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Nanoparticles functionalized with Pep-1 as potential glioma targeting delivery system via interleukin 13 receptor
Baoyan Wang1, Lingyan Lv2, Zhongyuan Wang2
1Department of Pharmaceutics, School of Pharmacy, Nanjing Medical University, Nanjing 211166, China; Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, China.
Abstract:
The treatment for glioma is one of the most challenging problems and therapeutic effect of glioma is often limited due to poor penetration into the tumor tissue. Interleukin 13 receptor α2 (IL-13Rα2) is over-expressed on tumor including established glioma cell lines and primary glioblastoma cell cultures. However, it will not cause activation of its signaling pathways. So it could be served as a promising targeted moiety for anti-glioma drug delivery. Pep-1, one specific ligand of IL-13Rα2, was identified to exhibit excellent capacity of crossing the blood tumor barrier (BTB) and homing to giloma. In this study, based on the IL-13Rα2-mediated endocytosis, Pep-1 was exploited as a potential ligand for effective glioma-targeting delivery. Pep-1 was functionalized to the surface of PEG-PLGA nanoparticles (Pep-NP) to evaluate its glioma homing, by taking advantage of the excessive expression of the IL-13Rα2 on the surface of glioma cells. Compared with non-targeting nanoparticles, Pep-NP exhibited a significantly enhanced cellular association in rat C6 glioma cells and improved penetration in 3D avascular C6 glioma spheroids. Following intravenous administration, Pep-NP could facilitate the distribution of the coumarin-6 in vivo glioma region, 2.21 times higher than that of NP for quantitative analysis. In conclusion, the Pep-NP could precisely target to the brain glioma, which was a potential targeting drug delivery system for glioma treatment.
Insights
Researchers developed Pep-1 functionalized nanoparticles (Pep-NP) for targeted glioma delivery. Pep-NP showed enhanced cellular uptake and penetration in glioma models, demonstrating potential for improved brain tumor treatment.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Glioma treatment faces challenges due to poor drug penetration into tumor tissue.
- Interleukin 13 receptor α2 (IL-13Rα2) is over-expressed on gliomas, making it a potential therapeutic target.
- Pep-1, an IL-13Rα2 ligand, can cross the blood-tumor barrier and target gliomas.
Purpose of the Study:
- To develop and evaluate Pep-1 functionalized nanoparticles (Pep-NP) for targeted glioma delivery.
- To leverage IL-13Rα2-mediated endocytosis for enhanced glioma homing.
- To assess the efficacy of Pep-NP in vitro and in vivo glioma models.
Main Methods:
- Functionalization of PEG-PLGA nanoparticles with Pep-1 ligand (Pep-NP).
- Evaluation of cellular association in rat C6 glioma cells.
- Assessment of nanoparticle penetration in 3D C6 glioma spheroids.
- In vivo studies using coumarin-6 labeled nanoparticles after intravenous administration.
Main Results:
- Pep-NP demonstrated significantly enhanced cellular association compared to non-targeting nanoparticles.
- Pep-NP showed improved penetration in 3D glioma spheroids.
- In vivo studies revealed a 2.21-fold higher distribution of Pep-NP in glioma regions compared to non-targeted nanoparticles.
Conclusions:
- Pep-NP precisely targets brain glioma.
- This Pep-1-based nanoparticle system shows potential as a drug delivery platform for glioma treatment.
