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Updated: Dec 7, 2025

Cytotoxic Efficacy of Photodynamic Therapy in Osteosarcoma Cells In Vitro
Published on: March 18, 2014
Overcoming therapeutic failure in osteosarcoma via Apatinib-encapsulated hydrophobic poly(ester amide) nanoparticles
Xiangyu Li1, Liying Wang2, Li Wang3
1The Stem Cell and Tissue Engineering Research Center, Changzhi Medical College, Changzhi, Shanxi 046000, P. R. China. mcxms@163.com.
Abstract:
Anti-angiogenic tyrosine kinase inhibitors (TKIs) have been proved to be effective in prolonging progression-free survival in advanced osteosarcoma. However, osteosarcoma stem-like cells persist for a long time and ultimately cause disease recurrence and therapy resistance. Here, we reveal that inefficient accumulation of Apatinib, an anti-angiogenic TKI, induces the expression of ribosome-associated genes in osteosarcoma, and confers apoptosis resistance. An engineered nanoscale delivery system based on hydrophobic poly(ester amide) has been established to effectively deliver Apatinib to improve the treatment. Notably, the considerable uptake by osteosarcoma cells enables this nanodrug to distribute increasingly inside the tumor. Furthermore, the delivered nano-Apatinib can suppress osteosarcoma stemness and enhance osteosarcoma stem-like cell apoptosis, and overcomes the crucial bottleneck of the unfavorable stem-like cell residue for TKI therapy. Importantly, nano-Apatinib significantly inhibits the osteosarcoma stem-like cell-derived tumor growth in contrast with free Apatinib, with minimal side effects. These results suggest that this Apatinib-loaded nano delivery system may serve as a promising strategy to solve the issue of TKI therapeutic resistance existing in advanced osteosarcoma.
Insights
Apatinib nanodrug delivery overcomes resistance in osteosarcoma by targeting stem-like cells. This novel approach enhances apoptosis and inhibits tumor growth, offering a promising strategy against TKI resistance.
Area of Science:
- Oncology
- Nanomedicine
- Biotechnology
Background:
- Advanced osteosarcoma treatment faces challenges from persistent stem-like cells, leading to recurrence and resistance to anti-angiogenic tyrosine kinase inhibitors (TKIs).
- Inefficient intracellular accumulation of TKIs like Apatinib can induce apoptosis resistance and promote stemness in osteosarcoma cells.
Purpose of the Study:
- To develop an engineered nanoscale delivery system for Apatinib to enhance its efficacy in treating osteosarcoma.
- To investigate the potential of nano-Apatinib to overcome TKI resistance by targeting osteosarcoma stem-like cells.
Main Methods:
- Fabrication of a nanoscale delivery system using hydrophobic poly(ester amide) for Apatinib.
- Evaluation of Apatinib accumulation, osteosarcoma stemness suppression, and apoptosis induction in vitro and in vivo.
- Comparison of the therapeutic effects of nano-Apatinib versus free Apatinib in osteosarcoma models.
Main Results:
- The engineered nanodelivery system effectively delivered Apatinib into osteosarcoma cells, leading to increased intracellular accumulation.
- Nano-Apatinib suppressed osteosarcoma stemness and enhanced apoptosis in stem-like cells, addressing a key cause of TKI resistance.
- Nano-Apatinib significantly inhibited tumor growth derived from osteosarcoma stem-like cells with reduced side effects compared to free Apatinib.
Conclusions:
- The Apatinib-loaded nanoscale delivery system is a promising strategy to overcome therapeutic resistance in advanced osteosarcoma.
- Targeting osteosarcoma stem-like cells with nano-delivered Apatinib offers a potential solution for improving treatment outcomes.
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