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Triphenylphosphonium-modified mitochondria-targeted paclitaxel nanocrystals for overcoming multidrug resistance

Xue Han1, Ruijuan Su1, Xiuqing Huang1

  • 1Shenyang Pharmaceutical University, Shenyang 110016, China.

Asian Journal of Pharmaceutical Sciences
|February 28, 2020
PubMed

Insights

This study developed mitochondria-targeted paclitaxel nanocrystals (PTX NCs) using TPP+-conjugated Brij 98 to combat multidrug resistance (MDR) in cancer. The targeted PTX NCs demonstrated superior efficacy against drug-resistant cancer cells and spheroids.

Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Cancer Therapy

Background:

  • Mitochondria are emerging targets for cancer treatment, particularly in multidrug-resistant (MDR) tumors.
  • Developing effective drug delivery systems is crucial for overcoming MDR.

Purpose of the Study:

  • To create a mitochondria-targeted paclitaxel (PTX) delivery system using triphenylphosphonium cation (TPP+)-conjugated Brij 98.
  • To evaluate the efficacy of TPP+-modified PTX nanocrystals (NCs) against drug-resistant cancer cells.

Main Methods:

  • Functionalization of PTX NCs with TPP+-conjugated Brij 98 for enhanced mitochondrial targeting.
  • Assessment of cytotoxicity and cellular uptake in 2D monolayer and 3D multicellular spheroids (MCs) of MCF-7 and MCF-7/ADR cells.
  • Evaluation of mitochondrial membrane potential and penetration depth in MCs.

Main Results:

  • Targeted PTX NCs exhibited significantly higher cytotoxicity against both sensitive (MCF-7) and MDR (MCF-7/ADR) cells compared to free PTX and non-targeted NCs.
  • The enhanced efficacy correlated with a reduced mitochondrial membrane potential.
  • Targeted PTX NCs demonstrated improved penetration into 3D MCs and greater growth inhibition.

Conclusions:

  • TPP+-modified PTX NCs represent a promising strategy for targeted delivery of chemotherapeutics to mitochondria.
  • This approach shows potential for overcoming multidrug resistance in cancer therapy.
  • The TPP+-conjugated Brij 98 stabilizer offers a viable method for creating mitochondria-targeted nanocarriers.
Keywords:
Brij 98MitochondriaMultidrug resistanceNanocrystalsPaclitaxelTriphenylphosphonium

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