Abstract: Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula where R1 is diaminocycloalkyl, and R2 and R3 each have the formula where R4, R5, and R6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having the formula R1—Pt—X2??(II) where X is halogen.

Abstract: Pharmaceutical compositions and methods of using them. Lipid formulations of a glutathione analog and methods of manufacturing them. Their use to stimulate hematopoiesis, protect hematopoietic cells from damage caused by radiation or chemotherapy, or potentiate the stimulatory action of one or a combination of cytokines on colony formation by hematopoietic progenitor cells, protect a subject from a destructive effect of a chemotherapeutic agent or irradiation, or to potentiate the effect of a chemotherapeutic agent.

Abstract: Liposomes containing lipophilic active ingredient are produced by dehydrating a mixture of liposomes, lipophilic active ingredient and sugar, usually followed by a rehydration step to form dehydration-rehydration vesicles. The lipophilic drug is suitably paclitaxel. The sugar is usually sucrose. The liposome forming compounds preferably include cholesterol and phosphatidylcholine, and optionally an anionic lipid. The ratio of sugar:lipid is preferably at least 5:1 w/w. The ratio of lipid:drug is preferably (up to 10):1 w/w.

Abstract: A pharmaceutical composition containing macrolide, e.g. a rapamycin compound in an emulsion preconcentrate or microemulsion preconcentrate for oral administration. The carrier medium for the rapamycin compound includes a hydrophilic phase, a lipophilic phase and a surfactant. The composition is stable and provides high absorption efficiency.

Abstract: New compositions formed from the combination of an active substance with a hydrogel carrier moiety are provided. The compositions are suitable for use in high-velocity transdermal particle injection techniques. Methods of providing the new compositions are also provided. In addition, methods for administering pharmacologically active agent to a subject are provided. These methods are useful for delivering drugs, biopharmaceuticals, vaccines and diagnostics agents.

Abstract: A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is packaged in one vial with a sufficient amount of solvent comprising anhydrous ethanol and a suitable nonionic surfactant in a second vial. All steps are carried out with protection from light. In use, the contents of the second or diluent vial are added to the lyophilized product and mixed to constitute the epothilone analog and the resulting solution is diluted with a suitable diluent to produce a solution for intravenous injection containing the epothilone analog in a concentration of from about 0.1 mg/mL to about 0.9 mg/mL. A preferred surfactant is polyethoxylated castor oil and a preferred diluent is Lactated Ringer's Injection.

Abstract: Nonalcoholic steatohepatitis (NASH) is a disease of the liver characterized by inflammation and damage to the liver cells. Typically, steatohepatitis involves inflammation of the liver related to fat accumulation, and mimics alcoholic hepatitis but is observed in patients who seldom or never consume alcohol. Nonalcoholic steatohepatitis can lead to serious liver damage, and ultimately cirrhosis. The present invention provides methods and compositions useful for the treatment or alleviation of nonalcoholic steatohepatitis and the pharmaceutical formulations for their administration to a human. Specifically, compositions comprised of lecithin, antioxidants and vitamin B complex are administered parenterally, most preferably by oral administration. Specific therapeutic formulations include admixtures of these compounds and specific dosage formulations include daily oral administrations of these compounds in tablet or powder forms.

Abstract: The present invention is directed to a formulation comprising a lipid-regulating agent dissolved in at least one structured lipid as the primary solvent medium for said agent. One or more emulsifiers may be added to the formulation.

Abstract: Liposomes encapsulating a ?-glucan have an improved activity of enhancing a cellular immunity, especially when they are transmucosally administered. Thus, the liposomes are useful for the treatment or prevention of infection or tumor.

Abstract: A description is given of the use of a nanodispersion, which comprises (a) a membrane-forming molecule, (b) a coemulsifier and (c) a lipophilic component, in cosmetic end formulation, which nanodispersion is obtainable by (?) mixing the components (a), (b) and (c) until a homogeneous clear liquid is obtained, and (?) adding the liquid obtained in step (?) to the water phase of the cosmetic end formulations, steps (?) and (?) being carried out without any additional supply of energy. The nanodispersions used according to this invention can be easily prepared and are suitable as carrier systems for a very wide range of cosmetic active agents and oil-soluble dyes.

Abstract: The present invention is directed to bone replacement devices and compositions containing a synthetic, bioabsorbable, biocompatible liquid polymer that is the reaction product of a polybasic acid or derivative thereof, a polyol and a fatty acid, the liquid polymer having a melting point less than about 40° C., as determined by differential scanning calorimetry.

Abstract: Polymeric drug formulations containing a non-releasing single-phase dispersion of a water-soluble drug in a water-insoluble tissue-compatible polymer matrix. Polymeric drug formulations are also disclosed containing a single-phase dispersion of a water-soluble drug and a water-insoluble tissue-compatible polymer matrix, and a second, phase-disrupting polymer that is non-miscible with the tissue-compatible polymer and is present in an amount sufficient to form phase-separated microdomains of the second polymer in the tissue-compatible polymer matrix, so that the release rate of the water-soluble drug from the tissue-compatible polymer matrix is related to the amount of the second polymer. Methods of preparing the polymeric drug formulations are also described, as well as methods for site-specific drug delivery utilizing the polymeric drug formulations.

Abstract: Highly efficient cationic liposomes have been developed as an improved delivery system for biologically-active reagents. A novel structure, the sandwich liposome, is formed and comprises one or more biologically active agents internalized between two bilomellar liposomes. This structure protects the incoming agent and accounts for the high efficiency of in vivo delivery and for the broad tissue distribution of the sandwich liposome complexes. These novel liposomes are also highly efficient carriers of nucleic acids. By using extruded DOTAP:cholesterol liposomes to form complexes with DNA encoding specific proteins, expression has been improved dramatically. Highest expression was achieved in the lung, while increased expression was detected in several organs and tissues.

Abstract: The present invention provides a liposomal composition for targeted delivery of drugs. The composition comprises poloxamer molecules and liposomes encapsulating one or more delivery agents. At above the critical micellar temperature of the poloxamer, a fraction of the poloxamer molecules form micelles and another fraction becomes incorporated into the liposome surface, thereby inhibiting their adhesion to cells. At a temperature below the critical micellar temperature, the poloxamer molecules dissociate into monomers allowing the liposomes to adhere to adjacent cells and effecting retention of the liposomes in the surrounding tissue. A method is provided for delivery of agents to target site comprising administering the composition to an individual and cooling the target site to cause retention of the liposomes at or near the target site.

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 generally to the amphiphilic polyelectrolyte, poly(2-ethylacrylic acid) and covalently bonded lipids to generate Lipo-PEAA. These Lipo-PEAA are then used to make pH-sensitive liposomes which become unstable, permeable or fusogenic with certain pH changes. In addition, this invention generally describes methods for delivering therapeutic compounds and drugs to target cells by administering to a host the pH-sensitive liposomes of the present invention.

Abstract: Conjugates of a hydrophobic moiety, such as a lipid, linked through a cleavable dithiobenzyl linkage to a therapeutic agent are described. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of the therapeutic agent in its original form. The linkage is stable under nonreducing conditions. The conjugate can be incorporated into liposomes for administration in vivo and release of the therapeutic agent in response to endogeneous in vivo reducing conditions or in response to administration of an exogeneous reducing agent.

Abstract: The present invention provides a pipecolic acid derivative-containing liposome preparation having has an excellent rapid action capable of coping with an emergent situation such as cerebral infarction. A liposome preparation characterized by comprising, as an active ingredient, a pipecolic acid derivative of the ingredient described in the present specification or a pharmaceutically acceptable salt thereof entrapped into liposomes, wherein lecithin is mainly used as the liposome-forming lipid, said liposome preparation containing no cholesterol as a stabilizer.

Abstract: Described herein are liposomes containing etherlipids of the formula: as well as a phosphatidylcholine, a sterol, and a headgroup-derivatized lipid. These liposomes are useful in a variety of therapeutic regimens, including the treatment of cancers and inflammatory disorders.

Abstract: The present invention relates to novel compositions based on hydrated lipidic lamellar phases or liposomal compositions, prepared by combining different lipid molecules, synthetic and/or from natural sources, said compositions comprising at least one of a) labd-13-ene-8?, 15-diol and/or derivatives thereof; b) labd-14-ene-8, 13-diol or derivatives thereof; c) 3?-hydroxy-labd-14-ene-8, 13-epoxy and/or derivatives thereof, d) a plant extract containing the aforementioned labdanes or derivatives thereof. The compositions of the invention exhibit cytotoxicity against cancerous cells and are utilized for the treatment of tumors and leukemias.