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Active targeting of cancer cells by CD44 binding peptide-functionalized oil core-based nanocapsules
A De Capua1,2, A Palladino3, M Chino4
1Center for Advanced Biomaterials for Health Care@CRIB, Istituto Italiano di Tecnologia Largo Barsanti e Matteucci 53 Napoli 80125 Italy raffaele.vecchione@iit.it.
Abstract:
Selectivity in tumor targeting is one of the major issues in cancer treatment. Therefore, surface functionalization of drug delivery systems with active moieties, able to selectively target tumors, has become a worldwide-recognized strategy. The CD44 receptor is largely used as a biomarker, being overexpressed in several tumors, and consequently as a target thanks to the identification of the CD44 binding peptide. Here we implemented the CD44 binding peptide logic onto an oil core-polymer multilayer shell, taking into account and optimizing all relevant features of drug delivery systems, such as small size (down to 100 nm), narrow size distribution, drug loading capability, antifouling and biodegradability. Besides promoting active targeting, the oil core-based system enables the delivery of natural and synthetic therapeutic compounds. Biological tests, using curcumin as a bioactive compound and fluorescent tag, demonstrated that CD44 binding peptide-functionalized nanocapsules selectively accumulate and internalize in cancer cells, compared to the control, thanks to ligand-receptor binding.
Insights
Researchers developed targeted nanocapsules using CD44 binding peptides to improve cancer treatment selectivity. These targeted nanocarriers effectively deliver drugs to cancer cells, enhancing therapeutic outcomes.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Tumor targeting selectivity is a critical challenge in cancer therapy.
- Surface functionalization of drug delivery systems with tumor-targeting moieties is a key strategy.
- The CD44 receptor, overexpressed in many tumors, is a validated target using CD44 binding peptides.
Purpose of the Study:
- To engineer oil core-polymer multilayer nanocapsules functionalized with CD44 binding peptides for targeted cancer drug delivery.
- To optimize nanocarrier features including size, drug loading, antifouling, and biodegradability.
- To evaluate the selective accumulation and internalization of these nanocapsules in cancer cells.
Main Methods:
- Development of oil core-polymer multilayer nanocapsules.
- Functionalization of nanocapsule surfaces with CD44 binding peptides.
- Optimization of nanocarrier physicochemical properties (size, distribution, loading).
- In vitro biological testing using curcumin as a model drug and fluorescent tag.
Main Results:
- Successfully created nanocapsules with optimized features (down to 100 nm, narrow size distribution).
- Demonstrated selective accumulation and internalization of CD44 binding peptide-functionalized nanocapsules in cancer cells.
- Confirmed ligand-receptor binding as the mechanism for targeted delivery.
Conclusions:
- CD44 binding peptide-functionalized nanocapsules represent a promising strategy for targeted cancer therapy.
- The developed system enables efficient delivery of therapeutic compounds to CD44-expressing tumors.
- This approach enhances drug delivery selectivity and potentially improves treatment efficacy.
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