Abstract: Liposomes of a size of less than 200 nanometers target ischemic myocardial tissue and preferentially deliver active agents to infarcted areas in the absence of antibodies bound to the liposomes to effect the delivery.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of zaxol and taxol-related compounds. Potency of the lipid prodrugs is comparable to that of the corresponding nonderivatized drugs. In a preferred embodiment, taxol or substituted taxol is covalently bound to a phospholipid.

Abstract: Lipid-containing prodrugs are provided for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids. Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids. The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.

Abstract: A method is provided for delivering micellular particles containing chemotherapeutic agents and a marker to tumors within a body for the diagnosis and treatment of such tumors. The micellular particles are small, less than 2000 .ANG. and incorporate pure, neutral phospholipid molecules in their external surface. Enhanced delivery of the micellular particles containing marker and chemotherapeutic agents may be achieved by introducing an initial group of positively charged micellular particles to block the reticuloendothelial cells present in the body.

Abstract: Micellular particles such as small unilamellar vesicles of less than 2000 .ANG. loaded with .sup.111 In are administered to BALB/c mice in which EMT6 tumors had been induced. Whole body scintographs of the mice to which either neutral or positively or negatively charged vesicles had been administered show a substantial quantity of the vesicle entrapped .sup.111 In localized in the tumor. Blocking of macrophages in the liver and spleen by first administering unlabeled, aminomannose substituted vesicles before administration of the labeled vesicles increases uptake of the .sup.111 In labeled vesicles in the tumor.

Abstract: Delivery vehicle formulations comprising active agents encapsulated within microparticles which include a succinimidyl moiety extending externally from a lipid molecule therein are capable of the cytoplasmic or nuclear cell delivery of intact encapsulated active agents.

Abstract: Adhesions in synovial capsules are prevented through the administration of liposome intercalated nonsteroidal anti-inflammatory agents.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

Abstract: Liposomes with hyperosmotic concentration of compounds encapsulated therein are targeted to tumors for neutron capture therapy. The compounds have an element with a large neutron capture cross section and an isotope that emits alpha particles when bombarded with neutrons. A method employing such liposomes for neutron capture therapy is also described.

Abstract: Delivery vehicles comprising an outer biocompatible encapsulating layer, an inner amphiphilic active ingredient-associated layer and an active ingredient are described. The delivery vehicles are biocompatible and are capable of solubilizing the active ingredient for in vivo delivery to bodily tissue or other bodily systems. Uses include nuclear magnetic resonance imaging and therapeutic drug delivery.

Abstract: Delivery vehicle formulations comprise active agents encapsulated within liposomal vesicles to which are attached protein hormones (ligands) such as interleukin-2. The ligands are capable of showing affinity for specific cell receptors resulting in delivery of the encapsulated active agent to target cells, enabling delivery of active agents to particular cell populations in the treatment of conditions such as immune system disorders.

Abstract: A process for the encapsulation of oligonucleotides in liposomes includes the suspending of liposomes containing a divalent cation in a solution containing an oligonucleotide and having an osmolarity of a less than that of the internal aqueous phase.

Abstract: Disclosed herein are vesicle compositions for controlled sustained release of an encapsulated therapeutic agent after parenteral administration. By adjusting the osmolarity between the suspending solution and the solution within the vesicles by adjusting the concentration of the suspending solution, the rate of release of the therapeutic agent after parenteral administration can be varied. The compositions can be effectively administered by intramuscular, subcutaneous injection or other means.

Abstract: In the presence of a preserving additive, unilamellar phospholipid vesicle preparations are preserved during dehydration. Dehydration is effected by subjecting said preparations to a drying operations capable of causing flash evaporation.

Abstract: A thin-film evaporator for preparing liposomes in commercial quantities provides a film-forming zone of uniform thickness which enables the uniform evaporation of an organic solvent to form a film of uniform thickness, followed by in situ hydration of the film in an aqueous phase by agitation with a rotor.

Abstract: A method is provided for delivering micellular particles containing a radiolabelled marker to tumors within humans. The micellular particles are less than approximately 2000.ANG. and incorporate essentially chemically pure phospholipid molecules in their external surface. Human patients given intravenous injections of such radiolabelled micellular particles showed tumors imaged by such method, without developing symptoms related to the micellular particles.

Abstract: The present invention relates to a process of stabilizing micellular particles such as vesicles and increasing the shelf life by suspending the particles in a polymeric gel matrix. The invention also relates to such particles suspended in the gel matrix with a protective gel surface thereabout which is capable of becoming fluid and converting the protective surface of an aqueous suspension.

Abstract: Compositions comprising phospholipid-encapsulated vesicles of active ingredient and triglyceride are described. In a preferred embodiment the vesicles are composed of a hexamethylmelamine active ingredient, with trilaurin or trimyristin as the triglyceride and a mixture of distearoylphosphatidylcholine, distearoylphosphatidylglycerol and cholesterol in the phospholipid outer layer. Preferably the molar ratios of active ingredient: triglyceride: DSPC: CHOL:DSPG will be from about 1:4:2:1:0 to about 1:4:1:1:1. Glycerol may be added to the carrier phase to reduce agglomeration. The composition may be used to deliver otherwise aqueous-insoluble agents to humans or animals to treat, for example, tumors.

Abstract: Novel liposome-entrapped cationic, lipophilic drug compositions, e.g., anthracycline antineoplastic agent compositions, and multistep entrapment/loading procedures for preparing them are disclosed. These procedures involve forming liposomes from phospholipids, such as distearoyl phosphatidylcholine or a similar long chain fatty acid diester phospholipid, to be loaded with the drug, e.g., daunorubicin or doxorubicin, in aqueous medium in the presence of an acid, e.g., an organic acid which can be monofunctional pyranosidyl acid such as lactobionic acid, adding the drug, and then adding a base such as calcium carbonate whose cations cannot pass through the vesicles' bilayers to charge neutralize the organic acid anions in the external aqueous phase and induce the acid anions in the internal aqueous phase to become neutralized by attracting the cationic, lipophilic drug.

Abstract: A single-vessel method is provided for preparing liposomes in commercial quantities by forming a homogeneous and uniform lipid film in a thin-film evaporator by evaporation of the organic solvent, followed by in situ hydration of the film in an aqueous phase by agitation with the rotor.