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Published on: July 4, 2017
Folic acid-functionalized PEGylated magnetic nanocarriers for targeted delivery of curcumin to inflamed tissues
Maria Anghelache1, Geanina Voicu1, Florentina Safciuc1
1"Medical and Pharmaceutical Bionanotechnologies" Department, Institute of Cellular Biology and Pathology "Nicolae Simionescu" of the Romanian Academy, Bucharest 050568, Romania.
Objectives:
Curcumin has potent anti-inflammatory and anticancer effects, but its clinical use is limited by poor bioavailability. Here, we developed folic acid-functionalized PEGylated magnetite nanoparticles (Fe₃O₄-PEG-FA-Curc) to improve targeted curcumin delivery in inflammatory and cancer conditions.
Methods:
The biodistribution, targeting efficiency, and safety of Fe₃O₄-PEG-FA-Curc nanoparticles were evaluated in LPS-treated mice, while their anticancer effects were assessed in MCF-7 and A549 cells through apoptosis, cell cycle, and DNA fragmentation analyses.
Key Findings:
In vivo biodistribution of curcumin and Prussian blue staining demonstrated enhanced accumulation of FA-targeted nanoparticles in inflamed lungs of LPS-treated mice versus non-targeted nanoparticles (~2.6-fold and ~ 1.5-fold increases, respectively), correlating with elevated folate receptor β (folate receptor [FR]-β; FOLR2) expression (~2.8-fold) in lung homogenates. This targeted localization was associated with improved plasma retention and hemocompatibility, confirmed by in vitro and in vivo safety assessments. In vitro, FA-targeted curcumin nanoparticles induced apoptosis in FR-positive MCF-7 cells by increasing Bax (~2-fold), decreasing Bcl-2 (~2-fold), promoting G0/G1 arrest, and enhancing DNA fragmentation (~1.6-fold), with minimal effects in FR-negative A549 cells.
Conclusions:
FA-decorated PEGylated magnetite nanoparticles enable selective, biocompatible delivery of hydrophobic compounds like curcumin to FR-overexpressing tumors and inflamed tissues. This platform shows strong potential for precision nanotherapy in inflammatory and cancer diseases.
