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Published on: December 15, 2010
PLGA Nanoplatform for the Hypoxic Tumor Delivery: Folate Targeting, Therapy, and Ultrasound/Photoacoustic Imaging
Abhishesh Kumar Mehata1, Jyoti Bonlawar1, Rupen Tamang2
1Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (BHU), Varanasi 221005, U.P., India.
Abstract:
Effective targeting of breast tumors is critical for improving therapeutic outcomes in breast cancer treatment. Additionally, hypoxic breast cancers are difficult to treat due to resistance toward chemotherapeutics, poor vascularity, and enhanced angiogenesis, which complicate effective drug delivery and therapeutic response. Addressing this formidable challenge requires designing a drug delivery system capable of targeted delivery of the anticancer agent, inhibition of efflux pump, and suppression of the tumor angiogenesis. Here, we have introduced Palbociclib (PCB)-loaded PLGA nanoparticles (NPs) consisting of chitosan-folate (CS-FOL) for folate receptor-targeted breast cancer therapy. The developed NPs were below 219 nm with a smooth, spherical surface shape. The entrapment efficiencies of NPs were achieved up to 85.78 ± 1.8%. Targeted NPs demonstrated faster drug release at pH 5.5, which potentiated the therapeutic efficacy of NPs due to the acidic microenvironment of breast cancer. In vitro cellular uptake study in MCF-7 cells confirmed the receptor-mediated endocytosis of targeted NPs. In vivo ultrasound and photoacoustic imaging studies on rats with hypoxic breast cancer showed that targeted NPs significantly reduced tumor growth and hypoxic tumor volume, and suppressed angiogenesis.
Insights
This study developed targeted nanoparticles loaded with Palbociclib for breast cancer therapy. These nanoparticles effectively reduced tumor growth and suppressed angiogenesis in hypoxic breast tumors.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Hypoxic breast cancers present treatment challenges due to drug resistance and poor vascularity.
- Targeted drug delivery systems are needed to overcome these challenges and improve therapeutic outcomes.
- Developing novel systems to inhibit efflux pumps and suppress tumor angiogenesis is crucial.
Purpose of the Study:
- To develop and evaluate folate receptor-targeted Palbociclib-loaded PLGA nanoparticles (NPs) for breast cancer therapy.
- To investigate the efficacy of these targeted NPs in addressing hypoxic tumor microenvironments.
- To assess the potential of the NPs to inhibit efflux pumps and suppress tumor angiogenesis.
Main Methods:
- Synthesis of chitosan-folate (CS-FOL) coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating Palbociclib (PCB).
- Characterization of NP size, shape, and drug entrapment efficiency.
- In vitro studies on drug release kinetics at different pH levels and cellular uptake in MCF-7 cells.
- In vivo evaluation using ultrasound and photoacoustic imaging in rats with induced hypoxic breast cancer.
Main Results:
- Developed NPs were spherical, <219 nm, with high entrapment efficiency (up to 85.78%).
- Targeted NPs exhibited faster drug release at acidic pH (5.5), enhancing therapeutic efficacy.
- In vitro studies confirmed receptor-mediated endocytosis, and in vivo imaging showed significant tumor growth reduction, decreased hypoxic volume, and suppressed angiogenesis.
Conclusions:
- Folate receptor-targeted Palbociclib-loaded PLGA nanoparticles represent a promising strategy for treating hypoxic breast cancer.
- The developed nanocarrier system effectively delivers the drug, enhances efficacy in acidic tumor microenvironments, and combats tumor angiogenesis.
- This approach offers a potential solution for overcoming therapeutic resistance in challenging breast cancer cases.
