Transferrin decorated PLGA encumbered moxifloxacin nanoparticles and in vitro cellular studies

Abstract

Purpose

Complicated intra-abdominal infection (cIAI) management involves administering antibiotics that destroy the cell wall and the genesis of bacterial lipopolysaccharide (LPS). During the infectious state, the expression of transferrin receptors upregulates on the intestinal epithelial cells, which are considered the site of infection. In the present research, transferrin decorated poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) encapsulated moxifloxacin (MOX) were developed for possible targeting of the receptors in the colon.

Significance

This study will explore more about the incorporation of transferrin as effective coating material in targeted drug delivery.

Methods

Nanoparticles were prepared using nano-emulsification and surface modification with transferrin was done by layer-by-layer methodology and evaluated by powder X-ray diffraction (PXRD), differential scanning calorimeter (DSC), FTIR, SEM, antibacterial activity, and cellular uptake studies.

Results

The formulated NPs exhibit a size of ≈170 nm, PDI ≈ 0.25, zeta potential ≈−4.0 mV, drug loading ≈ 6.8%, and entrapment efficiency of 82%. Transferrin-decorated NPs exhibit tailored release for almost 12 h and in vitro antibacterial activity for 14 h. The cellular uptake studies were done on a RAW264.7 cell line for better determination of transferrin uptake of fabricated NPs.

Conclusion

The above study circumvents around the preparation of transferrin decorated PLGA encumbered MOX NPs intended for cIAI-induced sepsis. PLGA NPs provide tailored release of MOX with primary burst and followed by sustained release. These observations confines with antibacterial activity studies. The prepared transferrin-coated NPs were stable and effectively uptaken by RAW264.7 cells. However, future studies include the preclinical investigation of these NPs in sepsis-induced murine models.

Graphical Abstract

Keywords:

• Transferrin
• moxifloxacin
• PLGA
• nanoparticles
• sepsis
• IBD

Acknowledgements

The authors acknowledge Department of Pharmaceuticals, Ministry of Chemical Fertilizers, Government of India, for providing funding and fellowships. Authors acknowledges CIF facility and SEM Facility of NIPER-R. The NIPER-R communication number for the review article is NIPER-R/Communication/408.

Disclosure statement

The authors declare no conflict of interest among themselves.

Additional information

Funding

The authors acknowledge the Department of Pharmaceuticals, Ministry of Chemical and Fertilizers, Govt. of India for supporting financially.