Abstract: The present invention relates to liposome formulations that are physically stable. In particular the present invention relates to steric stabilization of cationic liposomes by incorporating glycolipids into the liposomes. The stabilized liposomes can be used either as an adjuvant for antigenic components or as a drug delivery system. In particular the invention relates to vaccines with adjuvants in aqueous media for immunization, where the final product is stable.

Abstract: The invention relates to membrane vesicles from non-pathogenic amoeba, in particular from the amoeba Dictyostelium discoideum, containing a molecule of therapeutic interest, to a method of preparing such vesicles and to the use of said vesicles as a vehicle for transferring the molecule therapeutic interest to an eukaryotic mammalian cell.

Abstract: The invention, in one aspect, relates to radiolabeled compounds. The invention also relates to radiolabeled liposomes and methods of making and using thereof. The invention also relates to kits for preparing radiolabeled liposomes.

Abstract: Tumor targeting peptides and uses thereof in tumor diagnosis and treatment.

Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.

Abstract: Stabilized lipid construct comprising a liposome or polymerized vesicle, a targeting entity, a therapeutic entity, and a stabilizing entity are provided, as well as methods for their preparation and use.

Abstract: Sterically stabilized cationic liposomes (SSCL) encapsulating a K type oligodeoxynucleotide (ODN) including a CpG motif are disclosed. These SSCL encapuslating a K type ODN can be used to effectively deliver the ODN to a cell. A novel method is also disclosed for producing the SSCL encapsulating the K type ODN. Administration of the SSCL encapsulating a K type ODN and a chemotherapeutic agent, such as a chimeric molecule comprising a targeting molecule selected from the group consisting of an IL-13, and an anti-IL-13 receptor antibody; and an effector molecule selected from the group consisting of a Pseudomonas exotoxin, a Diphtheria toxin, and a radionuclide, can be used to dramatically reduce the growth of solid tumors.

Abstract: A delivery system. The delivery system includes a carrier having a surface, an active compound comprising small molecule compounds or peptides for use as an analgesic encapsulated into the carrier, and a glutathione or a glutathione derivative grafted on the surface of the carrier. The invention also provides a method of analgesia including conducting the active compound to a subject.

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: Vaccines directed against antigens such as membrane proteins from pathogens or tumor cells are disclosed. Also described are methods of forming reconstituted viral membranes, with membrane fusion activity, which are lipid bilayer membranes preferably containing natural lipids of a virus, a viral fusion protein, one or more optional further antigens as well as amphiphilic adjuvants. Pharmaceutical compositions including such reconstituted viral membranes are also described.

Abstract: The invention provides a method for a multi-layered lipid particles in the form of liposomes that are coated first with a cryoprotectant followed by a targeting moiety over the coat of cryoprotectant, and a method for encapsulating drugs and agents in the multi-layered coated liposomes. In addition, ready-to-use liposome kits for coating with targeting agent of choice and for drug and/or agent encapsulation.

Abstract: The present invention refers to the use of cationic liposomal preparations for the treatment or diagnosis of rheumatoid arthritis or related disorders.

Abstract: The invention concerns a block copolymer of polyethylene oxide and polycaprolactone, the polyethylene oxide having a number average molecular weight from about 2.0 to about 3.8 kD, the block copolymer having a fraction of polyethylene oxide of from about 11.8 to 18.8 percent by weight. The invention also concerns polymersomes made from such copolymers and to methods of making the polymersomes.

Abstract: A fluorescent phospholipase assay is disclosed. Further disclosed are the identification of alpha-1-antitrypsin as a phospholipase A2 stimulator and phospholipase C inhibitor and the identification of mercaptalbumin as a phospholipase A2 inhibitor. Various applications involving the use of the phospholipase assay, alpha-1-antitrypsin and mercaptalbumin are also disclosed.

Abstract: A detection agent, including a polymerized liposome, a lectin, and an imaging agent, can be administered to an animal for the detection of polyps in the lower gastrointestinal tract.

Abstract: The combined use of a TGF-? signaling inhibitor and an antitumor active substance or an imaging agent modified by a drug-encapsulating macromolecular micelle, or the like, is provided. The selective delivery capability of the antitumor active substance or the imaging agent to the target is improved, increasing the antitumoral activity in the target.

Abstract: An immunoliposome composition targeted to the alphaV-integrin subunit of integrin receptors comprised of ligand-targeted liposomes bearing at least one targeting-ligand derived from an antibody and having binding specificity for at least one integrin receptor comprising an alpha V subunit including ?v?1, ?v?3 ?v?5, ?v?6, or ?v?8 integrin cell receptors is described. The antibody-derived targeting ligand may be a Fab? fragment, a scFv, or the like. Binding of the immunoliposome to ?v-integrin expressing cells, preferably results in internalization of the immunoliposome for cytoplasmic delivery of a liposome-entrapped agent.

Abstract: A compound represented by the following general formula (I): wherein R1 and R2 represent an alkyl group or alkenyl group; X1 and X2 represent —O—, or —N(Z)-; Z represents hydrogen atom, or an alkyl group; L represents a divalent bridging group comprising an alkylene group, an alkenylene group, —CO—, —O— and the like wherein number of atoms constituting a chain length of the bridging group is 1 to 10; and Ch represents a partial structure containing 3 or more nitrogen atoms and capable of forming a chelate, and a chelate compound comprising the compound are provided. A vascular lesion can be selectively contrasted by MRI or scintigraphy imaging using a contrast medium comprising liposomes containing said compound or said chelate.

Abstract: Hepatocellular carcinoma (HCC) is the fourth leading cause of cancer death worldwide. Novel treatment strategies derived from increased knowledge of molecular oncology are constantly being developed to cure this disease. Here, we used phage display to identify novel peptides, including (SP94), which binds specifically to HCC cells. In vitro, the phage clone PC94 binds to HCC cell lines. In vivo, PC94 homed specifically to tumor tissues but not to normal visceral organs in SCID mice bearing human HCC xenografts. The homing ability could be competitively inhibited by synthetic peptide, SP94. PC94 localized to tumor tissues but could not be detected in SP94-competed tumor tissues or in normal organs. In addition, PC94 recognized the tumor tissue but not non-tumor tissue in surgical specimens from HCC patients, with a positive rate of 61.3% (19/31).

Abstract: The invention relates to supramolecular aggregates obtained by coaggregation of two monomers: —a first monomer containing a paramagnetic or radioactive metal ion complexed by a chelating agent having a lipophilic moiety, —a second monomer containing a bioactive peptide linked to a lipophilic moiety through an organic spacer. The aggregates are selectively driven by the exposed bioactive peptide on a desired biological target. The aggregates (micelles, vesicles or liposomes) could entrap on their inner region or on their surface a pharmaceutical active principle (drug). The invention thus relates to target specific delivery of drugs and/or metal ions. The invention therefore provides compositions containing said aggregates for use as contrast agents, in nuclear medicine or MRI, for the selective delivery of drugs, and for simultaneous delivery of a drug and a metal ion.

Abstract: A liposome contains an active agent and has a gel-phase lipid bilayer membrane comprising phospholipid and a surface active agent. The phospholipids are the primary lipid source for the lipid bilayer membrane and the surface active agent is contained in the bilayer membrane in an amount sufficient to increase the percentage of active agent released at the phase transition temperature of the lipid bilayer, compared to that which would occur in the absence of the surface active agent. The surface active agent is present in the lipid bilayer membrane so as to not destabilize the membrane in the gel phase.

Abstract: The invention relates to liposome compositions for delivering, for example, therapeutic, diagnostic, and imaging agents to a subject. Methods for preparing and using such liposome compositions are further provided. The compositions and methods of the invention find particular use in treating, diagnosing, and imaging a tumor in a subject.

Abstract: The present invention relates to the treatment of cancer with compounds that inhibit the activity of endo-exonuclease. Endo-exonuclease has been shown to be necessary for the repair of damaged DNA. Compounds that inhibit the activity of endo-exonuclease have been shown to be particularly effective for treating cancer when used in combination with drugs that induce DNA breaks such as cisplatin and mitomycin C. These compounds have a synergistic effect when used in combination for inhibiting tumour growth. The invention includes pharmaceutical compositions for inhibiting tumour growth comprising a compound that inhibits endo-exonuclease activity. These pharmaceutical compositions preferably include compounds that induce DNA breaks. The invention includes methods of treating cancer with these pharmaceutical compositions and uses of these compositions to treat cancer. The preferred compounds that inhibit the activity of endo-exonuclease have low toxicity. One such compound is pentamidine.

Abstract: An oil-in-water propofol emulsion that contains soybean oil and egg lecithin, which provide a source of nutrition for microorganisms. Current products include additives to act as a microbial growth retardation agent, the processes described herein detail several methods for the optimization of the innate microbial retardation capability of propofol. Using this process improves the safety of a propofol emulsion solution by controlling microbial growth without the side effects associated with growth retardation additives.

Abstract: An improved linker which lacks chiral centers between a hydrophobic anchor for coupling to lipid-based particles and a targeting agent has suitable hydrophobic/hydrophilic properties for use in vivo.

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: This invention is to manufacture a kit for preparation of nano-targeted liposome drugs in combined chemotherapy and radionuclide therapy. It is a kit consisting of three components: (1) A 10 ml vial A which contains BMEDA, gluconate acetate, SnCl2. (2) A 10 ml vial B which contains DSPC, cholesterol, DSPE-PEG, and Doxorubicin(DXR) (or Daunorubicin, Vinolbine). (3) A 10 ml vial C which contains 188ReO4? (or 186ReO4?) solution. The procedure of using the kit is as follows: (1) Remove the contents of the 188ReO4? (or 186ReO4?) solution from vial C. (2) Inject the 188ReO4? (or 186ReO4?) solution into the vial A, and the mixtures react in appropriate temperature. (3) Remove the contents of the 188Re-BMEDA (or 186Re-BMEDA) solution from vial A. (4) Inject the 188Re-BMEDA (or 186Re-BMEDA) solution into the vial B, and the mixtures react in appropriate temperature. The reconstituted solution in the vial B is applied to combine bimodality radiochemotherapy for treatment of tumor and ascites.

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: The present invention relates to cytotoxic agents comprising liposomes wherein the liposomes enclose a solution comprising at least one alpha emitting radionuclide and at least one other therapeutic agent, particularly a chemotherapeutic. The invention also provides methods for the formation of such cytotoxic agents, methods of therapy, especially cancer therapy employing the agents and methods for their use in the manufacture of medicaments.

Abstract: The invention provides nucleic acids, peptides, and antibodies for use in applications including diagnosis and therapy. The peptides target lung cancer and were identified by phage display. Targeting phage PC5-2 and synthetic peptide SP5-2 were both able to recognize human pulmonary tumor specimens from lung cancer patients. In SCID mice bearing NSCLC xenografts, the targeting phage was able to target tumor masses specifically. When the peptide was coupled to liposomes containing the anti-cancer drugs vinorelbine or doxorubicin, the efficacy of these drugs against human lung cancer xenografts was improved, the survival rate increased, and the drug toxicity was reduced.

Abstract: Compounds useful for associating with nanoparticle or microparticle emulsions to obtain magnetic resonance images permit control of the relaxivity of the signal and readily associate with the particulate components.

Abstract: The invention relates to a pharmaceutically active substance for producing a drug that is capable of generating thrombin or that contains thrombin and compositions comprising thereof. The pharmaceutically active substance contains (A) prothrombin (coagulation factor II) obtained from plasma or by genetic engineering, (B) coagulation factors V, VIII, IX, X obtained from plasma or by genetic engineering that at least partially may be present in their activated state, and coagulation factor XIa obtained from plasma or by genetic engineering, and (C) prion-safe, coagulation-promoting phospholipids, where the phospholipids are optionally contained in liposomes.

Abstract: A compound represented by the following general formula (IA) or a salt thereof: wherein Ar1 represents hydrogen atom or an aryl group having at least one iodine atom as a substituent; Ar2 represents an aryl group having at least one iodine atom as a substituent; L1 and L2 independently represent a divalent bridging group of which main chain contains 6 or more carbon atoms; L3 represents a single bond or a divalent bridging group of which main chain contains 1 to 6 carbon atoms and one oxygen atom; X represents a functional group containing at least one heteroatom, provided that, when L3 is a single bond, X represents a functional group other than hydroxyl group. The compound can be used as a membrane component of liposomes, and the liposomes can be used as a contrast medium for X-ray radiography.

Abstract: Disclosed is a new structural class of amphiphilic molecules which incorporate a hydrophilic material or polymer attached, at spatially distinct sites, to at least two hydrophobic residues. Certain of the amphiphilic molecules comprise a plurality of hydrophobic moieties. All such amphiphilic molecules have a common structural motif and, in contact with water, display surface activity and self-assemble into multimolecular aggregates and liquid crystalline phases. Also disclosed are enhanced stability liposomes that incorporate such amphiphilic molecules via unique interactions, and methods of using such formulations in a variety of applications including drug delivery, nutrition, bio-diagnostics, cosmetics, blood products and related applications.

Abstract: An object of the present invention is to provide a method of producing liposome wherein a complex of a short half-life metallic radioactive nuclide such as 99mTc and CD is encapsulated, with radiochemical yield and purity enabling practical application. The present invention provides a method of producing a liposome wherein a complex of a short half-life metallic radioactive nuclide and ethylenedicysteine (CD) is encapsulated, which comprises mixing a complex of a short half-life metallic radioactive nuclide and N-[2-(1H-pyrrolylmethyl)]-N?-(4-penten-3-on-2)-ethane-1,2-diamine with an ethylenedicysteine (CD)-encapsulated liposome, and incubating the mixture.

Abstract: The present invention provides a method of inhibiting growth of lung metastases in an individual comprising the steps of administering a dose of a lipid-drug enhancer liposomal complex and, in sequence, administering a dose of a lipid-anticancer drug liposomal complex. Furthermore, the lipid-drug enhancer liposomal complex may be administered in a continuing dose with the lipid-anticancer drug liposomal complex whereby both liposomal complexes are mixed in the nebulizer. Methods of inhibiting growth of lung metastases in an individual by the sequential administration via aerosolization of a dilauroylphosphatidylcholine-cyclosporin A liposomal complex and a dilauroylphosphatidylcholine-paclitaxel liposomal complex are also provided.

Abstract: The present invention relates to nanoparticle vaccines comprised of a carrier, particularly polymerized lipids, having multiple copies of an antigen or combinations of different antigens displayed on the carrier. Such antigen-displaying nanoparticles may also display a targeting molecule on its surface in order to direct it to a specific site or cell type to optimize a desired immune response. The present invention also relates to encapsulating an antigen or combinations of different antigens within such nanoparticles, with or without a targeting molecule displayed on its surface. The antigens used in this invention are effective to produce an immune response against a variety of pathological conditions.

Abstract: Polyhydroxy phenols, which are non-peptidic mimetics of galloyl peptides, and a process for the preparation of gallic acid derivatives using a gallic-acid providing moiety are provided as well as polyhydroxy phenol-containing pharmaceutical and nutraceutical compositions. The use of polyhydroxy phenols as a medicament and especially for the manufacture of a medicament for the prevention, treatment or diagnosis of a disease or a condition, wherein P-selectin is involved, is provided. The same compounds can also be used as targeting tools to P-selectin expressing cells or tissues in a composition, further comprising an active compound in a vehicle.

Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein Ar1 and Ar2 independently represent a substituted or unsubstituted aryl group having at least one iodine atom as a substituent; L1 and L2 independently represent a divalent bridging group of which main chain consists of 7 or more atoms at least one of which is a heteroatom; and X represents —CH(OH)— or —CO—, which is suitable for an iodine-containing contrast medium containing liposomes.

Abstract: The present invention provides biocompatible vesicles comprising semi-permeable, thin-walled encapsulating membranes which are formed in an aqueous solution, and which comprise one or more synthetic super-amphiphilic molecules. When at least one super-amphiphile molecule is a block copolymer, the resulting synthetic vesicle is termed a “polymersome.” The synthetic, reactive nature of the amphiphilic composition enables extensive, covalent cross-linking of the membrane, while maintaining semi-permeability. Cross-linking of the polymer building-block components provides mechanical control and long-term stability to the vesicle, thereby also providing a means of controlling the encapsulation or release of materials from the vesicle by modifying the composition of the membrane. Thus, the encapsulating membranes of the present invention are particularly suited for the reliable, durable and controlled transport, delivery and storage of materials.

Abstract: The invention relates to a structured mixed phase formed by the incorporation of a biological macromolecule into a liquid-crystal phase of amphiphiles, preferably a lamellar phase, wherein said biological macromolecule is present in said structured mixed phase in an amount of at least 5% by weight, based on the amphiphilic compounds constituting said liquid-crystal phase of amphiphiles, and wherein at least one of the two entities consisting of the biological macromolecules, on the one hand, and all the amphiphilic compounds, on the other, is of an uncharged nature. The biological macromolecules incorporated into the structured mixed phases of the invention are preferably selected from polynucleotides, particularly DNA or RNA, proteins and polysaccharides. The invention further relates to vesicles obtained by dispersion of the above structured mixed phases.

Abstract: A skin treatment composition comprising a Mahonia aquifolium extract in a liposome delivery system. The Mahonia aquifolium extract is present in the skin treatment composition in a range of from 5% to 20% by weight of the total composition. The skin treatment composition is particularly effective in the treatment of psoriasis, eczema and other dry skin conditions. The invention further provides a process for obtaining an extract of Mahonia aquifolium.

Abstract: The present invention is directed to a lipid-based delivery system for administration of an active drug substance selected from lysolipid derivatives which are particularly useful in the treatment or detection of parasitic infections, especially parasitic infections which cause an elevated PLA2 level in the infected mammal. Preferred parasitic infections are infections wherein the life cycle of the parasite involves the liver and/or spleen of the infected organism.

Abstract: The present invention provides a pharmaceutical composition, comprising: (a) cationic lipids, wherein said lipids are a liposomal mixture of a diacyl-ethyl-phosphocholine and 1,2-diacyl-sn-glycero-3-phosphoethanolamine; and (b) a plasmid cDNA sequence encoding a protein having tumor suppressor or pro-apoptotic activity. This composition has a high gene transfection efficiency at non-toxic doses and is designed to transfect human bronchial premalignant lesions and early endo-bronchial malignancies.

Abstract: Angiogenic endothelial cells are selectively targeted with lipid/DNA complexes or cationic liposomes containing a substance which affects the targeted cells by inhibiting or promoting their growth. A site of angiogenesis can be precisely located by administering cationic liposomes containing a detectable label. The complexes may comprise nucleotide constructs which are comprised of promoters which are selectively and exclusively activated in the environment of an angiogenic endothelial cell.

Abstract: A pharmaceutical composition for boron neutron capture therapy (BNCT), and in particular for BNCT on hepatoma is disclosed. The pharmaceutical composition contains a therapeutically effective amount of triphenylboroxin (phenylboronic anhydride) as a boron source and a pharmaceutically acceptable carrier, such as lipiodol.

Abstract: The present invention provides a sugar-modified liposome having a sugar chain bonded to its membrane surface, preferably through a linker protein, and having excellent absorption qualities, particularly in the intestine. The molecular structure and quantity of the sugar chain is selectively varied to allow the liposome to be delivered in a targeted manner to selected cells and tissues. The liposome is applicable to medicinal drugs, cosmetics and other various products in the medical/pharmaceutical fields, and it is especially useful in a therapeutic drug delivery system that recognizes target cells and tissues, such as cancer cells, and in the delivery of drugs or genes locally to a selected region, or in a diagnostic cell/tissue sensing probe.

Abstract: A liposome including a fusogenic liposome, a linking moiety and a targeting moiety. The fusogenic liposome is a lipid bilayer encapsulating contents. The linking moiety is electrostatically bound to the lipid bilayer, and the targeting moiety is covalently bound to the linking moiety. The liposome may also include a stabilizing moiety interposed between the linking and targeting moieties, and covalently bound to both. Alternatively, the stabilizing and targeting moieties may be covalently bound to separate linking moieties, the linking moieties being electrostatically bound to the lipid bilayer.

Abstract: This invention features in vitro methods of determining the rate and extent to which test compounds, such as drug candidates, enter, move within, and traverse lipid-associated barriers. This invention also features method that measure the accumulation, that is the partition coefficient, of test compounds in lipid structures relative to, e.g., an aqueous phase, as well as the rate of accumulation of test compounds in the lipid structures. In addition, the invention features lipid vesicles that contain fluorophores localized within the aqueous interior that can be employed in the methods described herein.

Abstract: The present invention provides a method of increasing the deposition of aerosolized drug in the respiratory tract of an individual or animal, comprising the step of administering said aerosolized drug in an air mixture containing up to about 10% carbon dioxide gas.