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Solubilized chlorin e6-layered double hydroxide complex for anticancer photodynamic therapy.

Young-Um Jo1, HyunJune Sim1,2, Chung-Sung Lee3

  • 1Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Gyeonggi-do, Bucheon-si, 14662, Republic of Korea.

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Summary

Mono-layered double hydroxides (MLHs) effectively solubilize hydrophobic photosensitizers for anticancer photodynamic therapy (PDT). This approach enhances drug delivery and significantly improves tumor suppression in vivo.

Keywords:
Anticancer photodynamic therapyLayered double hydroxideMono-layered double hydroxidePhotosensitizerSolubilization

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Area of Science:

  • Materials Science
  • Nanotechnology
  • Biomedical Engineering

Background:

  • Layered double hydroxides (LDHs) are 2D materials with positive surface charges, exfoliatable into single-layered MLHs with increased surface area.
  • Hydrophobic photosensitizers often lack aqueous solubility, limiting their application in therapies like photodynamic therapy (PDT).
  • MLHs offer a promising platform for drug delivery due to their unique structure and charge properties.

Purpose of the Study:

  • To develop a simple method for solubilizing hydrophobic photosensitizers using MLHs.
  • To investigate the potential of MLH-photosensitizer complexes for anticancer photodynamic therapy (PDT).
  • To evaluate the efficacy of this approach in vitro and in vivo.

Main Methods:

  • Negatively charged hydrophobic photosensitizer chlorin e6 (Ce6) was loaded onto positively charged MLHs via electrostatic interactions.
  • MLH/Ce6 complexes underwent physico-chemical characterization, pH-sensitive release studies, in vitro photocytotoxicity assays, and in vivo tumor ablation experiments.
  • Encapsulation efficiency of Ce6 was compared between MLH and LDH.

Main Results:

  • Solubilized Ce6 retained fluorescence and singlet oxygen generation in aqueous solutions without chemical modification.
  • MLH encapsulation significantly increased Ce6 loading efficiency to 21.2% compared to 0.6% for LDH.
  • In vivo studies showed MLH/Ce6 achieved a 3.4-fold greater tumor-suppressing effect than Ce6 alone.

Conclusions:

  • A straightforward method was established to solubilize Ce6 using MLHs without chemical modification.
  • The developed MLH/Ce6 complexes demonstrate significant potential for effective anticancer PDT applications.