Galactosylated iron oxide nanoparticles for enhancing oral bioavailability of ceftriaxone

Abstract

The current study focuses on the development, characterization, biocompatibility investigation and oral bioavailability evaluation of ceftriaxone (CFT)-loaded lactobionic acid (LBA)-functionalized iron oxide magnetic nanoparticles (MNP-LBA). Atomic force microscopy and dynamic light scattering showed that the developed CFT-loaded MNP-LBA is spherical, with a measured hydrodynamic size of 147 ± 15.9 nm and negative zeta potential values (–35 ± 0.58 mV). Fourier transformed infrared analysis revealed interactions between the nanocarrier and the drug. Nanoparticles showed high drug entrapment efficiencies of 91.5 ± 2.2%, and the drug was released gradually in vitro and shows prolonged in vitro stability using simulated gastrointestinal (GI) fluids. The formulations were found to be highly biocompatible (up to 100 µg/mL) and hemocompatible (up to 1.0 mg/mL). Using an albino rabbit model, the formulation showed a significant enhancement in drug plasma concentration up to 14.46 ± 2.5 µg/mL in comparison with its control (1.96 ± 0.58 µg/mL). Overall, the developed MNP-LBA formulation was found promising for provision of high-drug entrapment, gradual drug release and was appropriate for enhancing the oral delivery of CFT.

Keywords:

• Magnetic NPs
• mucoadhesive
• ceftriaxone
• biocompatibility
• oral bioavailability

Acknowledgements

The authors would like to thank Pakistan Science Foundation (PSF) and International Center for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, Pakistan for providing research funding and utilities.

Disclosure statement

All the authors declare no conflict of interest.

Additional information

Funding

. The financial support is from Pakistan Science Foundation for this project through project no PSF/CRP/ NSFC III/Med/S-HEJ (15).