The Journal of pharmacy and pharmacology · 2026
Folic acid-functionalized PEGylated magnetic nanocarriers for targeted delivery of curcumin to inflamed tissues.
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Anghelache Maria, Voicu Geanina, Safciuc Florentina, Turtoi Mihaela, Deleanu Mariana, Movileanu Codina, Ficai Denisa, Ficai Anton, Calin Manuela
Аннотация
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.
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.