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Multicomponent folate-targeted magnetoliposomes: design, characterization, and cellular uptake.

Geoffrey D Bothun1, Alline Lelis, Yanjing Chen

  • 1Department of Chemical Engineering, University of Rhode Island, Kingston, Rhode Island 02881, USA. bothun@egr.uri.edu

Nanomedicine : Nanotechnology, Biology, and Medicine
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Folate-targeted magnetoliposomes effectively deliver doxorubicin to cancer cells expressing folate receptors. Radiofrequency heating enhances drug release, showing promise for targeted cancer therapy.

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Area of Science:

  • Nanotechnology
  • Materials Science
  • Biomedical Engineering

Background:

  • Development of novel drug delivery systems is crucial for targeted cancer therapy.
  • Magnetoliposomes offer potential for controlled drug release and imaging.
  • Folate receptor targeting enhances specificity for cancer cells.

Purpose of the Study:

  • To design and characterize folate-targeted cationic magnetoliposomes (FTMLs) coencapsulating doxorubicin (DOX) and superparamagnetic iron oxide (SPIO) nanoparticles.
  • To investigate the triggered release of DOX from FTMLs using radiofrequency (RF) heating.
  • To evaluate the cellular uptake of FTMLs by cancer cells with varying folate receptor (FR) expression.

Main Methods:

  • Preparation and characterization of FTMLs using cryogenic transmission electron microscopy (TEM).
  • Assessment of DOX release kinetics under RF-induced heating of SPIO nanoparticles.
  • In vitro cellular uptake studies using HeLa (high FR) and ZR-75-1 (low FR) cancer cell lines.

Main Results:

  • FTMLs successfully encapsulated DOX and SPIO NPs with high efficiency (89%) and appropriate size (174 ± 53 nm).
  • RF heating of SPIO NPs within FTMLs induced a 3-fold increase in DOX release over 2 hours.
  • Significant FTML binding and cellular uptake were observed in high FR-expressing HeLa cells, but not in low FR-expressing ZR-75-1 cells.

Conclusions:

  • FTMLs are a promising platform for targeted delivery of doxorubicin to folate receptor-positive cancer cells.
  • RF-triggered drug release offers a mechanism for spatiotemporal control of chemotherapy.
  • The folate-targeting strategy ensures selective uptake by cancer cells, minimizing off-target effects.