Disclosed herein are complexes of gadolinium metal, ligand and meglumine that are substantially free of non-aqueous solvents. In particular, solvent-free complexes of 1) gadopentetate dimeglumine and 2) gadoterate meglumine are disclosed and methods of their preparation are disclosed. In addition, methods are disclosed for purifying reactants, monitoring and controlling pH, quantifying the free gadolinium content, quantifying the concentration of gadolinium-ligand complex in aqueous solution, and procedures for producing a drug product in one step. The one step process eliminates the need to dry the gadolinium-ligand complex, which is typically highly hygroscopic. The one step process includes purification steps that do not require the use of non-aqueous solvents.

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

Disclosed is a lymph targeting nuclear magnetic contrast agent using a brown algae polysaccharide as a carrier, and a preparation method and a use thereof. A macromolecular contrast agent with good water solubility was prepared by using the brown algae polysaccharide as the carrier, using mannose or mannose derivatives as a mannose receptor (MBP) recognition group, and using a paramagnetic metal ion chelate as a nuclear magnetic resonance imaging group. The binding capacity of lymphoid tissue was improved. The mannose or mannose derivative group introduced into the synthesized contrast agent molecule achieves the goal of binding to the enriched mannose receptors in the lymphoid tissues. At the same time, after the contrast agent is injected subcutaneously, both lymph vessels and lymph nodes were clearly visualized under MRI scanning. The intensification rate and enhancement time of the lymph node signal at one side of the animal body injected with the contrast agent was significantly enhanced, so as to achieve a clear mapping and precise positioning of the lymph nodes and the lymph vessels. It is of great significance for the detection and diagnosis of lymph system diseases.

In the present invention, the development of various oil-in-water (O/W) nanoemulsions containing an oil phase or oil core, preferably selected from vitamin E or oleic acid, stabilized by a sphingolipid of the sphingomyelin type, and optionally other lipids such as phospholipids, cholesterol, octadecylamine, DOTAP (N-[1-(2,3-Dioleoyloxy) propyl]-N, N, N-trimethylammonium methyl-sulfate), and PEGylated derivatives (derivatives with polyethylene glycol), for use as a nanotech vehicle, in particular for the management of cancer and metastatic disease, is herein described. Said nanoemulsions can be functionalized with ligands capable of interacting or binding to receptors expressed on the cell membrane of tumor cells, and in particular capable of interacting or binding to receptors expressed on the membrane of primary and/or disseminated or metastatic tumor cells. Also, antitumor drugs or therapeutic biomolecules can be encapsulated in said nanoemulsions and, finally, contrast agents can be incorporated for their use in the in vivo diagnosis in said nanoemulsions.

Provided herein is a compound useful as a magnetic resonance imaging (MRI) contrast agent and a therapeutic agent, said compound having a structure represented by: Y—X—Z wherein, X is Mn(II), and Y and Z are each independently a bisphosphonate coupled to one or more therapeutic agents. Methods of use of the compound for MRI imaging and treatment for cancer or a microbial infection are also provided.

The disclosure discloses an amphiphilic polymer nano micelle containing poly-3,4-dihydroxyphenylalanine chelated ferric ions, in which ferric ions are chelated with a catechol structure on a side chain of a biodegradable poly-3,4-dihydroxyphenylalanine block. The disclosure also provides a method for preparing the above micelle, comprising: complexing an amphiphilic polymer containing poly-3,4-dihydroxyphenylalanine with a ferric ion compound, and obtaining the amphiphilic polymer nano micelle containing poly-3,4-dihydroxyphenylalanine chelated ferric ions through a solvent replacement method. The micelle prepared by the disclosure is used as a Fe.sup.3+ magnetic resonance Ti imaging contrast agent, which can avoid toxic or side effects caused by a traditional gadolinium reagent, has a longitudinal relaxation rate of 5.6 mM.sup.1.Math.s.sup.1, can cycle for 150 min in a mice body, and has an obvious imaging effect and a far higher comprehensive performance than that of a commercial gadolinium contrast agent, and as well as a promising application prospect.

Provided herein are examples of metal chelating ligands that have high affinity for manganese. The resultant metal complexes can be used as MRI contrast agents, and can be functionalized with moieties that bind to or cause relaxivity change in the presence of biochemical targets.

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

The present invention relates to the use of a formation agent, such as nitric oxide or sodium nitrite to produce methemoglobin as an alternative MRI contrast agent. The formation agent can be infused using either a respiratory system or a delivery mechanism. One embodiment of this invention relates to systems and methods for producing an image of an internal region with a magnetic resonance scanning system. Blood is drawn from the patient. The blood is exposed to formation agent through a delivery system, to produce blood that has a higher saturation of methemoglobin. Where in vitro techniques are used the treated blood is injected back into the patient. The patient is scanned in the magnetic resonance scanner. These systems and methods can be used to produce images of regions which may not otherwise be possible with other contrasting agents. For example, an accurate vascular brain MRI may not be as informative if the patient is injected with an existing contrasting agent. In addition, an alternate embodiment of the invention relates to internally exposing the blood to the formation agent by placing the gas-permeable membrane along a particular blood pathway or intravenous sodium nitrite.

A composition in the form of a water-in-oil emulsion comprising: from 20% to 40% (v/v) of aqueous phase, in the form of droplets, comprising an anti-cancer agent and a densifying agent chosen from the complexes of nonionic macrocyclic chelate with a paramagnetic metal, from 60% to 80% (v/v) of lipid phase comprising an iodized oil and at least one surfactant of formula (I) in a proportion, by weight of surfactant relative to the total volume of the composition, of 0.3% to 5%, formula (I) of said surfactant being the following: ##STR00001##
in which: s is 0 or 1, m is an integer from 2 to 30, R.sub.1 represents a group of formula (II) ##STR00002## in which n is an integer from 4 to 10, o is an integer from 1 to 4, p is an integer from 3 to 7, q is an integer from 2 to 10, and r is 0 or 1, R.sub.2 represents a hydrogen atom or is identical to R.sub.1, and each R.sub.3 independently represents a hydrogen atom or is identical to R.sub.1.