Self-Assembled Coumarin Nanoparticle in Aqueous Solution as Selective Mitochondrial-Targeting Drug Delivery System

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Abstract
The development of specifically targeted nanoparticles for subcellular organelles modified with a low-molecular-weight organic compound as drug nanocarriers can bring about wide applications in cancer therapy. However, their utility has been hampered by low selectivity, poor biodistribution, and limited efficiency. Herein, we report the aggregation behavior of a triphenyl phosphonium-appended coumarin probe (TPP-C) in aqueous solution and its applications as a mitochondria-targeting probe, and drug delivery carrier, which is a rare example for a low molecular-weight organic compound. TPP-C formed homogeneous nanoparticles with small diameters in water as well as in mixtures of organic solvents and water. In pure water, the homogeneous nanoparticles induced J-aggregation, while in mixed solvents, the homogeneous nanoparticles induced H-aggregation. The luminescence intensities of nanoparticles originated from the aggregation-induced emission (AIE) effect in pure water and also in mixtures of organic solvents and water. These findings indicate that the AIE effect of TPP-C was dependent on the solvent. More interestingly, TPP-C nanoparticles selectively accumulated in mitochondria. The TPP-C nanoparticles alone exhibited non-cytotoxicity toward cancer cells. However, with the encapsulation of the anticancer drug doxorubicin (DOX) into TPP-C nanoparticles, DOX was efficiently delivered to the mitochondria. These results indicated that the proposed system demonstrates promise as a platform for future clinical medication, particularly for specific sub-organelle-targeted drug delivery systems for cancer therapy.
Funding Information
  • National Research Foundation of Korea (2017R1A4A1014595)
  • Next-Generation BioGreen 21 Program (PJ01318605)

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