Abstract: The present invention relates to targeted delivery systems for delivering therapeutic agents to tumor. The invention further relates to methods of delivering a therapeutic agent to a tumor for the prevention and treatment of cancer by killing tumor cells and tumor-associated endothelial cells. In particular, the present invention provides a tumor-targeted drug delivery system comprising a NGR-containing molecule linked to a delivery vehicle encapsulating a therapeutic agent, preferably a drug, such as a cytotoxic agent or a chemotherapeutic agent. Specifically, the delivery systems of the present invention are capable of delivering an increased amount of therapeutic agent to a tumor as compared to other delivery systems.

Abstract: The present invention relates to targeted delivery systems for delivering therapeutic agents to tumor. The invention further relates to methods of delivering a therapeutic agent to a tumor for the prevention and treatment of cancer by killing tumor cells and tumor-associated endothelial cells. In particular, the present invention provides a tumor-targeted drug delivery system comprising a NGR-containing molecule linked to a delivery vehicle encapsulating a therapeutic agent, preferably a drug, such as a cytotoxic agent or a chemotherapeutic agent. Specifically, the delivery systems of the present invention are capable of delivering an increased amount of therapeutic agent to a tumor as compared to other delivery systems.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: A liposomal composition and a method of using the same for achieving intracellular delivery of a liposome-entrapped agent is described. The liposomes are composed of a pH sensitive lipid and include a targeting ligand to direct the liposomes to a target cell. The liposomes also include a stabilizing component, such a polymer-derivatized lipid, where the polymer is attached to the lipid by a releasable linkage. Administration of the liposomes results in cellular internalization and destabilization of the liposome for intracellular delivery of the entrapped agent.

Abstract: The present invention relates to targeted delivery systems for delivering therapeutic agents to tumor. The invention further relates to methods of delivering a therapeutic agent to a tumor for the prevention and treatment of cancer by killing tumor cells and tumor-associated endothelial cells. In particular, the present invention provides a tumor-targeted drug delivery system comprising a NGR-containing molecule linked to a delivery vehicle encapsulating a therapeutic agent, preferably a drug, such as a cytotoxic agent or a chemotherapeutic agent. Specifically, the delivery systems of the present invention are capable of delivering an increased amount of therapeutic agent to a tumor as compared to other delivery systems.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: A liposomal composition and a method of using the same for achieving intracellular delivery of a liposome-entrapped agent is described. The liposomes are composed of a pH sensitive lipid and include a targeting ligand to direct the liposomes to a target cell. The liposomes also include a stabilizing component, such a polymer-derivatized lipid, where the polymer is attached to the lipid by a releasable linkage. Administration of the liposomes results in cellular internalization and destabilization of the liposome for intracellular delivery of the entrapped agent.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: A liposome composition for administration of a polynucleotide and a method of preparing the composition are described. The liposomes in the suspension are composed predominantly of liposomes having a bilayer membrane formed of cationic vesicle-forming lipids and neutral vesicle forming lipids. The polynucleotide is entrapped in the central core of the liposomes and is localized predominantly on the inner surface of the core.

Abstract: Reagents for use in preparing a therapeutic liposome composition sensitized to a target cell are described. The reagents include a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent and a plurality of targeting conjugates composed of a lipid, a hydrophilic polymer and a targeting ligand. The therapeutic, target-cell sensitized liposome composition is formed by incubating the liposomal composition with a selected conjugate.

Abstract: Steroid compounds of the contignasterol family, including stereoisomers and pharmaceutically acceptable salts, as well as compositions containing these materials and a pharmaceutically acceptable carrier, are disclosed. The steroid compounds have a 3.alpha.-hydroxyl, a 4.beta.-hydroxyl, a 6.alpha.-hydroxyl, a 7.beta.-hydroxyl, a 15-ketone, a trans A/B ring juncture and a cis or trans C/D ring juncture. The compounds and compositions may be used, for example, for the prevention of inflammatory or allergic reactions, or the treatment of cardiovascular or haemodynamic disorders.

Abstract: A method of treating a subject having a disorder characterized by a neoplasm of B-lymphocyte or T-lymphocyte lineage cells is described. The method includes administering a suspension of liposomes having a surface coating of polyethylene glycol chains. Attached to the distal ends of the chains are antibodies or antibody fragments effective to bind to an antigen specific to the affected cells. In one embodiment, anti-CD19 antibodies are attached to the liposome-bound chains, for treatment of multiple myeloma.

Abstract: A method of administering an anti-tumor compound to a subject is disclosed. The method includes administering to a subject liposomes having sizes predominantly in the range 0.05 to 0.12 microns, and containing an anti-tumor compound in liposome-entrapped form, a surface coating of polyethylene glycol chains, at a surface concentration thereof sufficient to extend the blood circulation time of the liposomes severalfold over that of liposomes in the absence of such coating, and surface-attached antibody molecules effective to bind specifically to tumor-associated antigens present at the tumor site. One liposome composition includes doxorubicin in entrapped form, and, on the liposome surface, a monoclonal antibody against highly proliferating cells in a lung squamous cell carcinoma.

Abstract: The invention presents compounds useful for the prevention of inflammatory or allergic reaction or the treatment of cardiovascular or haemodynamic disorders having the formula: ##STR1## where R= ##STR2## where R= ##STR3## or pharmaceutically acceptable acids or salts thereof.

Abstract: 5-Methylimidazo[4,5-e]-1,2-thiazin-4(5-H)-one, having the structure ##STR1## a cytotoxic metabolite of the marine sponge Neamphius huxleyi, has been isolated from the sponge by extraction and chromatography.

Abstract: A composition of liposomes which contain an entrapped pharmaceutical agent and are characterized by (a) liposome sizes predominantly between about 0.07 and 0.5 microns; (b) at least about 50 mole percent of a membrane-rigidifying lipid, such as sphingomyelin or neutral phospholipids with predominantly saturated acyl chains; and (c) between about 5-20 mole percent of a glycolipid selected from the group consisting of ganglioside GM.sub.1, saturated phosphatidylinositol, and monogalactosyl stearate. The liposomes show high blood/RES tissue distribution ratios, and are effective for drug administration to tumors via intravenous drug delivery.

Abstract: A composition of liposomes which contain an entrapped pharmaceutical agent and are characterized by: (a) liposome sizes predominantly between about 0.08 and 0.5 microns: (b) at least about 50 mole percent of a membrane-rigidifying component, such as sphingomyelin or neutral phospholipids with predominantly saturated acyl chains: and (c) between about 5-15 mole percent ganglioside G.sub.M1. The liposomes show a blood/RES tissue distribution ratio, two hours after intravenous administration, which is substantially greater than the sum of the distribution ratios observed with similarly constructed liposome compositions containing the membrane-rigidifying agent alone and gangliosides alone. Also disclosed are methods for enhancing the blood/RES ratio of intravenously administered liposomes, and for assessing the effect of selected liposome components on in vivo uptake of liposomes by cells of the reticuloendothelial system (RES).