive chitosan (CS)/ tripolyphosphatesodium (TPP) and chitosan (CS)/ tripolyphosphatesodium (TPP)-alginate (ALG) nanoparticles were investigated for the prolonged topical ophthalmic delivery of ofloxacin. A modified ionotropic gelation method was used to produce ofloxacin-loaded nanoreservoir systems. The ofloxacin-loaded CS/TPP and CS/TPP-ALG nanoparticles were characterized for particle size, morphology, zeta potential, encapsulation efficiency, subsequent release and corneal penetration study. The designed nanoparticles have a particle size from 113.8 nm to 509 nm and zeta potential from 16.2 mV to 40.3 mV and encapsulation efficiency values ranging from 19.7% to 33.1%. Nanoparticles revealed a release during the first hours, followed by a more gradual drug release. The ofloxacin-loading CS/TPP or CS/TPP-ALG NPs developed are pronounced penetration enhancing effect as compared to OFX solution (5-6.5 times). Thus, these nanoparticles have a strong potential for ocular drug delivery.