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Acylsulfonamide-Functionalized Zwitterionic Gold Nanoparticles for Enhanced Cellular Uptake at Tumor pH
Tsukasa Mizuhara1,2, Krishnendu Saha1, Daniel F Moyano1
1Department of Chemistry, University of Massachusetts Amherst, 710 North Pleasant Street, Amherst, MA 01003 (USA).
Angewandte Chemie (International Ed. in English)
|April 16, 2015
Summary
This study introduces pH-responsive nanoparticles that become positively charged in acidic tumor environments. This targeted charge change enhances particle uptake and toxicity, offering a promising approach for selective cancer therapy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Medicinal Chemistry
Background:
- Developing targeted drug delivery systems is crucial for improving cancer therapy efficacy.
- Nanoparticles offer a versatile platform for drug delivery, but achieving tumor selectivity remains a challenge.
- Modulating nanoparticle properties in response to the tumor microenvironment can enhance therapeutic outcomes.
Purpose of the Study:
- To design and characterize pH-responsive nanoparticles for tumor-selective therapy.
- To investigate the charge transition of nanoparticles at physiological and tumor-associated pH levels.
- To evaluate the impact of pH-controlled charge on nanoparticle uptake and cytotoxicity in cancer cells.
Main Methods:
- Synthesis of nanoparticles functionalized with pH-responsive alkoxyphenyl acylsulfonamide ligands.
- Measurement of nanoparticle surface charge (zeta potential) at pH 7.4 and pH < 6.5.
- Assessment of nanoparticle cellular uptake using flow cytometry or microscopy.
- Evaluation of nanoparticle cytotoxicity using cell viability assays.
Main Results:
- The designed nanoparticles exhibited neutral charge at pH 7.4 and transitioned to a positive charge at pH < 6.5, mimicking tumor microenvironment conditions.
- A significant increase in nanoparticle uptake was observed at lower pH values.
- Cytotoxicity of the nanoparticles was enhanced at tumor-associated acidic pH.
- The pH-triggered charge modulation directly correlated with increased cellular internalization and cell death.
Conclusions:
- The developed pH-responsive nanoparticles demonstrate tunable properties for enhanced tumor targeting.
- The charge-reversal mechanism facilitates selective accumulation and action within the acidic tumor microenvironment.
- These nanoparticles represent a promising strategy for developing effective and tumor-selective cancer therapies.
