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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
Bio-inspired self-assembly of omega-3 fatty acids and peptides for responsive drug delivery
Simone Braccia1,2, Luigi Alfano3, Maria Carmen Ragosta4
1Department of Pharmacy, School of Medicine, University of Naples Federico II, Naples, Italy.
Abstract:
Cancer treatments often yield unsatisfactory long-term clinical outcomes due to issues such as drug resistance, systemic toxicity, and suboptimal efficacy. Therefore, there is a need to develop novel drug delivery platforms for personalized medicine to enhance patient quality of life. In this study, an eicosapentaenoic acid (EPA)-based delivery system was developed and characterized. The system was functionalized with two different anticancer drugs, doxorubicin or pemetrexed, using an on-demand release strategy based on a proteolytic sequence specifically recognized by metalloproteinase-9 (MMP-9), an enzyme overexpressed in various cancers. We set-up the formulation procedure to obtain EPA-based nanoparticles (EPA-NPs) with a diameter of approximately 200 nm and low polydispersity, which were characterized for their aggregation properties and structural stability. The therapeutic efficacy was initially analyzed on HeLa cells as a cancer model due to their high transfection efficiency, reproducibility, and overexpression of MMP-9, using doxorubicin (Dox) as the drug. Enzyme-triggered drug release studies showed a rapid and controlled release profile, with approximately 80% of Dox released within 120 min in the presence of MMP-9. The efficient internalization was assessed using confocal microscopy; furthermore, Dox release induced an antiproliferative effect on HeLa cells (up to ∼60% cytotoxicity at 72 h) comparable to Dox free, while exhibiting no cytotoxicity toward healthy keratinocyte cells. Based on these results, the platform was later tested on a more disease-specific model, the mesothelioma, to confirm its relevance and adaptability for treating this aggressive cancer. These findings suggest that EPA nanoparticles could serve as a promising drug delivery platform.
Insights
A novel eicosapentaenoic acid (EPA) nanoparticle system delivers anticancer drugs like doxorubicin specifically to cancer cells. This targeted approach shows promise for personalized medicine by releasing drugs on-demand and reducing toxicity.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery Systems
Background:
- Current cancer treatments face challenges including drug resistance, systemic toxicity, and limited efficacy.
- There is a critical need for advanced drug delivery platforms to improve personalized medicine and patient outcomes.
- Metalloproteinase-9 (MMP-9) is an enzyme overexpressed in many cancers, presenting a potential target for drug delivery.
Purpose of the Study:
- To develop and characterize a novel eicosapentaenoic acid (EPA)-based nanoparticle (NP) drug delivery system.
- To functionalize EPA-NPs with anticancer drugs (doxorubicin or pemetrexed) for on-demand release triggered by MMP-9.
- To evaluate the therapeutic efficacy and specificity of the EPA-NP system in cancer models.
Main Methods:
- Formulation of EPA-based nanoparticles (EPA-NPs) with controlled size (~200 nm) and low polydispersity.
- Functionalization of EPA-NPs with doxorubicin (Dox) using an MMP-9-sensitive linker for triggered release.
- In vitro assessment of drug release kinetics, cellular internalization (confocal microscopy), and antiproliferative effects on HeLa cells and healthy keratinocytes.
Main Results:
- EPA-NPs demonstrated rapid and controlled release of Dox (~80% in 120 min) in the presence of MMP-9.
- The Dox-loaded EPA-NPs were efficiently internalized by cancer cells.
- Dox-loaded EPA-NPs induced significant antiproliferative effects on HeLa cells comparable to free Dox, with minimal toxicity to healthy keratinocytes.
Conclusions:
- Eicosapentaenoic acid nanoparticles represent a promising platform for targeted cancer drug delivery.
- The MMP-9-triggered release strategy enhances drug specificity and potentially reduces systemic toxicity.
- This platform shows adaptability for treating aggressive cancers like mesothelioma, supporting its potential in personalized medicine.
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