Folate-conjugated albumin nanoparticles for rheumatoid arthritis-targeted delivery of etoricoxib

Abstract

Objective: The present study discusses folic acid-etoricoxib-bovine serum albumin nanoparticles (F-ETX-NPs) using folic acid as an over expressed folate receptor ligand for activated macrophages in targeting of rheumatoid arthritis.

Materials and methods: For this purpose etoricoxib-loaded BSA nanoparticles (ETX-NPs) were prepared by desolvation method and activated folic acid conjugation with free amine group of BSA was confirmed by FTIR study and zeta potential measurements.

Results: The F-ETX-NPs showed spherical in shape with 215.8 ± 3.2 nm average size + 7.8 mV zeta potential, 72 ± 1.3% etoricoxib entrapment efficiency and showed 93.1 ± 2.2% cumulative etoricoxib release upto 72 h. The etoricoxib concentration from F-ETX-NPs was found to be 9.67 ± 0.34 µg/g in inflamed joint after 24 h administration revealed remarkably targeting potential to the activated macrophages cells and keep at a high level during the experiment.

Discussion and conclusion: These results suggest that F-ETX-NPs are potentially vector for activated macrophages cells targeting of rheumatoid arthritis.

• Activated macrophages targeting
• etoricoxib
• folate conjugation
• inflammation screening
• rheumatoid arthritis

Acknowledgements

The authors thank to AIIMS, New Delhi for providing the necessary facilities for conducting TEM and SEM of samples, NIPER Chandigarh for particle size and zeta potential analysis, FTIR from Chemistry Department of Dr H. S. Gour University and CDRI Lucknow. They thank Institutional Animal Ethical Committee, ADINA Institute of Pharmaceutical Sciences, Sagar (MP), India for permission of in vivo studies.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article. Upasana Bilthariya thanks the All India Council for Technical Education (New Delhi, India) for providing financial assistance.