Abstract: Disclosed are osteogenic devices comprising a matrix containing substantially pure mammalian osteogenic protein and methods of inducing endochondral bone growth in mammals. A partial amino acid sequence, amino acid composition, solubility properties, and various other data characterizing osteogenic protein are also disclosed, as well as a nucleic acid sequences encoding a consensus osteogenic protein.

Abstract: A new method of producing paucilamellar lipid vesicles has been developed. The vesicles are made of non-phospholipid surfactants. The paucilamellar lipid vesicles have 2-8 lipid bilayers surrounding a central cavity which may be filled with either an aqueous-based solution or an oil or wax.

Abstract: A process is described for generating conjugates of lipids and biologically active agents to produce compositions having therapeutic utility, such as drug delivery vehicles. The process involves mixing the reactive lipid with an appropriate amount of diketene to form an acetoacetylated lipid which is then isolated, dissolved in a suitable medium, and mixed with a nucleophilic-containing biologically active agent to form a biologically active agent-lipid conjugate. Alternatively, the acetoacetylated lipid can be mixed with a polyamine to form a cationic lipid.

Abstract: An insecticidal composition comprising a first composition having an effective amount of at least one species of entomopathogen distributed in a matrix. A second composition selected from vegetable oil, crop oil and partially hydrogenated oil containing mono- and di-glycerides surrounds the first composition and significantly prolongs nematode viability. The matrix is a nematode-containing macrogel or paste of partially hydrogenated oils containing mono- and di-glycerides. The macrogel matrix is selected from a continuous polymer macrogel or microcapsule-containing macrogel. Partially hydrogenated oils containing mono- and di-glycerides, (e.g., Crisco.RTM. shortening), can also be mixed with free nematodes to produce a paste formulation. Trapping nematodes in a Crisco.RTM. matrix formulation along with a water retentive polymer results in increased protection against desiccation and significantly prolongs viability during storage. An insect feeding stimulant, such as raffinose, may also be added to the mix.

Abstract: Stabilized microspherical particles having hydrophobic liquid cores prepared as oil-in-water microemulsions. The particles are stabilized by a surface layer comprising an amphiphilic compound and may be functionalized to allow covalent coupling of a ligand to the surface of the particle. When used as tracers in assays, a water insoluble dye may be incorporated in the core liquid of the microparticles.

Abstract: A microbiocide-containing concentrate for use in thermoplastic polymers as well as in plastisols, is disclosed. The concentrate is primarily solid at ambient conditions and comprises from 1-30 wt% of a microbiocide, a polymer plasticizer and up to 20 wt% of a thermoplastic resin. These concentrates are primarily useful as masterbatch compositions used for incorporation into polymers in order to protect said polymers from fungal or bacterial attack. Along these lines, the present document also discloses processes for incorporating these materials into a polymer or plastisol, and polymers or plastisols made by these processes.

Abstract: Compositions, for example cosmetic or pharmaceutical compositions, and methods of increasing melanin formation on the skin or scalp employ liposomes including between 0.001 and 10 weight percent, with respect to the total weight of the composition, of tyrosine or a tyrosine derivative selected from the group consisting of an alkali metal salt of L-tyrosine, an alkaline earth metal salt of L-tyrosine, methyl L-tyrosinate, ethyl L-tyrosinate, and stearyl L-tyrosinate.

Abstract: Pesticide granules especially for delivering a biological pesticide in aquatic applications have a wax core and the pesticide secured to the core in a water dispersible or water soluble matrix. More specifically the pesticide composition is free flowing and water floatable with the biological pesticide being of the genus Bacillus and the coating matrix being proteinaceous.

Abstract: The invention relates to a cosmetic or pharmaceutical composition, containing hydroquinone and kojic acid or a derivative thereof, especially the salts or esters thereof. The hydroquinone and/or kojic acid component is in a form which is at least partially incorporated into liposomes.The combination of these components in liposomes makes it possible to obtain a synergistic effect in their use as topical formulations, especially dermatological or cosmetic compositions, especially for their skin-lightening activity.

Abstract: A liposome composition is obtained by using as constituent components of the liposome membrane a polyoxyethylene derivative represented by the general formula:X--O--(CH.sub.2 CH.sub.2 O).sub.n --Y (I)wherein X represents an alkanoyl group or an alkyl group, Y represents a residue of a compound having a negative charge, and n is an integer of 2 to 50, and a phospholipid. The liposome composition has good dispersibility, high drug-encapsulation property and high stability.

Abstract: The novel uses of the phospholipid-coated microcrystal in the delivery of water-soluble biomolecules such as polypeptides and proteins. The proteins are rendered insoluble by complexation and the resulting material forms the solid core of the phospholipid-coated particle. Alternatively, the proteins, bio-molecules or drugs can be entrapped in water-soluble form between the membranous layers of the coated microcrystal. All types of phospholipid microcrystals can incorporate 5 nm to 10 um diameter iron oxide particles to allow for manipulation by magnetic fields. Water-soluble bio-molecules including proteins, peptides, and drugs can be entrapped and retained with long shelf life in liposomes at high concentrations, provided that the phospholipid concentration is greater than 10% (w/v) such that greater than 50% of the system volume is enclosed within phospholipid membranes. Both the phospholipid-coated microcrystal and the phospholipid-coated microdroplet can be used as vaccine adjuvants.

Abstract: Encapsulating particles of solid thiocarbonate salts, esters and complexes with air- and water-impermiable coatings produces compositions having long-term stability.

Abstract: The present invention concerns lipid vesicles having dimethylamides as their primary structural lipid. Preferred dimethylamides useful in the invention are DMATO and DMASO oils. These vesicles are useful as carriers of water immiscible oily material such as fungicides. In a most preferred aspect, the invention has DMATO vesicles with TCMTB as a fungicide in trapped therein. The vesicles can be made rapidly and provide aqueous dispersion of these materials without the need for additional organic solvents.

Abstract: A water-dilutable preservative (antimicrobial) concentrate comprising an isothiazolone, a first solvent capable of solubilizing the isothiazolone and having a specific gravity <0.95, a second solvent capable of solubilizing the isothiazolone and having a specific gravity >0.95, and an emulsifier is disclosed. The isothiazolone emulsive concentrates of the invention may be formulated to produce physically stable emulsions.

Abstract: A sustained release pesticide comprises solid pesticidal particles comprising a solid, pesticidally active ingredient, substantially the whole surface of the pesticidal particles being coated with a hydrophobic substance.

Abstract: The invention relates to a process for the preparation of cosmetics or pharmaceutical foam by foaming with the aid of a propellant. According to the invention, a charge consisting of a cosmetics or pharmaceutical product comprising a dispersion of a water-immiscible product in an aqueous solution, the said dispersion being stabilized by niosomes consisting of one or more nonionic lipid layers encapsulating an aqueous phase, the charge comprising 40 to 95% by weight of dispersion and 5 to 60% by weight of propellant, the proportions being stated with respect to the weight of the total charge of the chamber, are introduced into a chamber which is under pressure and fitted with a valve.

Abstract: A photoresponsive liposome which comprises a compound represented by the following general formula (I): ##STR1## wherein R.sub.1 is an alkyl group; R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are selected from the group consisting of an alkyl group, a substituted alkyl group, an alkoxy group, a substituted alkoxy group, a halogen atom and a hydrogen atom; R.sub.6 and R.sub.7, which may be the same or different, are an alkyl group or a hydrogen atom; n is an integer of 1 to 2; and X represents a hydrophilic group, a hydrophobic group or a combination of hydrophilic and hydrophobic groups, bonded through a connecting group, provided that any of these hydrophilic and hydrophobic groups has such properties that the compound represented by the general formula (I) becomes available as a component forming the membrane of liposome.

Abstract: The present invention features a method of making lipid vesicles and the lipid vesicles themselves made from monomeric and dimeric alkyds. These alkyds are esters made as a condensation product of a first reactant having at least one free hydroxyl group and a C.sub.12 -C.sub.20 fatty acids chain and a second reactant which is an aromatic acid chloride or anhydride. Preferred first reactants are esters of polyols and C.sub.12 -C.sub.20 fatty acids, ethers of polyols and C.sub.12 -C.sub.20 fatty acids, and C.sub.12 -C.sub.20 fatty alcohols.

Abstract: A new method of producing paucilamellar lipid vesicles has been developed. The vesicles are made of non-phospholipid surfactants. The paucilamellar lipid vesicles have 2-8 lipid bilayers surrounding a central cavity which may be filled with either an aqueous-based solution or an oil or wax.

Abstract: Microparticles which are less than 12 .mu.m in size and are formed of or comprise a solid lipophilic group-containing compound having an HLB value less than about 20 produce a long lived ultrasonically echogenic entity in aqueous liquid and are useful as left heart ultrasonic contrast image enhancing agents. Contrast media for ultrasonic diagnostics comprising a liquid vehicle containing (a) suspended therein microparticles of a mixture of at least one (C.sub.8 -C.sub.20)-fatty acid and at least one solid that is not a surfactant and (b) microbubbles, are especially effective upon ultrasonic imaging after intravenous administration, for the contrasting of both the right heart and left heart, of the myocardium, as well as other organs, such as liver, spleen, and kidneys.

Abstract: New polysaccharide esters are disclosed, and more precisely esters of acidic polysaccharides chosen from the group formed by carboxymethylcellulose, carboxymethyl starch and carboxymethylchitin. These new esters and some esters of the type already known are useful as medicaments, for the manufacture of pharmaceutical and cosmetic preparations, in the field of biodegradable plastic materials and, therefore, for the manufacture of medical, surgical and sanitary articles, as well as numerous other industrial sectors in the place of acidic polysaccharides now in common use.

Abstract: This invention relates to devices useful for the controlled delivery of one or more beneficial agents to an environment of use. More specifically, this invention concerns such devices which are powered by lyotropic liquid crystals. This invention also relates to the controlled delivery of one or more beneficial agents to an aqueous environment of use through the use of such lyotropic liquid crystal powered dispensing devices. Also disclosed are methods for the controlled delivery of one or more beneficial agents to an aqueous environment of use which comprise administering to or otherwise placing the devices of this invention in the environment of use.

Abstract: Disclosed are osteogenic devices comprising a matrix containing substantially pure mammalian osteogenic protein and methods of inducing endochondral bone growth in mammals. A partial amino acid sequence, amino acid composition, solubility properties, and various other data characterizing osteogenic protein are also disclosed, as well as a nucleic acid sequences encoding a consensus osteogenic protein.

Abstract: This invention concerns compositions for zootechnical and veterinary use, characterized in that biologically active substances are incorporated in protective matrices, which have the following properties: 1) controlled release (ruminal by-pass) effect; 2) chemical-physical protection of active principles against degradation induced by technological processes of production, storage and pellettization of fodders for all animal species. The matrices of the invention are characterized by a plastic rheological behaviour due to the presence of lipogelling agents. The obtained products show the following advantages: increased active principle stability in feeds for all animal species; protection of the active principles from attack of Rumen microorganisms in fodder from attack of for ruminants.

Abstract: The present invention relates to encapsulated parasiticides, a method for their production, and methods of treatment to prevent or eradicate infestation using the encapsulated parasiticides. The formulations of the present invention are water or oil-based and have many advantages over conventional formulations in safety, cost, and utility.

Abstract: A new method of coupling proteins and other targeting molecules to lipid vesicles has been developed. A bifunctional agent forms a covalent bond without damaging the lipid structure and permits retention of protein activity.

Abstract: A wax composition prepared by polymerizing a mixture of at least one macromonomer selected from methylpolysiloxane(meth)acrylate macromonomers containing one (meth)acryl group and three of more methylsiloxy groups in a molecule with one or more of a vinyl monomer(s), which is copolymerizable with said macromonomer, to undergo polymerization using a radical producing agent in the presence of both a polysiloxane component (dimethylpolysiloxane and/or methylphenylpolysiloxane) and an organic wax, in which portions of said polysiloxane component, said organic wax and said mixture are controlled to 20-80 pts. wt., 5-75 pts. wt. and 5-50 pts. wt., respectively, to acquire extremely high uniformity and stability while retaining excellent properties inherent in silicone-containing wax compositions.

Abstract: The invention provides a freeze-dried potential liposome mixture having an amphipathic lipid and a cyclosporin or derivative thereof for use in possible liposome delivery of cyclosporin into cells. A method to produce the freeze-dried mixture is also disclosed. When reconstituted to yield liposomes in an aqueous medium, substantially all of the cyclosporin present in the freeze-dried mixture is encapsulated in the liposomes.

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: The A fragment of the diphtheria toxin (DTA) was encapsulated in pH-sensitive liposomes. This novel reagent is extremely cytotoxic to cells expressing surface antigen which is recognized by the immunoliposome. The reagent is not toxic to cells which do not express the antigen. Thus, this reagent, or others similarly prepared represent potential anticancer reagents.

Abstract: A new method of producing paucilamellar lipid vesicles has been developed. The vesicles are made of non-phospholipid surfactants. The paucilamellar lipid vesicles have 2-8 lipid bilayers surrounding a central cavity which may be filled with either an aqueous-based solution or an oil or wax.

Abstract: The invention relates to a process for preparing immunogenic complexes in which an amphiphatic antigenic protein or peptide in dissolved or solubilized form is contacted with a solution containing a detergent, a sterol, and a glycoside comprising hydrophobic and hydrophilic regions, in at least the critical micelle forming concentration, the detergent is removed, and the immunogenic complex formed is purified. Optionally, the solution with which the antigenic protein or peptide is contacted also contains a phospholipid, preferably phosphatidylethanolamine. The preferred sterol is cholesterol, and preferred glycosides are saponins, espeically Quil A.The immunogenic complex is useful as a vaccine. Its immunogenic power is higher than that of corresponding micelles formed by aggregation of the antigens, and is also higher than that of the antigens incorporated in liposomes.

Abstract: A novel hydrophobic polymeric matrix is provided which is suitable for use after implantation in vivo in a subject for the controlled release and delivery of biologically active substances such as drugs, antibiotics, steroids and the like. Alternatively, the matrix can be used outside the body for release of fragrances, pesticides and the like. The implantable matrix comprises a polymeric polyanhydride formulation whose internal anhydride linkages are hydrolytic in nature in varying degrees in accordance with the chemical composition of the backbone, pH and temperature of the environment. As the individual anhydride linkages become hydrolyzed, the matrix erodes predominantly by surface erosion into non-toxic biocompatible degradation products with concomitant release of the biologically active substance.

Abstract: Nitroxide contrast agents for MRI have a long useful life and can be administered in low concentration doses. Such agents include nitroxide-doped liposomes that encapsulate an oxidant and large molecules having surfaces covered with persistent nitroxide free radicals.

Abstract: Liposomes containing phosphatidylethanolamine, palmitoyl homocysteine or oleic acid or palmitic acid, fuse rapidly when the pH of the medium is reduced below 7. Liposome fusion was measured by (a) mixing of the liposomal lipids as shown by resonance energy transfer, (b) gel filtration and (c) electron microscopy. The presence of phosphatidylethanolamine or acid addition esters thereof in the liposomes greatly enhances fusion; whereas the presence of phosphatidylcholine inhibits fusion. During fusion of liposomes containing phosphatidylethanolamine:palmitoyl homocysteine (8:2), almost all of the encapsulate calcein is released. Inclusion of cholesterol (40%) in the liposomes substantially decreases leakage without impairing fusion. Those pH sensitive liposomes are fused to deliver biologically active molecules such as DNA, into living cells.

Abstract: A miticidal composition for controlling spider mite populations is formed by impregnating a controlled release substrate with farnesol and nerolidol to form a flowable liquid concentrate or wettable powder. The flowable liquid concentrate or wettable powder is added to a liquid spray base to which a miticide has been added, and mixed therewith to form the miticidal composition. The resulting composition is applied by conventional tank spray equipment to the foliage of plants or trees to control spider mite populations therein.

Abstract: A method is provided for preparing small (less than 2000 .ANG.) lipid vesicles in commercial quantities by microemulsifying lipid compositions using very high shear forces generated in a homogenizing apparatus operated at high pressures at a selected temperature. These vesicles are suitable for various biological applications including targeting of tumors in a body for diagnosis and treatment.

Abstract: Drug-containing lipid vesicle preparations are prepared by adding an aqueous solution or suspension to a phospholipid which contains a lipophilic surfactant to form a mixture, stirring said mixture whereby lipid vesides are formed, then dispersing said vesicles in a dispersion medium to form an emulsion.

Abstract: A suspension of liposomes whose sizes are predominantly greater than about 1 micron is passed through an asymmetric ceramic filter whose inner-surface pore size is about 1 micron. The processed liposomes have a selected average size of about 0.4 microns or less, depending on the number of filter cycles, and a narrow distribution.

Abstract: The novel uses of the phospholipid-coated microcrystal in the delivery of water-soluble biomolecules such as polypeptides and proteins. The proteins are rendered insoluble by complexation and the resulting material forms the solid core of the phospholipid-coated particle. Alternatively, the proteins, bio-molecules or drugs can be entrapped in water-soluble form between the membranous layers of the coated microcrystal. All types of phospholipid microcrystals can incorporate 5 nm to 10 um diameter iron oxide particles to allow for manipulation by magnetic fields. Water-soluble bio-molecules including proteins, peptides, and drugs can be entrapped and retained with long shelf life in liposomes at high concentrations, provided that the phospholipid concentration is greater than 10% (w/v) such that greater than 50% of the system volume is enclosed within phospholipid membranes. Both the phospholipid-coated microcrystal and the phospholipid-coated microdroplet can be used as vaccine adjuvants.