3 years ago

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

Coumarin Nanoparticle in Aqueous Solution as Selective Mitochondrial-Targeting
Drug Delivery System
Ji Ha Lee, Jong Hwa Jung, Yeong Eun Baek, Ka Young Kim, Yeonweon Choi, Shim Sung Lee, Sung Ho Jung, Jeehyeon Bae, Hanyong Jin
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 triphenylphosphonium-appended coumarin probe (TPP-C) in an 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. The 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, whereas 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, the TPP-C nanoparticles selectively accumulated in mitochondria. The TPP-C nanoparticles alone exhibited noncytotoxicity toward cancer cells. However, with the encapsulation of the anticancer drug doxorubicin (DOX) into the TPP-C nanoparticles, the 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 suborganelle-targeted drug delivery systems for cancer therapy.

Publisher URL: http://dx.doi.org/10.1021/acsami.7b17711

DOI: 10.1021/acsami.7b17711

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