Cyclodextrin-assisted assembly of PEGylated polyester nanoparticles decorated with folate
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Claudia Conte1, Iolanda Fotticchia1, Pasquale Tirino2
1Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
Abstract:
In the last decades, nano-oncologicals bearing a polyethylene glycol (PEG) coating are being emerging as biomimetic devices able to drive their drug cargo to solid tumors through passive mechanisms. To improve selectivity toward cancer cells, nanocarriers decorated with the small ligand folate have been widely investigated. Nevertheless, a great challenge remains the effective exposition of folate on nanoparticles (NPs), which is a key prerequisite to ensure the correct binding to receptor and the following endocytic uptake. On these premises, in this study we propose a novel strategy to produce core-shell folate-targeted NPs based on diblock copolymers of poly(ε-caprolactone) (PCL) and PEG through the aid of (2-hydroxypropyl)-β-cyclodextrin (HPβCD). PCL4300-PEG2000 and PCL4300-PEG2000-Fol copolymers were synthesized, characterized and employed to produce NPs without and with HPβCD by a melting/sonication procedure. Colloidal properties of targeted NPs produced with HPβCD demonstrated a highly extended conformation of PEG chains in the shell, an enhanced interaction with a specific antibody against folate and a higher uptake in cells overexpressing folate receptor. Overall, these results suggest that proper manipulation of PEG shell conformation through HPβCD can represent a novel non-covalent strategy to modify shell features.
Insights
Researchers developed novel folate-targeted nanoparticles using poly(ε-caprolactone) (PCL) and polyethylene glycol (PEG) with (2-hydroxypropyl)-β-cyclodextrin (HPβCD). This strategy enhances folate presentation on nanoparticles, improving cancer cell targeting and uptake.
Area of Science:
- Nanomedicine
- Biomaterials Science
- Oncology
Background:
- Polyethylene glycol (PEG)-coated nano-oncologicals facilitate passive tumor targeting.
- Folate-decorated nanocarriers improve cancer cell selectivity.
- Effective folate display on nanoparticles is crucial for receptor binding and cellular uptake.
Purpose of the Study:
- To develop a novel strategy for producing core-shell folate-targeted nanoparticles (NPs).
- To investigate the role of (2-hydroxypropyl)-β-cyclodextrin (HPβCD) in enhancing folate presentation on NPs.
- To improve the efficacy of folate-mediated cancer cell targeting.
Main Methods:
- Synthesis and characterization of PCL-PEG and PCL-PEG-folate copolymers.
- Production of NPs using a melting/sonication method with and without HPβCD.
- Evaluation of colloidal properties, folate interaction, and cellular uptake of targeted NPs.
Main Results:
- NPs produced with HPβCD exhibited extended polyethylene glycol (PEG) chain conformation.
- Enhanced interaction with anti-folate antibodies was observed for HPβCD-modified NPs.
- A higher uptake of targeted NPs was noted in cells overexpressing folate receptors.
Conclusions:
- HPβCD aids in the effective display of folate on nanoparticle surfaces.
- Manipulation of PEG shell conformation via HPβCD is a viable non-covalent strategy.
- This approach offers a promising method for improving folate-targeted nanomedicine delivery.
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