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A Novel Triptolide Nano-Liposome with Mitochondrial Targeting for Treatment of Hepatocellular Carcinoma
Lili Zhou1, Yang Du2, Yating Shang1
1School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, People's Republic of China.
Background:
Modern pharmacological studies have demonstrated that although triptolide (TP) is effective against hepatocellular carcinoma, it has poor water solubility and more toxic side effects. In this study, we used triptolide (TP), a bioactive constituent in Tripterygium wilfordii Hook F, as a model drug to develop a novel nano-liposome drug delivery system for the treatment of liver tumours.
Methods:
We constructed a functionally-modified triptolide liposome (FA+TPP-TP-Lips) using the film-dispersion method and investigated its physicochemical properties, mitochondrial targeting of hepatic tumour cells, in vitro and in vivo anti-hepatic tumour activity and its mechanism.
Results:
The prepared FA+TPP-TP-Lips had a particle size of 99.28 ± 5.7 nm, a PDI of 0.20 ± 0.02, a zeta potential of 1.2 ± 0.08 mV, and an encapsulation rate of 74.37% ± 1.07%.FA+TPP-TP-Lips facilitates the cellular uptake of drug delivery systems and improves their targeted delivery to mitochondria. The results of cell efficacy showed that FA+TPP-TP-Lips significantly inhibited the growth of liver cancer cells, decreased mitochondrial membrane potential, and increased intracellular ROS, thus enhancing the highest apoptosis rate of liver cancer cells. The targeted liposomes (FA-TP-Lips, TPP-TP-Lips, and FA+TPP-TP-Lips) had some degree of inhibitory migration effect on Huh-7 cells relative to the unmodified TP-Lips. Studies on tumor-bearing mice demonstrated that FA+ TPP-TP-Lips effectively accumulated in tumor tissues and significantly inhibited the growth of subcutaneous tumors, achieving a tumor inhibition rate of 79.37%. FA+ TPP-TP-Lips demonstrated an enhanced anti-liver tumor effect and significantly mitigated the hepatotoxicity and systemic toxicity associated with TP.
Conclusion:
In summary, the results of this study can provide a feasible solution for improving the mitochondrial targeting of nano-liposomes, and lay a foundation for further developing a novel nano targeting preparation of triptolide for the treatment of hepatocellular carcinoma.
Insights
This study developed a novel nano-liposome drug delivery system using triptolide (TP) to treat liver cancer. The new system enhances targeted delivery to mitochondria, improving efficacy and reducing toxicity for hepatocellular carcinoma treatment.
Area of Science:
- Nanomedicine
- Pharmacology
- Oncology
Background:
- Triptolide (TP) shows efficacy against hepatocellular carcinoma but suffers from poor water solubility and high toxicity.
- Developing improved drug delivery systems is crucial for enhancing TP's therapeutic potential in liver cancer treatment.
Purpose of the Study:
- To develop and characterize a novel, functionally-modified triptolide liposome (FA+TPP-TP-Lips) for targeted hepatocellular carcinoma therapy.
- To evaluate the physicochemical properties, mitochondrial targeting, and anti-tumor activity of the developed nano-liposome system both in vitro and in vivo.
Main Methods:
- Liposomes encapsulating triptolide were prepared using the film-dispersion method.
- Physicochemical properties, cellular uptake, mitochondrial targeting, and in vitro/in vivo anti-tumor effects were investigated.
Main Results:
- The FA+TPP-TP-Lips exhibited optimal particle size, encapsulation efficiency, and enhanced cellular uptake and mitochondrial targeting.
- In vitro studies showed significant inhibition of liver cancer cell growth, increased apoptosis, and reduced mitochondrial potential.
- In vivo studies in tumor-bearing mice demonstrated significant tumor growth inhibition (79.37%) and reduced systemic toxicity.
Conclusions:
- The developed FA+TPP-TP-Lips represent a promising nano-liposome system for improving mitochondrial targeting and enhancing the efficacy of triptolide in hepatocellular carcinoma treatment.
- This study provides a foundation for developing novel nano-targeting triptolide preparations for liver cancer therapy.
