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Co-delivery of doxorubicin and siRNA for glioma therapy by a brain targeting system: angiopep-2-modified
Lei Wang1, Yongwei Hao1, Haixia Li1
1a School of Pharmaceutical Sciences, Zhengzhou University , Zhengzhou , PR China.
Abstract:
It is very challenging to treat brain cancer because of the blood-brain barrier (BBB) restricting therapeutic drug or gene to access the brain. In this research project, angiopep-2 (ANG) was used as a brain-targeted peptide for preparing multifunctional ANG-modified poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), which encapsulated both doxorubicin (DOX) and epidermal growth factor receptor (EGFR) siRNA, designated as ANG/PLGA/DOX/siRNA. This system could efficiently deliver DOX and siRNA into U87MG cells leading to significant cell inhibition, apoptosis and EGFR silencing in vitro. It demonstrated that this drug system was capable of penetrating the BBB in vivo, resulting in more drugs accumulation in the brain. The animal study using the brain orthotopic U87MG glioma xenograft model indicated that the ANG-targeted co-delivery of DOX and EGFR siRNA resulted in not only the prolongation of the life span of the glioma-bearing mice but also an obvious cell apoptosis in glioma tissue.
Insights
This study developed angiopep-2 modified nanoparticles to overcome the blood-brain barrier for brain cancer treatment. The nanoparticles successfully delivered drugs and siRNA, inhibiting tumor growth and extending survival in mice.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Research
Background:
- The blood-brain barrier (BBB) poses a significant challenge for treating brain cancers, limiting drug and gene delivery.
- Effective strategies are needed to enhance therapeutic agent penetration into the brain for improved cancer treatment outcomes.
Purpose of the Study:
- To develop a multifunctional nanoparticle system for targeted delivery of doxorubicin (DOX) and epidermal growth factor receptor (EGFR) siRNA across the BBB.
- To evaluate the efficacy of angiopep-2 (ANG) modified nanoparticles in treating U87MG glioblastoma models both in vitro and in vivo.
Main Methods:
- Preparation of ANG-modified poly(lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating DOX and EGFR siRNA (ANG/PLGA/DOX/siRNA).
- In vitro assessment of nanoparticle uptake, cytotoxicity, apoptosis, and EGFR silencing in U87MG cells.
- In vivo evaluation of BBB penetration, brain drug accumulation, and therapeutic efficacy in a U87MG glioma xenograft mouse model.
Main Results:
- ANG/PLGA/DOX/siRNA nanoparticles demonstrated efficient delivery of DOX and siRNA into U87MG cells, leading to significant cell inhibition, apoptosis, and EGFR silencing in vitro.
- The nanoparticles successfully penetrated the BBB in vivo, increasing drug accumulation in the brain.
- Treatment with ANG-targeted nanoparticles significantly prolonged the lifespan of glioma-bearing mice and induced apoptosis in glioma tissues.
Conclusions:
- Multifunctional ANG-modified PLGA nanoparticles represent a promising strategy for overcoming the BBB and co-delivering therapeutic agents for brain cancer.
- This targeted delivery system enhances drug accumulation in the brain and demonstrates significant therapeutic benefits in preclinical models of glioblastoma.
