Related Experiment Video
Updated: Aug 9, 2025
Using In Vitro Live-cell Imaging to Explore Chemotherapeutics Delivered by Lipid-based Nanoparticles
Published on: November 1, 2017
Nanoemulsion Composed of α-Tocopherol Succinate and Dequalinium Shows Mitochondria-Targeting and Anticancer Effects
Le Thi Thuy1, Seulgi Lee2, Viet Dongquoc3
1Department of Biochemistry, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, Republic of Korea.
Abstract:
Targeted drugs have been used to treat mitochondrial dysfunction-related diseases, including metabolic disorders and cancer; however, targeting and penetrating intracellular organelles remains a challenge. Dominant targeting approaches for therapeutic delivery are detailed in many nanoemulsion studies and show the tremendous potential of targeted delivery to inhibit cancer cell growth. Dequalinium (DQA) and α-tocopherol succinate (α-TOS) are good agents for targeting mitochondria. In this study, we aimed to develop a mitochondria-targeting emulsion, using DQA and α-TOS (DTOS), for cancer treatment. DTOS emulsions of 150-170 nm in diameter were formulated using homogenization. DQA and α-TOS were used as bifunctional agents (surfactants) to stabilize the nanoemulsion and anticancer drugs. Various molar ratios of DQA and α-TOS were tested to determine the optimal condition, and DTOS 5-5 was selected for further study. The DTOS emulsion showed improved stability, as evidenced by its ability to remain stable for three years at room temperature. This stability, combined with its effective targeting of mitochondria, led to inhibition of 71.5% of HeLa cells after 24 h. The DTOS emulsion effectively inhibited spheroid growth in the 3D model, as well as prevented the growth of HeLa cells grafted onto zebrafish larvae. These results highlight the DTOS emulsion's promising potential for mitochondria-targeting and cancer treatment.
Insights
Researchers developed a novel nanoemulsion using Dequalinium (DQA) and α-tocopherol succinate (α-TOS) for targeted cancer therapy. This DTOS emulsion effectively targets mitochondria, inhibiting cancer cell growth in vitro and in vivo.
Area of Science:
- Biotechnology
- Nanomedicine
- Cancer Research
Background:
- Targeted drug delivery to intracellular organelles like mitochondria remains a significant challenge for treating diseases such as cancer.
- Nanoemulsions show promise for targeted therapeutic delivery, particularly in inhibiting cancer cell proliferation.
- Dequalinium (DQA) and α-tocopherol succinate (α-TOS) are known agents effective in targeting mitochondria.
Purpose of the Study:
- To develop a novel mitochondria-targeting nanoemulsion (DTOS) for enhanced cancer treatment.
- To utilize DQA and α-TOS as bifunctional agents for nanoemulsion stabilization and therapeutic delivery.
- To evaluate the efficacy of the DTOS emulsion in preclinical cancer models.
Main Methods:
- Formulation of DTOS nanoemulsions (150-170 nm) via homogenization.
- Optimization of DQA and α-TOS molar ratios to achieve stable and effective nanoemulsions (DTOS 5-5 selected).
- Assessment of nanoemulsion stability, mitochondrial targeting, and anticancer efficacy in HeLa cells, 3D spheroid models, and zebrafish larvae.
Main Results:
- The DTOS emulsion demonstrated remarkable stability, remaining stable for three years at room temperature.
- Significant inhibition of HeLa cells (71.5%) was observed within 24 hours post-treatment.
- The DTOS emulsion effectively suppressed tumor growth in 3D spheroid models and xenografted zebrafish larvae.
Conclusions:
- The developed DTOS nanoemulsion offers a stable and effective platform for mitochondria-targeted cancer therapy.
- This approach shows significant potential for inhibiting cancer cell growth and progression.
- DTOS nanoemulsions represent a promising strategy for future cancer treatment development.
