Described herein are novel conjugates containing an inhibitor (e.g., a PSMA inhibitor, e.g., a gastrin-releasing peptide receptor inhibitor) and metal chelator that are covalently attached to a macromolecule (e.g., a nanoparticle, a polymer, a protein). Such conjugates exhibit distinct properties over the free, unbound inhibitor/chelator construct.

The present invention provides a fluorescent silica-based nanoparticle that allows for precise detection, characterization, monitoring and treatment of a disease such as cancer. The nanoparticle has a range of diameters including between about 0.1 nm and about 100 nm, between about 0.5 nm and about 50 nm, between about 1 nm and about 25 nm, between about 1 nm and about 15 nm, or between about 1 nm and about 8 nm. The nanoparticle has a fluorescent compound positioned within the nanoparticle, and has greater brightness and fluorescent quantum yield than the free fluorescent compound. The nanoparticle also exhibits high biostability and biocompatibility. To facilitate efficient urinary excretion of the nanoparticle, it may be coated with an organic polymer, such as poly(ethylene glycol) (PEG). The small size of the nanoparticle, the silica base and the organic polymer coating minimizes the toxicity of the nanoparticle when administered in vivo. In order to target a specific cell type, the nanoparticle may further be conjugated to a ligand, which is capable of binding to a cellular component associated with the specific cell type, such as a tumor marker. In one embodiment, a therapeutic agent may be attached to the nanoparticle. To permit the nanoparticle to be detectable by not only optical fluorescence imaging, but also other imaging techniques, such as positron emission tomography (PET), single photon emission computed tomography (SPECT), computerized tomography (CT), bioluminescence imaging, and magnetic resonance imaging (MRI), radionuclides/radiometals or paramagnetic ions may be conjugated to the nanoparticle.

A drug carrier nanoparticle has been synthesized that can specifically target the proximal tubules of the kidneys. The nanoparticles accumulate in the kidneys to a greater extent than other organs (e.g., up to 3 or more times greater in the kidney than any other organ). They can encapsulate many classes of drug molecules. The nanoparticles are biodegradable and release the drug as they degrade. The particles can sustainably release a drug within the kidneys for up to two months. The nanoparticles are useful for the treatment of diseases that affect the proximal tubules, such as heart failure, liver cirrhosis, hypertension, and renal failure; the study of relative blood flow to the renal cortex and medulla; and delivery of agents to treat gout.

Shielding enzymes are made by modifying the enzyme surface with silica precursors and then depositing silica to a desired thickness while retaining biological activity of the enzyme.

The invention relates to a multifunctional system stable in a physiological medium, which includes in the same platform an anti-carcinogenic molecule, an imaging agent and a directing molecule that interacts specifically with cancer-cell membrane receptors, the system allowing pathological tissue imaging and pharmacological action to be carried out jointly with high specificity. The intratumoral administration of the system facilitates selective diffusion to cancer cells and minimises the disadvantages of chemotherapy.

A multimodal PET (positron emission tomography)/MRI (magnetic resonance imaging) contrast agent, a process of synthesizing said PET/MRI contrast agent, and a pharmaceutical formulation comprising said PET/MRI contrast agent are disclosed. The PET/MRI contrast agent comprises a magnetic signal generating core, and a coating portion formed at least partially over a surface of said magnetic signal generating core, wherein the coating portion comprises a plurality of layers, including an inner layer having a functionalized surface, and an outer layer in the form of a radionuclide electrolessly plated layer formed on said functionalized surface.

Provided are a contrast agent for optical imaging, a use thereof and an apparatus using the same. The contrast agent for optical imaging of the present disclosure allows optical imaging without requiring a fluorophore or a luminophore. As a result, the optical images can be acquired without changing the physicochemical properties of a substrate. The contrast agent for optical imaging of the present disclosure may be used as an optical/nuclear bimodal imaging contrast agent for many applications, and allows radiation therapy as well as monitoring of a therapeutic effect thereof through optical imaging at the same time. Further, when a fluorophore is attached thereto, light emission may be enhanced without energy input from outside since light is emitted from the fluorophore, thereby increasing luminescence intensity and improving tissue penetration.

Described is a versatile surface modification approach to, for example, modularly and orthogonally functionalize nanoparticles (NPs) such as, for example, PEGylated nanoparticles, ith various types of different functional ligands (functional groups) on the NP surface. It enables the synthesis of, for example, penta-functional PEGylated nanoparticles integrating a variety of properties into a single NP, e.g., fluorescence detection, specific cell targeting, radioisotope chelating/labeling, ratiometric pH sensing, and drug delivery, while the overall NP size remains, for example, below 10 nm.

This invention relates to strontium-phosphate microparticles that incorporate radioisotopes for radiation therapy and imaging.

Provided are radiopaque compositions comprising one or more of yttrium (Y), strontium (Sr), gallium (Ga), and silicon, or oxides and salts thereof. The composition can comprise a combination of Y.sub.2O.sub.3, SrCO.sub.3, Ga.sub.2O.sub.3, and SiO.sub.2, and optionally MnO.sub.2, and TiO.sub.2. Other compositions comprise SrCO.sub.3, Ga.sub.2O.sub.3, TiO.sub.2, MnO.sub.2, and SiO.sub.2. The composition can be a particulate material. The compositions are useful for radioembolization to treat tumors.