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Published on: July 20, 2019
Inhibition of Cancer Angiogenesis Using Triptolide Nanoparticles
Abstract:
Tumor-associated angiogenesis is triggered by multiple angiogenic factors. Vascular endothelial growth factor blockers are currently a major mechanism of angiogenesis inhibition; however, either insensitivity due to the targeting of single angiogenic factors or serious side effects due to non-specific exposure ultimately leads to the failure of treatment. The herb-derived compound triptolide (TP) can inhibit tumor growth through multiple mechanisms. However, its hydrophobicity and side effects have hindered its translation to the clinic. Here, we have prepared TP-polymeric micelles (TP-PMs) using methoxy poly(ethylene glycol)-block-poly(ε-caprolactone). The drug loading efficiency and encapsulation efficiency can reach 7.2 ± 0.10% and 99.1 ± 1.05%, respectively. The TP-PM solution consisted of monodispersed particles (PDI = 0.100 ± 0.023), which were 53.1 ± 1.2 nm in size. In vitro release profiles indicated that the TP-PM solution exhibited better sustained-release action when compared with free TP solution. Pharmacokinetic and tumor tissue distribution studies showed that TP-PMs facilitated TP accumulation in tumor tissues. The tumor inhibition rate upon treatment with TP-PMs was higher than 50%, and the survival time of B16-F10 melanoma bearing mice was efficiently prolonged after TP-PM administration. In addition, serum VEGF levels and tumor incidence of the TP-PM-treated group were both significantly reduced, and histological analyses revealed that the tumor vessel diameter and density in the TP-PM-treated group were much smaller than those observed in the control groups. These results indicated that TP-PMs serve as a potential angiogenesis inhibitor.
Insights
This study developed triptolide-polymeric micelles (TP-PMs) to overcome the limitations of triptolide (TP) for cancer treatment. TP-PMs effectively inhibited tumor growth and angiogenesis, showing promise as an improved therapeutic strategy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Tumor angiogenesis is crucial for cancer growth, but current therapies like vascular endothelial growth factor blockers have limitations.
- Triptolide (TP) exhibits anti-tumor properties but faces challenges due to hydrophobicity and side effects.
- Developing effective drug delivery systems is essential for improving TP's therapeutic potential.
Purpose of the Study:
- To develop and characterize triptolide-polymeric micelles (TP-PMs) for enhanced anti-angiogenesis therapy.
- To evaluate the efficacy of TP-PMs in vitro and in vivo, focusing on tumor growth inhibition and angiogenesis.
- To assess the pharmacokinetic and biodistribution profile of TP-PMs for improved tumor targeting.
Main Methods:
- TP-PMs were formulated using methoxy poly(ethylene glycol)-block-poly(ε-caprolactone).
- Particle size, drug loading, encapsulation efficiency, and in vitro release were analyzed.
- In vivo studies involved pharmacokinetic analysis, tumor tissue distribution, tumor inhibition rate, survival analysis, and histological examination of tumor vasculature.
Main Results:
- TP-PMs demonstrated high drug loading (7.2%) and encapsulation efficiency (99.1%) with optimal particle size (53.1 nm).
- TP-PMs exhibited sustained drug release and enhanced accumulation in tumor tissues compared to free TP.
- TP-PM treatment significantly inhibited tumor growth, reduced serum VEGF levels, decreased tumor incidence, and diminished tumor vessel density, prolonging survival in mice.
Conclusions:
- TP-polymeric micelles represent a promising nano-delivery system for triptolide.
- TP-PMs effectively inhibit tumor-associated angiogenesis and enhance anti-tumor efficacy.
- This formulation offers a potential strategy to overcome the clinical limitations of triptolide for cancer therapy.
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