Abstract: The present invention is directed to therapeutic compounds capable of targeting cancer cells and cancer stem cells. The present invention is further directed to compositions comprising these therapeutic compounds and methods of treating cancer comprising administering these therapeutic compounds.

Abstract: Supramolecular assemblies for delivering active agents to cancerous or precancerous tissues in a subject are provided. These supramolecular assemblies are also useful in assays for detecting and imaging of cancerous and precancerous cells. The assemblies are protease-sensitive and comprise a peptide linkage containing a protease consensus sequence. The assemblies can be selectively targeted to cancerous tissue where the protease enzymes degrade the peptide linkage thereby releasing the active agents which were physically or mechanically contained in or retained by the supramolecular assembly.

Abstract: An aqueous terconazole composition comprises at least about 0.4 percent by weight of terconazole dissolved in water, and a terconazole crystallization-inhibiting amount of an organic acid. Preferably the organic acid is a water soluble alkyl carboxylic acid, a polybasic organic acid, or a combination thereof. The composition is free from terconazole crystals at an ambient temperature of about 20° C. Methods of preparing the composition are also described. The compositions provide for improved therapeutic release of terconazole.

Abstract: One aspect of the disclosure relates to a new form of lipid-complexed active platinum compound, which allows for high concentrations of platinum compound in the composition. For example, the concentration of cisplatin in the composition is higher at room temperature, e.g., about greater than 1.2 mg/mL, compared to 1 mg/mL in aqueous solution. In one embodiment, the present invention is directed to a composition comprising a lipid-complexed active platinum compound, wherein the complex has a lipid to drug (L/D) ratio of less than about 1 by weight, e.g. about 0.10 to 1, wherein the lipid-complexed active platinum compound comprises at least one lipid and at least one active platinum compound. In other embodiments, wherein lipid-complexed active platinum compound has an average volume-weighted diameter of about 0.5 to about 20 microns. In still other embodiments, the composition further comprises a liposome.

Abstract: The invention broadly comprises a chemical composition including a plurality of cholesteryl esters arranged to form a vesicle. In several embodiments, all of the plurality of cholesteryl esters have a same molecular length, which in some embodiments provides a vesicle having a generally smooth outer surface, while in other embodiments, a portion of the plurality of cholesteryl esters have different molecular lengths, which in some embodiments provides a vesicle having a generally irregular outer surface. In yet further embodiments, a shape of the vesicle is selected from the group consisting of spherical, oval, disc-like, tubular and polyhedral shapes, and in yet other embodiments, a wall of the vesicle is selected from the group consisting of a monolayer and a bilayer. In still further embodiments, the chemical composition further includes a polyethylene glycol coat of mixed polymer size.

Abstract: This invention provides polynucleotide molecules and methods for regulating genes in plants, e.g., by providing RNA for systemic regulation of genes. Various aspects of the invention provide polynucleotide molecules and methods for regulating endogenous genes and transgenes in a plant cell and polynucleotide molecules.

Abstract: A method for treating cancer, preventing cancer or delaying the progression of a cancer in an animal or human comprising the step of: administering to the animal or the human having a cancer a composition in an amount effective to treat cancer, prevent cancer or delay the progression of cancer in the animal or the human. The composition comprises a pharmaceutically acceptable excipient, and ascorbate which is joined to a carrier structure containing an anti-cancer active agent, said carrier structure being capable of releasing the anti-cancer agent in the presence of a reactive oxygen species.

Abstract: The present disclosure is related to a pharmaceutical composition for detecting human melanoma cells, including: a liposome, a biomolecule having specificity for ?v?3 integrin and a radionuclide. The present disclosure also provides a method using the pharmaceutical composition for detecting human melanoma cells and a kit performing the method. By means of the specificity of the biomolecule for the ?v?3 integrin, the liposome is enabled to have recognition ability and facilitates the interaction between the liposome and a target cell. Therefore, the present disclosure is capable of being widely applied in the field of melanoma diagnosis, lymphatic metastasis detection and post-surgical monitoring, and so on.

Abstract: The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

Abstract: Disclosed are compositions that include anti-CD74 immunoconjugates and optionally a therapeutic and/or diagnostic agent. In preferred embodiments, the immunoconjugates comprise one or more anti-CD74 antibodies or antigen-binding fragments thereof, conjugated to a carrier such as a polymer, nanoparticle, complex or micelle. Also disclosed are methods for preparing the immunoconjugates and using the immunoconjugates in diagnostic and therapeutic procedures. In certain preferred embodiments, the therapeutic methods comprise administering to a subject with a CD74-expressing disease an anti-CD74 immunoconjugate and thereby inducing cell death of CD74-expressing cells. In more preferred embodiments, the CD74 immunoconjugate is capable of inducing cell death in the absence of any other therapeutic agent, although such agents may be optionally administered prior to, together with or subsequent to administration of the anti-CD74 immunoconjugate.

Abstract: The present invention provides a polymer-metal complex composite, which comprises a block copolymer capable of serving as a constituent member of a polymeric micelle and a metal complex having MRI contrast ability, accumulates in a tumor-specific manner, achieves high image contrast even in a small amount, and has reduced side effects and a long retention time in blood. The polymer-metal complex composite of the present invention comprises a block copolymer (A) represented by general formula (a) and a metal complex (B) having MRI contrast ability, wherein the composite comprises a structure in which a carboxyl anion of poly(carbo) in the copolymer (A) is attached to the metal complex (B) via a metal atom (M).

Abstract: A liposome containing a regulatory cell ligand such as ?-galactosyl ceramide or ?-galactosyl ceramide is employed as the active ingredient of a drug for preventing or treating immune diseases etc.

Abstract: An automated synthesis device to produce Re-188-BMEDA solution including: a plurality of reagent vials, three-way solenoid valves, gel filtration columns and micro pumps, and a reaction vial, a product vial, a temporary storage vial, a filter membrane, and a waste vial, wherein the plurality of reagent vials include first reagent vial and second reagent vials being connected to the reaction vial through first micro pump, the third reagent vial and fourth reagent vial being connected to the reaction vial through second micro pump, fifth reagent vial being connected to the reaction vial through third micro pump, and sixth reagent vial being connected to the temporary storage vial through fourth micro pump, wherein the reaction vial is connected to the plurality of gel filtration columns through the micro-pump, respectively. The automated synthesis device is operable with program to upgrade yield and avoid contamination.

Abstract: The present invention relates generally to the field of prevention of diseases caused by enveloped viruses. More particularly, this invention concerns a composition for inactivating an enveloped virus comprising at least one non phospholipid Lipid Vesicle (nPLV) able to interact with said enveloped virus and an agent that enhances the lipid exchange between said nPLV and the membrane of said enveloped virus.

Abstract: The present invention provides an oligopeptidic compound comprising a PCNA interacting motif, or a nucleic acid molecule comprising a sequence encoding said oligopeptidic compound, for use in therapy, wherein the PCNA interacting motif is X1X2X3X3?X1?- (SEQ ID NO: 1), wherein X1 and X1?- are independently selected from the group of basic amino acids, X2 is a lipophilic amino acid and X3 and X3? are independently selected from the group of uncharged amino acids; and wherein the oligopeptidic compound is further characterized by at least one of the following: (i) the oligopeptidic compound comprises at least one signal sequence; (ii) the PCNA interacting motif is [K/R]-F-[L/I/V]-[L/I/V]-[K/R] (SEQ ID NO: 27). Particularly the therapy may be the treatment of a disorder or condition where it is desirable to inhibit the growth of cells, for example a hyperproliferative disorder, or a treatment which involves cytostatic therapy e.g., myeloablation.

Abstract: The present invention is related to a lipid composition comprising at least a first lipid component, at least a first helper lipid, and a shielding compound which is removable from the lipid composition under in vivo conditions.

Abstract: Disclosed are compositions that include anti-CD74 immunoconjugates and optionally a therapeutic and/or diagnostic agent. In preferred embodiments, the immunoconjugates comprise one or more anti-CD74 antibodies or antigen-binding fragments thereof, conjugated to a liposome or micelle. Also disclosed are methods for preparing the immunoconjugates and using the immunoconjugates in diagnostic and therapeutic procedures. In certain preferred embodiments, the therapeutic methods comprise administering to a subject with a CD74-expressing disease an anti-CD74 immunoconjugate and thereby inducing apoptosis of CD74-expressing cells. In more preferred embodiments, the CD74 immunoconjugate is capable of inducing cell death in the absence of any other therapeutic agent, although such agents may be optionally administered prior to, together with or subsequent to administration of the anti-CD74 immunoconjugate. The compositions may be part of a kit for administering the anti-CD74 immunoconjugates or compositions.

Abstract: Metal-bisphosphonate nanoparticles are disclosed. Also disclosed are pharmaceutical compositions including the metal-bisphosphonate nanoparticles, methods of preparing the metal-bisphosphonate nanoparticles and materials comprising the nanoparticles, and methods of using the compositions to treat cancer or bone-related disorders (e.g., bone-resorption-related diseases, osteoporosis, Paget's disease, and bone metastases) and as imaging agents.

Abstract: Delivery systems based on liposomes functionalized with peptides and chelating agents, for therapy and imaging by selective targeting of tumour cells expressing the receptors GRP, BB1, BB2, BB3 e BB4 and any other receptor which recognizes the bombesin peptide or analogues thereof are described. In particular, the liposomes contain within them cytotoxic drugs, such as for example doxorubicin, for target-selective antitumour therapy, and, through the presence of the chelating agent, can contain radioactive or paramagnetic ions for the real time visualization of the tumour cells. The liposomes described in this invention thus act as a selective delivery system for drugs and/or contrast agents onto tumour cells expressing the receptors for the class of known peptides such as bombesin (endogenous sequence, analogous or peptidomimetic peptides, agonists or non agonists).

Abstract: The invention relates to Cathepsin-binding compounds bound to a carrier comprising a diagnostic moiety, for use in the diagnosis of inflammatory diseases, and/or for use in the diagnosis of neoplastic diseases, wherein the Cathepsin-binding compound binds to inflammatory cells of the tumour stroma. The invention also relates to Cathepsin B-targeting compounds and Cathepsin B-binding and liposome-binding compounds.

Abstract: Compositions that facilitate the delivery of an active agent or an active agent carrier wherein the compositions are capable of penetrating the stratum corneum (SC) and/or the cellular membranes of viable cells are provided. In some embodiments, the compositions include a peptide, an active agent, and a carrier that includes the active agent, wherein the peptide has an amino acid sequence set forth in any of SEQ ID NOs: 1-18; the peptide is associated with and/or conjugated to the active agent, the carrier, or both; the carrier is selected from the group consisting of a micelle, a liposome, an ethosome, and combinations thereof; and the composition is capable of penetrating a stratum corneum (SC) layer when contacted therewith or penetrating a cell when contacted therewith, and optionally wherein the composition further includes one or more free peptides having an amino acid sequence set forth in any of SEQ ID NOs: 1-18.

Abstract: There is provided signal modifying compositions for medical imaging comprising a carrier and signal modifying agents specific for two or more imaging modalities. The compositions are characterized by retention efficiency, with respect of the signal modifying agents that enables prolonged contrast imaging without significant depletion of the signal modifying agent from the carrier. The carriers of the present invention are lipid based or polymer based the physico-chemical properties of which can be modified to entrap or chelate different signal modifying agents and mixtures thereof and to target specific organs or tumors or tissues within a mammal.

Abstract: The present invention is in the fields of drug delivery, cancer treatment and diagnosis and pharmaceuticals. This invention provides a method of making antibody- or antibody fragment-targeted immunoliposomes for the systemic delivery of molecules to treat and image diseases, including cancerous tumors. The invention also provides immunoliposomes and compositions, as well as methods of imaging various tissues. The liposome complexes are useful for encapsulation of imaging agents, for example, for use in magnetic resonance imaging. The specificity of the delivery system is derived from the targeting antibodies or antibody fragments.

Abstract: Compositions and methods for improved delivery of macromolecules into eukaryotic cells are provided. Fusogenic peptides from fusion proteins of non-enveloped viruses enhance the efficiency of transfection of eukaryotic cells mediated by transfection agents such as cationic lipids, polycationic polymers such as PEI and dendrimers. These fusogenic peptides are used as part of a transfection complex that efficiently delivers a macromolecule, for example, a nucleic acid, into a eukaryotic cell. Novel cationic lipids and compositions of cationic lipids also are provided that may be used for the introduction of macromolecules such as nucleic acids, proteins and peptides into a variety of cells and tissues. The lipids can be used alone, in combination with other lipids and/or in combination with fusogenic peptides to prepare transfection complexes.

Abstract: Guanylin cyclase C compound of the inventions are disclosed. Conjugated compounds comprising guanylin cyclase C compound of the inventions conjugated to detectable or therapeutic moieties are disclosed. Methods of detecting, imaging and treating cancer and treating diarrhea are disclosed.

Abstract: Provided are signal modifying compositions for medical imaging comprising a carrier and two or more signal modifying agents specific for two or more imaging modalities. The compositions are characterized by retention efficiency, with respect to the signal modifying agents, which enables prolonged contrast imaging without significant depletion of the signal modifying agents from the carrier. The carriers of the present invention are lipid based or polymer based, the physico-chemical properties of which can be modified to entrap or chelate different signal modifying agents and mixtures thereof and to target specific organs or tumors or tissues within a mammal.

Abstract: A vehicle composition in the form of a vesicular composition or a particular composition and, optionally, an active agent associated with the vesicle forming components or particles, and folate receptor alpha is used as a delivery system for the transport of components and/or active agents into the cerebrospinal fluid (CSF) and/or brain and/or central nervous system and/or spinal cord. The composition is used for treating of CSF or brain pertaining diseases, disorders or conditions, such as preventing or treating neurological or neurodegenerative diseases, disorders or conditions.

Abstract: The present invention includes a composition comprising at least one oleosin-like protein. The present invention also includes a composition comprising a vesicle comprising at least one oleosin-like protein.

Abstract: A device for large-scale lyophilization of pharmaceutical solutions in medical hollow bodies, includes a lyophilization device and at least one camera. Images of at least one pharmaceutical solution to be lyophilized are recorded by the at least one camera. The images may be used for controlling and/or monitoring the lyophilization process.

Abstract: A delivery system is provided. The delivery system includes a carrier or an active compound and a glutathione or a glutathione derivative grafted thereon. The invention also provides a compound including a moiety comprising a vitamin E derivative or a phospholipid derivative, a polyethylene glycol (PEG) or a polyethylene glycol derivative bonded thereto, and a glutathione (GSH) or a glutathione derivative bonded to the polyethylene glycol or the polyethylene glycol derivative.

Abstract: Methods are disclosed for producing defective ribosomal products (DRiPs) in blebs (DRibbles) by contacting cells with a proteasome inhibitor, and in some examples also an autophagy inducer, thereby producing treated cells. DRibbles can be used to load antigen presenting cells (APCs), thereby allowing the APCs to present the DRiPs and antigenic fragments thereof. Immunogenic compositions that include treated cells, isolated DRibbles, or DRibble-loaded APCs are also disclosed. Methods are also provided for using treated cells, isolated DRibbles, or DRibble-loaded APCs to stimulate an immune response, for example in a subject. For example, DRibbles obtained from a tumor cell can be used to stimulate an immune response against the same type of tumor cells in the subject. In another example, DRibbles obtained from a pathogen-infected cell or cell engineered to express one or more antigens of a pathogen can be used to stimulate an immune response against the pathogen in the subject.

Abstract: The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.

Abstract: The present invention describes the modification of polypeptides, more particularly channel proteins with a thiol reactive agent so as to introduce an azide group. The present invention further describes vesicles comprising channel proteins modified according to the invention, which upon reaction with a phosphine open up thereby releasing the content of the vesicles. The reagents, polypeptides and vesicles described in the present invention have in vivo and in vitro applications in both drug delivery and imaging.

Abstract: The present invention is in the fields of drug delivery, cancer treatment and diagnosis and pharmaceuticals. This invention provides a method of making antibody- or antibody fragment-targeted immunoliposomes for the systemic delivery of molecules to treat and image diseases, including cancerous tumors. The invention also provides immunoliposomes and compositions, as well as methods of imaging various tissues. The liposome complexes are useful for encapsulation of imaging agents, for example, for use in magnetic resonance imaging. The specificity of the delivery system is derived from the targeting antibodies or antibody fragments.

Abstract: Macrophages within the tumor microenvironment, also called tumor associated macrophages (TAMs) have been shown to play a major role in the growth and spread of many types of cancer. Cancer cells produce cytokines that cause the macrophages to differentiate into an M2 subtype. We have designed a mannosylated liposome (MAN-LIPs) and successfully showed it to accumulate in TAMs in a mouse model of pulmonary adenocarcinoma. These liposomes are loaded with 64Cu to allow tracking by PET imaging, and contain a fluorescent dye in the lipid bilayer permitting subsequent fluorescence microscopy. MAN-LIPs are a promising new vehicle for the delivery of imaging agents to lung TAMs. In addition to imaging, they hold the potential for delivery of therapeutic agents to the tumor microenvironment.

Abstract: Disclosed are nanoparticle compositions comprising paramagnetic particles, radiolabels, fluorophores, and/or positron emission tomography agents encapsulated within a biocompatible vehicle. In addition, methods of multi-modal diagnostic imaging and treating diseased tissues are disclosed, wherein the methods comprises administering a nanoparticle composition to a subject in which the nanoparticle composition comprises paramagnetic particles, radiolabels, fluorophores, and positron emission tomography agents encapsulated within a biocompatible vehicle.

Abstract: A delivery system. The delivery system includes a carrier or an active compound and a glutathione or a glutathione derivative grafted thereon. The invention also provides a compound including a moiety comprising a vitamin E derivative or a phospholipid derivative, a polyethylene glycol (PEG) or a polyethylene glycol derivative bonded thereto, and a glutathione (GSH) or a glutathione derivative bonded to the polyethylene glycol or the polyethylene glycol derivative.

Abstract: The present invention is directed to the technical field of imaging compositions useful for diagnosing cancer and other diseases in a subject. In particular, the invention relates to a class of diagnostic compounds comprising a novel liposome composition with encapsulated metal entities such as radionuclides, for example 61Cu and 64Cu copper isotopes. The invention further relates to a novel method for loading delivery systems, such as liposome compositions, with metal entities such as radionuclides, and the use of liposomes for targeted diagnosis and treatment of a target site, such as cancerous tissue and, in general, pathological conditions associated with leaky blood vessels. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

Abstract: Anionic non-phospholipids, as well as lipid nanostructures formed therefrom, are disclosed herein. Also disclosed are methods of producing and using same.

Abstract: The present invention relates to a radiation sensitive liposome, and the use of this liposome as carrier for therapeutic and diagnostic agent(s). In particular, the invention encompasses a liposomal delivery system, comprising a stable liposome-forming lipid and a polymerizable colipid, a fraction of which polymerizable colipid polymerizes upon exposure to ionizing radiation, thereby destabilizing the liposomal membrane. Destabilization of liposomes allows for leakage of liposomal contents. The present invention further contemplates methods of diagnosing and treating conditions and diseases that are responsive to liposome-encapsulated or associated agents.

Abstract: The present invention relates to a formulation of thermosensitive liposomes, and more specifically to a formulation of liposomes comprising phospholipids and a surface active agent, wherein the liposomes support long term storage at temperatures less than or equal to about 8° C., control degradate formation to maximize product potency and release their contents at mild hyperthermic temperatures. Methods of making formulations are also described.

Abstract: Compositions useful for target detection, imaging and treatment, as well as methods of production and use thereof, are disclosed herein.

Abstract: Certain embodiments disclosed herein include, but are not limited to, at least one of compositions, methods, devices, systems, kits, or products regarding rejuvenation or preservation of germ cells or gametes. Certain embodiments disclosed herein include, but are not limited to, methods of modifying germ cells or gametes, or methods of administering modified germ cells or gametes to at least one biological tissue.

Abstract: Disclosed are compositions that include anti-CD74 immunoconjugates and a therapeutic and/or diagnostic agent. Also disclosed are methods for preparing the immunoconjugates and using the immunoconjugates in diagnostic and therapeutic procedures. The compositions may be part of a kit for administering the anti-CD74 immunoconjugate compositions in therapeutic and/or diagnostic methods.

Abstract: Disclosed are compositions that include anti-CD74 immunoconjugates and optionally a therapeutic and/or diagnostic agent. In preferred embodiments, the immunoconjugates comprise one or more anti-CD74 antibodies or antigen-binding fragments thereof, conjugated to a liposome or micelle. Also disclosed are methods for preparing the immunoconjugates and using the immunoconjugates in diagnostic and therapeutic procedures. In certain preferred embodiments, the therapeutic methods comprise administering to a subject with a CD74-expressing disease an anti-CD74 immunoconjugate and thereby inducing apoptosis of CD74-expressing cells. In more preferred embodiments, the CD74 immunoconjugate is capable of inducing cell death in the absence of any other therapeutic agent, although such agents may be optionally administered prior to, together with or subsequent to administration of the anti-CD74 immunoconjugate. The compositions may be part of a kit for administering the anti-CD74 immunoconjugates or compositions.

Abstract: A method of formulating insulin compositions comprises preparing a carrier having a phosphatidylcholine component which entraps insulin, stabilizing insulin compositions at room temperatures.

Abstract: The invention described herein pertains to folate-receptor targeted agents comprising therapeutic agents useful for the treatment of inflammatory disease, including folate-receptor targeted liposomes (folate-targeted liposomes) containing entrapped therapeutic agents and folate-receptor targeted dendrimers conjugated to therapeutic agents (folate-targeted dendrimer conjugates), useful for the treatment of inflammatory disease, including auto-immune disease, as well as to folate-targeted liposomes containing entrapped imaging agents and dendrimer conjugates conjugated to imaging agents, for use in the diagnosis and monitoring of treatment in such disease.

Abstract: Disclosed are compositions that include anti-CD74 immunoconjugates and optionally a therapeutic and/or diagnostic agent. In preferred embodiments, the immunoconjugates comprise one or more anti-CD74 antibodies or antigen-binding fragments thereof, conjugated to a liposome or micelle. Also disclosed are methods for preparing the immunoconjugates and using the immunoconjugates in diagnostic and therapeutic procedures. In certain preferred embodiments, the therapeutic methods comprise administering to a subject with a CD74-expressing disease an anti-CD74 immunoconjugate and thereby inducing apoptosis of CD74-expressing cells. In more preferred embodiments, the CD74 immunoconjugate is capable of inducing cell death in the absence of any other therapeutic agent, although such agents may be optionally administered prior to, together with or subsequent to administration of the anti-CD74 immunoconjugate. The compositions may be part of a kit for administering the anti-CD74 immunoconjugates or compositions.

Abstract: An engineered lipoprotein including (a) a core particle or a plurality of core particles, each core particle has (i) an inner part comprising a hydrophilic active agent and a hydrophilic portion of an amphiphilic cholesterol and (ii) an outer part including a hydrophobic portion of the amphiphilic cholesterol, (b) a layer surrounding the core particle or a plurality of core particles, the layer includes a phospholipid, (c) an apoprotein associated with the layer, and optionally, (d) a homing molecule associated with at least one of the apoprotein or the phospholipid.

Abstract: Disclosed are compositions that include anti-CD74 immunoconjugates and a therapeutic and/or diagnostic agent. Also disclosed are methods for preparing the immunoconjugates and using the immunoconjugates in diagnostic and therapeutic procedures. The compositions may be part of a kit for administering the anti-CD74 immunoconjugate compositions in therapeutic and/or diagnostic methods.