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The Interactions between L-tyrosine based nanoparticles decorated with folic acid and cervical cancer cells under
Andrew J Ditto1, Kush N Shah, Nikki K Robishaw
1Department of Biomedical Engineering, The University of Akron, Olson Research Center, Akron, Ohio 44325-0302, United States.
Abstract:
Many anticancer drugs have been established clinically, but their efficacy can be compromised by nonspecific toxicity and an inability to reach the desired cancerous intracellular spaces. In order to address these issues, researchers have explored the use of folic acid as a targeted moiety to increase specificity of chemotherapeutic drugs. To expand upon such research, we have conjugated folic acid to functionalized poly(ethylene glycol) and subsequently decorated the surface of l-tyrosine polyphosphate (LTP) nanoparticles. These nanoparticles possess the appropriate size (100-500 nm) for internalization as shown by scanning electron microscopy and dynamic light scattering. Under simulated physiological flow, LTP nanoparticles decorated with folic acid (targeted nanoparticles) show a 10-fold greater attachment to HeLa, a cervical cancer cell line, compared to control nanoparticles and to human dermal fibroblasts. The attachment of these targeted nanoparticles progresses at a linear rate, and the strength of this nanoparticle attachment is shown to withstand shear stresses of 3.0 dyn/cm(2). These interactions of the targeted nanoparticles to HeLa are likely a result of a receptor-ligand binding, as a competition study with free folic acid inhibits the nanoparticle attachment. Finally, the targeted nanoparticles encapsulated with a silver based drug show increased efficacy in comparison to nondecorated (plain) nanoparticles and drug alone against HeLa cells. Thus, targeted nanoparticles are a promising delivery platform for developing anticancer therapies that overexpress the folate receptors (FRs).
Insights
Targeted nanoparticles using folic acid show a 10-fold increase in attachment to cervical cancer cells. These novel drug delivery systems demonstrate enhanced efficacy against cancer cells overexpressing folate receptors (FRs).
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Conventional anticancer drugs face challenges with nonspecific toxicity and limited cellular uptake.
- Folic acid conjugation is explored to enhance chemotherapeutic drug specificity.
- Folate receptors (FRs) are often overexpressed in various cancer cells, presenting a therapeutic target.
Purpose of the Study:
- To develop and evaluate folic acid-conjugated nanoparticles for targeted cancer therapy.
- To assess the cellular attachment, stability, and drug efficacy of these targeted nanoparticles.
Main Methods:
- Folic acid was conjugated to functionalized poly(ethylene glycol) and used to decorate l-tyrosine polyphosphate (LTP) nanoparticles.
- Nanoparticle size and internalization potential were analyzed using scanning electron microscopy and dynamic light scattering.
- Attachment efficiency to HeLa cervical cancer cells and human dermal fibroblasts under simulated physiological flow was quantified.
- Competition studies with free folic acid were performed to confirm receptor-ligand interactions.
- Efficacy of targeted nanoparticles loaded with a silver-based drug was compared to controls.
Main Results:
- LTP nanoparticles decorated with folic acid (targeted nanoparticles) exhibited a 10-fold greater attachment to HeLa cells compared to controls.
- Targeted nanoparticle attachment demonstrated a linear rate and withstood shear stresses up to 3.0 dyn/cm(2).
- Competition studies confirmed that attachment to HeLa cells is mediated by folate receptor binding.
- Targeted nanoparticles encapsulated with a silver-based drug showed increased efficacy against HeLa cells.
Conclusions:
- Folic acid-conjugated LTP nanoparticles represent a promising targeted delivery platform for anticancer therapies.
- This approach enhances drug specificity and efficacy, particularly for cancers overexpressing folate receptors (FRs).
- The developed nanoparticles show favorable characteristics for internalization and stability in physiological conditions.
