Development and Characterization of Folic Acid-Conjugated Amodiaquine-Loaded Nanoparticles-Efficacy in Cancer Treatment

Vineela Parvathaneni; Snehal K Shukla; Vivek Gupta

doi:10.3390/pharmaceutics15031001

Development and Characterization of Folic Acid-Conjugated Amodiaquine-Loaded Nanoparticles-Efficacy in Cancer Treatment

Pharmaceutics. 2023 Mar 20;15(3):1001. doi: 10.3390/pharmaceutics15031001.

Authors

Vineela Parvathaneni¹, Snehal K Shukla¹, Vivek Gupta¹

Affiliation

¹ Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA.

Abstract

The objective of this study was to construct amodiaquine-loaded, folic acid-conjugated polymeric nanoparticles (FA-AQ NPs) to treat cancer that could be scaled to commercial production. In this study, folic acid (FA) was conjugated with a PLGA polymer followed by the formulation of drug-loaded NPs. The results of the conjugation efficiency confirmed the conjugation of FA with PLGA. The developed folic acid-conjugated nanoparticles demonstrated uniform particle size distributions and had visible spherical shapes under transmission electron microscopy. The cellular uptake results suggested that FA modification could enhance the cellular internalization of nanoparticulate systems in non-small cell lung cancer, cervical, and breast cancer cell types. Furthermore, cytotoxicity studies showed the superior efficacy of FA-AQ NPs in different cancer cells such as MDAMB-231 and HeLA. FA-AQ NPs had better anti-tumor abilities demonstrated via 3D spheroid cell culture studies. Therefore, FA-AQ NPs could be a promising drug delivery system for cancer therapy.

Keywords: 3D spheroid studies; amodiaquine; cancer; folic acid; nano-repurposing; nanoparticles; repurposing; targeted delivery.

Grants and funding

This study was supported by research funds to V.G. from the College of Pharmacy and Health Sciences (CPHS), St. John’s University. V.P. was supported by the Doctoral Fellowship offered by the College of Pharmacy and Health Sciences at St. John’s University. S.K.S. was supported by research assistantship provided by an NIH Academic Research Enhancement Award (R15), 1R15HL138606-01A1 awarded to V.G.