Abstract
Nanoparticles have been employed to develop nanosensors and drug carriers that accumulate in tumors. Thus, it is necessary to control the particle size, surface potential, and biodegradability of these nanoparticles for effective tumor accumulation and safe medical application. In this study, to form a nanoparticle platform suitable for diagnostic and drug delivery system (DDS) applications, peptides composed of aromatic amino acid residues were designed and synthesized based on the radiation crosslinking mechanism of proteins. The peptide nanoparticles, which were produced by γ-ray irradiation, displayed a positive surface potential, maintained biodegradability, and were stable in water and phosphoric buffer solution during actual diagnosis. The surface potential of the peptide nanoparticles could be changed to negative by using a fluorescent labeling reagent, so that the fluorescent-labeled peptide nanoparticles were uptaken by HeLa cells. The radiation-crosslinked nanoparticles can be applied as a platform for tumor-targeting diagnostics and DDS therapy.
Highlights
There are various diagnostic methods for tumors in medical treatment; some of them impose drug side-effects on the patients
Nanoparticlebased contrast agents that can be applied to common biomedical imaging devices such as fluorescence imaging, magnetic resonance imaging (MRI), computerized tomography (CT), positron emission tomography (PET), and single-photon emission computerized tomography (SPECT) have been developed [6]
Nanoparticle cell uptake depends on the surface potential, which is measured as a Zeta potential by the electrophoretic light scattering (ELS) method
Summary
There are various diagnostic methods for tumors in medical treatment; some of them impose drug side-effects on the patients. 150 nm-sized nanoparticles with a trace negative charge tended to effectively accumulate in the tumor [18] These reported results indicate that the nanoparticle surface potential significantly affects their accumulation and stability in the cell. Apart from the particle size and surface potential, the amino acid composition in nanoparticles is an important factor for cell adhesion and accumulation to the tumor cell. Techniques that produce nanoparticles with precisely controlled particle sizes, surface charge, cell adhesion, and biodegradability are required to accumulate nanoparticles to the tumor and eliminate from the body. Peptide nanoparticles with a particle size of ~100 nm, controlled surface potential, no toxic crosslinking agent, and biodegradability were developed by the radiation crosslinking technique. We employed five amino acid residues per peptide and designed and synthesized six peptides to form a radiation-crosslinked nanoparticle platform
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