ConA-Coated Liposomes as a System to Delivery β-Lapachone to Breast Cancer Cells

Abstract

Background: Target treatment using site-specific nanosystems is a hot topic for treating several diseases, especially cancer. Objective: The study was set out to develop site-specific liposomes using ConcanavalinA (ConA) to target β-lapachone(β-lap) to human breast cancer cells. Methods: Liposomes were prepared and characterized according to diameter size, zeta potential, ConA conjugation(%), and β-lap encapsulation efficiency (%). Isothermal Titration Calorimetry evaluated the binding energy between the biomolecules, which compose the liposomes. ConA avidity was assessed before and after conjugation. Cytotoxicity was evaluated, and fluorescence microscopy was performed to investigate the influence of ConA influenced on MCF-7 uptake. Results: Uncoated and ConA-coated liposomes presented size, and zeta potential values from 97.46 ± 2.01 to 152.23 ± 2.73nm, and -6.83 ± 0.28 to -17.23 ±0.64mV, respectively. Both ConA conjugation and β-lap encapsulation efficiency were approximately 100%. The favorable and spontaneous process confirmed the binding between ConA and the lipid. Hemagglutination assay confirmed ConA avidity once Lipo-ConA and Lipo-PEG-ConA were able to hemagglutinate the red blood cells at 128-1 and 256-1, respectively. Lipo-ConA was not cytotoxic, and the site-specific liposomes presented the highest toxicity. ConA-coated liposomes were more internalized by MCF7 than uncoated liposomes. Conclusion: Therefore, the presence of ConA on the surface of liposomes influenced MCF7 uptake, suggesting that it could be used as a promising site-specific system to target β-lap to cancer cells.