Introduction: High grade gliomas are characterized by a very poor prognosis due to fatal relapses after surgery. Current chemotherapy is only a palliative care, while potential drug candidates are limited by poor overcoming of the blood-brain barrier.
Aims: A suitable chemotherapeutic approach should be engineered to overcome both the altered blood-brain barrier in the glioma site, as well as the intact one in the brain adjacent to tumor zone, and to target the multiple factors influencing glioma proliferation, differentiation, migration, and angiogenesis.
This work presents a group of high-quality hydrophilic and negatively charged coated, iron oxide magnetic nanoparticles (MNPs) that have been prepared using a microwave-ultrasound-assisted protocol, and demonstrates the great impact that the synthetic strategy has on the resulting MNPs. The different coatings tested, including citric acid, carboxymethyl dextran and β-cyclodextrin (βCD)/citric acid have been compared and have shown good dispersibility and stability. The ability of βCD to maintain the inclusive properties of the coated MNPs has been proven as well as their cytocompatibility.
View Article and Find Full Text PDFMacrocyclic chelators play a central role in medical imaging and nuclear medicine owing to their unparalleled metal cation coordination abilities. Their functionalization by fluorinated groups is an attractive design, to combine their properties with those of F for Positron Emission Tomography (PET) or natural F for Magnetic Resonance Imaging (MRI), and access potential theranostic or smart medical imaging probes. For the first time, a compact fluorinated macrocyclic architecture has been synthesized, based on a cyclen chelator bearing additional pyridine coordinating units and simple methyltrifluoroborate prosthetic groups.
View Article and Find Full Text PDFThe certification of cosmetic products has always been a prominent concern. Here, we have developed a pH sensor and applied it in the field of cosmetic safety. Initially, we designed two probes, CH with aggregation-induced emission (AIE) effect and the near-infrared fluorophore derivative CYTYR.
View Article and Find Full Text PDFThe self-assembly of peptides and peptide analogues may be exploited to develop platforms for different biomedical applications, among which CEST-MRI (chemical exchange saturation transfer magnetic resonance imaging) represents one of the most attractive techniques to be explored as a novel metal-free contrast approach in imaging acquisitions. A lysine-containing peptide sequence (LIVAGK-NH, named K2) was thus modified by insertion, at the N-terminus, of a peptide nucleic acid (PNA) base, leading to a primary amine suitable for the signal generation. a-K2, c-K2, g-K2 and t-K2 peptides were synthesized and characterized.
View Article and Find Full Text PDFThis paper describes a novel nanoformulation for dual MRI/US in vivo monitoring of drug delivery/release. The nanosystem was made of a perfluoropentane core coated with phospholipids stabilized by glycol chitosan crosslinked with triphosphate ions, and it was co-loaded with the prodrug prednisolone phosphate (PLP) and the structurally similar MRI agent Gd-DTPAMA-CHOL. Importantly, the in vitro release of PLP and Gd-DTPAMA-CHOL from the nanocarrier showed similar profiles, validating the potential impact of the MRI agent as an imaging reporter for the drug release.
View Article and Find Full Text PDFPeptide-based hydrogels have been recently investigated as materials for biomedical applications like tissue engineering and delivery of drugs and imaging agents. Among the synthetic peptide hydrogelators, the cationic hexapeptides Ac-K1 and Ac-K2 were proposed as scaffolds for bioprinting applications. Here, we report the formulation of Ac-K1 and Ac-K2 hydrogels loaded with iopamidol, an iodinated contrast agent clinically approved for X-ray computed tomography, and more recently identified as an efficient CEST-MRI probe.
View Article and Find Full Text PDFDrug repurposing is a valuable strategy for rare diseases. Sickle cell disease (SCD) is a rare hereditary hemolytic anemia accompanied by acute and chronic painful episodes, most often in the context of vaso-occlusive crisis (VOC). Although progress in the knowledge of pathophysiology of SCD have allowed the development of new therapeutic options, a large fraction of patients still exhibits unmet therapeutic needs, with persistence of VOCs and chronic disease progression.
View Article and Find Full Text PDFBackground: Breast cancer is the most common malignancy in women, with high morbidity and mortality. Molecular alterations in breast cancer involve the expression or upregulation of various molecular targets that can be used for diagnostic nuclear medicine imaging and radiopharmaceutical treatment. Theragnostics is based on the binding of radionuclides to molecular targets.
View Article and Find Full Text PDFOvarian cancer (OC) is characterised by the highest mortality of all gynaecological malignancies, frequent relapses, and the development of resistance to drug therapy. Sonodynamic therapy (SDT) is an innovative anticancer approach that combines a chemical/drug (sonosensitizer) with low-intensity ultrasound (US), which are both harmless per sé, with the sonosensitizer being acoustically activated, thus yielding localized cytotoxicity often via reactive oxygen species (ROS) generation. Doxorubicin (Doxo) is a potent chemotherapeutic drug that has also been recommended as a first-line treatment against OC.
View Article and Find Full Text PDFDevelopment of the field of magnetic resonance imaging (MRI) chemical exchange saturation transfer (CEST) contrast agents is hampered by the limited sensitivity of the technique. In water, the high proton concentration allows for an enormous amplification of the exchanging proton pool. However, the H CEST in water implies that the number of nuclear spins of the CEST-generating species has to be in the millimolar range.
View Article and Find Full Text PDFThe development of multimodal imaging techniques such as positron emission tomography (PET) and magnetic resonance imaging (MRI) allows the contemporary obtaining of metabolic and morphological information. To fully exploit the complementarity of the two imaging modalities, the design of probes displaying radioactive and magnetic properties at the same time could be very beneficial. In this regard, transition metals offer appealing options, with manganese representing an ideal candidate.
View Article and Find Full Text PDFBreast cancer is one of the most common malignancies in women, with high morbidity and mortality rates. In breast cancer, the use of novel radiopharmaceuticals in nuclear medicine can improve the accuracy of diagnosis and staging, refine surveillance strategies and accuracy in choosing personalized treatment approaches, including radioligand therapy. Nuclear medicine thus shows great promise for improving the quality of life of breast cancer patients by allowing non-invasive assessment of the diverse and complex biological processes underlying the development of breast cancer and its evolution under therapy.
View Article and Find Full Text PDFNanogels (NGs) obtained by electrostatic interactions between chitosan and hyaluronic acid and comprising paramagnetic Gd chelates are gaining increasing attention for their potential application in magnetic resonance bioimaging. Herein, the macrocyclic complexes [Gd(DOTP)], lacking metal-bound water molecules ( = 0), were confined or used as a cross-linker in this type of NG. Unlike the typical behavior of Gd complexes with = 0, a remarkable relaxivity value of 78.
View Article and Find Full Text PDFNovel Mn(II)-based nanoprobes were rationally designed as high contrast enhancing agents for magnetic resonance imaging (MRI) and obtained by anchoring a Mn(II)-CDTA derivative to the surface of organo-modified silica nanoparticles (SiNPs). Large payloads of paramagnetic metal-chelates have been immobilized on biocompatible SiNPs with spherical shape and narrow size distribution of 80-90 nm, resulting in a relaxivity gain of 250% at clinical fields (0.5 T) as compared to the free chelate.
View Article and Find Full Text PDFD-Glucose and 3-O-Methyl-D-glucose (3OMG) have been shown to provide contrast in magnetic resonance imaging-chemical exchange saturation transfer (MRI-CEST) images. However, a systematic comparison between these two molecules has yet to be performed. The current study deals with the assessment of the effect of pH, saturation power level (B ) and magnetic field strength (B ) on the MRI-CEST contrast with the aim of comparing the in vivo CEST contrast detectability of these two agents in the glucoCEST procedure.
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