Abstract: The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof, and their salts, hydrates and solvates. In particular, the present invention relates to a method of preparing N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC) and its corresponding disodium monohydrate.

Abstract: The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

Abstract: The present invention provides targeting lipids of structure L100—linker—L101 ??(CI), where L100 is a lipid, lipophile, alkyl, alkenyl or alkynyl, L101 is a ligand or —CH2CH2(OCH2CH2)pO(CH2)qCH2-ligand, p is 1-1000, and q is 1-20. In addition, the invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo.

Abstract: Single phase pharmaceutical compositions for topical application, in addition to kits and methods of use and administration are provided. The compositions comprise a biologically active agent; a delivery vehicle comprising at least a non-polymeric crystallization inhibitor and a film-former; and a volatile solvent; wherein the biologically active agent is present in the composition in a subsaturated state, the biologically active agent is present in the delivery vehicle in a supersaturated state, and the crystallization inhibitor is capable of delaying crystallization of the biologically active agent in the delivery vehicle. Biologically active agents include terbinafine and acyclovir. Treatments for onychomycosis and Varicella zoster infection, HSV-1 infection or HSV-2 infection are provided.

Abstract: The invention relates to nonaqueous pharmaceutical preparations comprising a glucocorticoid ester and an acid, and to the stabilization of glucocorticoid esters in such preparations by acids.

Abstract: The invention concerns nanocapsules, in particular with an average size less than 50 nm, consisting of an essentially lipid core liquid or semiliquid at room temperature, coated with an essentially lipid film solid at room temperature having a thickness of 2-10 nm. The invention also concerns a method for preparing same which consists in producing a reverse phase of an aqueous emulsion brought about by several temperature raising and lowering cycles. Said lipid nanocapsules are particularly designed for producing a medicine.

Abstract: The invention provides lubricant compositions comprising magnesium stearate dihydrate. The lubricant compositions may be used to lubricate a variety of bioactive formulations including pharmaceutical compositions.

Abstract: The invention relates to a water-based delivery system for an active substance, characterized by enhancing skin barrier restoration in the stratum corneum comprising water, a fatty acid, cholesterol, a ceramide and at least one skin lipid precursor.

Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Fatty acid-based, pre-cure-derived biomaterials, methods of making the biomaterials, and methods of using them as drug delivery carriers are described. The fatty acid-derived biomaterials can be utilized alone or in combination with a medical device for the release and local delivery of one or more therapeutic agents. Methods of forming and tailoring the properties of said biomaterials and methods of using said biomaterials for treating injury in a mammal are also provided.

Abstract: Pharmaceutical compositions comprising a water/oil/water (W1/O2/W3) or an oil/water/oil (O1/W2/O3) double microemulsion, with droplets size below one micron, with the drug included in the internal water phase W1 or internal oil phase 01, whereas the external oil 02 and second water phase W3 or the external water phase W2 and second oil phase 03 contain substances able to inhibit the enzymes, present in the mucosa or biological barrier to be permeated or physiological environment of administration, capable to degrade the drug or to cause its efflux from the barrier; alternatively the external oil and second water phase or external water phase and second oil phase contain permeation enhancing agents, i.e., substances able to increase the diffusion of the drug through the biological barrier.

Abstract: This application relates to a composition comprising a mixture of different organic solvents formulated for controlled drug release. The release profile of the drug can be regulated by adjusting the compositional ratios of the solvents. In one embodiment of the invention a first solvent is water-soluble and a second solvent is water-insoluble. The first and second solvents are miscible and together form a solution containing the drug. The hydrophobicity of the composition can be adjusted by altering the relative amount of the second solvent. The composition also includes a solid lipid dissolved in the drug-containing solution. In aqueous environments the lipid may precipitate to form a thin membrane in an outer surface portion of the composition, thereby further regulating the release of the drug. The membrane is preferably renewable. That is, as the outermost portion of the lipid is biodegraded at a target location in vivo, additional outer portions of the lipid precipitate to renew the thin membrane.

Abstract: A new method for the preparation of microencapsulated essential oils is disclosed. The microcapsules containing essential oils or a formulation containing thereof may be used for various non-agricultural applications.

Abstract: This invention relates to a bioactive composition comprising: (d) pH sensitive bioactive agent (e) an edible carboxylic acid containing moiety and (f) an edible alkalising moiety, wherein the proportion of said moieties and active agent provide pH control such that (i) when 400 mg of said composition is added to 20 ml of 0.033 normal hydrochloric acid and at a temperature of 37+/?3° C., the pH reaches a value in the range 4 to 8, and (ii) when 400 mg of said composition is added to 20 ml of deionised water at pH 7 and at a temperature of 37+/?3° C., the pH reaches a value less than 8.5.

Abstract: The invention provides methods and compositions for providing biocompatible surfaces to medical articles. In particular the invention provides biocompatible coatings with heparin activity. In some aspects, the biocompatible coatings of the invention are able to release a bioactive agent. The coatings can be formed using biostable or biodegradable polymeric material and photoreactive groups. The invention also provides methods for improving the quality of bioactive agent-containing coatings by performing pre-irradiation of biocompatible coating compositions.

Abstract: Provided is a flowable bioresorbable tissue dressing comprising a gas-forming porogen and a gel or gel-forming solution. Also provided is kits for preparing the above-described tissue dressing. Further provided are methods of treating a tissue site of a mammal with the above dressing. Also provided is a reduced pressure delivery system for applying a reduced pressure tissue treatment to a tissue site.

Abstract: Stable oil containing long-chain polyunsaturated essential fatty acids (LC-PUFAs) in the form of triacylglycerols, in particular arachidonic acid (ARA), dihomogammalinolenic acid (DHGLA), docosahexaenoic acid (DHA) or eicosapentaenoic acid (EPA). Such an oil may be prepared by bringing a carrier oil into contact with a biomass obtained from the culture of a microorganism, in particular a fungus or a microalga containing the acids ARA, DHGLA, DHA or EPA. These oils can be incorporated into the composition of a foodstuff, of a cosmetic or pharmaceutical product.

Abstract: A non-tumorigenic skin care composition is provided.

Abstract: The invention relates to an improved bleach activator and bleach activator compositions in the form of granules for use in washing, cleaning and disinfectant compositions. More specifically, the invention relates to granular bleach-activating mixtures that consist substantially of a) a hydroxybenzoic acid derivative of formula (I) in which R is C8-C11-alkyl and b) tetraacetyl ethylene diamine and/or 1,5-diacetyl-2,4-dioxo-1,3,5-hexahydrotriazine, the granules being free of binding agents.

Abstract: An alcohol-free, transdermal drug delivery composition administered via a metered spray drug delivery device is described herein. The non-occlusive transdermal drug delivery composition includes a therapeutically effective amount of at least one physiologically active agent or prodrug thereof, an effective amount of at least one dermal penetration enhancer; and at least one non-volatile liquid. The transdermal drug delivery composition is administered to a dermal or mucosal surface of an animal needing the same using a metered spray device capable of delivering a fine spray of substantially uniform particle size to minimize the required drying time therefor.

Abstract: The present invention provides particle conjugates for drug delivery. Such conjugates comprise one or more heatable surfaces, one or more thermally-responsive linkers, and one or more agents to be delivered. In some embodiments, conjugates and populations of conjugates can be used to treat and/or diagnose a disease, disorder, and/or condition. The present invention provides methods for producing and/or using thermally-responsive conjugates.

Abstract: The present invention relates to the addition of lecithin during the crystallization of organic molecules in organic solvents as an antistatic agent to reduce or eliminate static buildup, thus reducing the potential for explosion and equipment damage during chemical processing.

Abstract: The present invention provides dialkyl ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same.

Abstract: A formulation and dosage form for enhancing the bioavailability of orally administered hydrophilic macromolecules includes a permeation enhancer, a hydrophilic macromolecule, and a carrier such as a nonionic surfactant that exhibits in-situ gelling properties. The formulation is delivered within the GI tract as a liquid having at least some affinity for the surface of the GI mucosal membrane. Once released, it is believed that the liquid formulation spreads across one or more areas of the surface of the GI mucosal membrane, where the carrier of the formulation then transitions into a bioadhesive gel in-situ. As a bioadhesive gel, the formulation presents the hydrophilic macromolecule and the permeation enhancer at the surface of the GI mucosal membrane at concentrations sufficient to increase absorption of the hydrophilic macromolecule through the GI mucosal membrane over a period of time.

Abstract: The invention relates to a water-based delivery system for an active substance, characterized by enhancing skin barrier restoration in the stratum corneum comprising water, a fatty acid, cholesterol, a ceramide and at least one skin lipid precursor.

Abstract: This invention provides a pharmaceutical composition comprising a lipase inhibitor; a lipophilic oil absorbent selected from the group consisting of hydrogenated castor oil, hydrogenated vegetable oil, glyceryl behenate, glyceryl palmitostearate and a mixture thereof; and a pharmaceutically acceptable additive, an oral formulation of a lipase inhibitor prepared there from and a method for preparing said formulation. The formulation of the present invention can minimize side effects such as oily spotting, fatty/oily stool, abdominal distension and flatus, and thus it can be advantageously used for preventing or treating obesity and hyperlipaemia.

Abstract: Magneto-vesicles with two different surfactants, i.e., Dioleoyl phosphatidylethanolamine (DOPE) and dimethyl dioctadecylammonium bromide (DDAB), were synthesized using size controllable magnetite nanoparticles (Dm=9 nm) as cores. From AFM measurements, the average sizes of vesicles and magneto-vesicles are approximately 316 nm and approximately 311 nm, respectively. These biocompatible magneto-vesicles have very good dispersity in aqueous solution and affinity to cells, rendering them potentially useful as magnetic carriers for field-guided drug delivery. Light-emitting dye molecules together with magnetic particles were encapsulated inside these vesicles. An experiment showed that disruption of the vesicles releases the encapsulated dye molecules, thus the principle of using the drug-carrying magneto-vesicles as a drug delivery agent that can be guided by applied magnetic field has been demonstrated.

Abstract: Disclosed are bupivacaine transdermal delivery systems, and related methods.

Abstract: The present invention relates to compositions and methods for use in delivering nucleic acids and other agents into cells and tissues. In particular, the present invention provides lipid mixtures at the gel-liquid crystalline phase transition providing superior lipofection activity for transferring materials into cells and tissues.

Abstract: Cosmetic compositions comprising at least one structuring polymer chosen from polymers of following formula (I): in which n denotes a number of amide units, such that the number of ester groups represents from 10% to 50% of the total number of ester and amide groups; R1 is, in each case, independently an alkyl or alkenyl group having at least 4 carbon atoms; R2 independently represents, in each case, a C4 to C42 hydrocarbonaceous group, provided that 50% of the R2 groups represent a C30 to C42 hydrocarbonaceous group; R3 independently represents, in each case, an organic group provided with at least 2 carbon atoms, with hydrogen atoms and optionally with one or more oxygen or nitrogen atoms; and R4 independently represents, in each case, a hydrogen atom, a C1 to C10 alkyl group or a direct bond to R3 or another R4, so that the nitrogen atom to which both R3 and R4 are bonded forms part of a heterocyclic structure defined by R4—N—R3, with at least 50% of the R4 groups representing a hydrogen atom and at le

Abstract: New non-ionic surfactants in the form of polyoxyalkylene glycol hydroxy fatty acid derivatives or monoalkylated polyoxyalkylene glycol hydroxy fatty acid derivatives having a polyoxyalkylene/alkyl polyoxyalkylene chain with a chain-length of 25-455 repeating units and a specified substituent on the hydroxy position of the specified hydroxy fatty acid, according to the general formula (I) CH3—(CH2)x—CH—(CH2)y—CO—[—O—R3—]z—O—R1 R2—O (I); wherein for example R1 is methyl, R2 is optionally substituted C14-C22 acyl, alkyl, or alkenyl, R3 is ethylene, x is 2-12, y is 7-17, (x+y) is 3-19 and z is 25-57; advantageously prepared by involving an enzymatic process, formulations comprising them, their use as solubilizers and a process involving a hydrolytic enzyme for preparing them.

Abstract: A composition and method of use of a composition for enhancing the usability of eye cosmetics, including but not limited to mascara and liquid eyeliner. The composition and its formulation contains a liquid enhancer, such that a few drops of the liquid enhancer added to the mascara and/or liquid eyeliner are used to maintain the viscosity, consistency, and smoothness of the cosmetic at the levels of the original, newly provided cosmetic. This enhancement thus allows continued ease of use and longer useful life of the cosmetic material.

Abstract: A pharmaceutically delivery system and method of use therefor are described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.

Abstract: The invention relates to a carrier for administering biologically active compounds comprising one or more C1-C4 alcohols, polyols and polymers thereof, water and one or more di and/or mono-(electron transfer agent) phosphate derivatives or complexes thereof. The carrier may be used in administering biologically active compounds, in particular pharmaceuticals including cosmetic agents.

Abstract: The present application relates to a cosmetic or pharmaceutical, in particular lipstick, composition comprising a polycondensate The application also relates to a method of cosmetic treatment using the composition, the polycondensate thus defined and a method of preparing the polycondensate.

Abstract: Thickening agents which containing a specific N-acylamino acid (component A) and a specific amideamine (component B) are capable of generating, when used in combination with a wide variety of oily bases including a hydrocarbon oil and silicone, a creamy thickening composition having a practical dissolution temperature and a smooth feeling in use when applied to the skin.

Abstract: A process for producing a small-sized, lipid-based cochleate. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structures by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca2+ or Zn2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing biologically relevant molecules.

Abstract: A novel artificial muscle material and miniature valves and micropumps made therefrom are provided. The artificial muscle material bends reversibly when electroactuated by applying low voltage, in a wide pH range, even at that of physiological pH, and works without contact with electrodes. Miniature valves made from the artificial material are successfully triggered for the fluid release in a wide pH range, even at that of physiological pH. Novel fluid release devices were manufactured using this artificial muscle, and methods using the same were provided, including an implantable device optimized for trans-scleral drug delivery.

Abstract: The invention relates to pharmaceutical compositions that provide sustained-release of a pharmaceutically active compound and to methods of treating or preventing a condition in an animal by administering the pharmaceutical compositions to the animal. When the pharmaceutical compositions are administered to an animal by injection, they form a drug depot that releases the pharmaceutically active compound over time. The pharmaceutical compositions can also be administered orally.

Abstract: The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.

Abstract: Pigment wetting agent contains a mixture of monoesters and diesters of butylene glycol and fatty acids.

Abstract: The present invention relates to nanoparticles comprising a metallic core with a surface coating, wherein the coating comprises at least an excitable radiative molecule attached thereto or impregnated therein, and wherein the excitable molecule is positioned at a sufficient distance from metallic core to enhance emissions when excited. The nanoparticles are included in compositions that may be used for surface coatings, cosmetics, assays, flow velocity measurements and targeting of tissue.

Abstract: The present invention encompasses pharmaceutical excipient complexes comprising combining at least one carrier with an oily substance, and processes for preparing the same, stable pharmaceutical compositions comprising such complexes and active pharmaceutical ingredients and processes for preparing the same.

Abstract: Methods for hydrolyzing solid ungranulated lysophosphatidylcholine with phospholipase A2 are provided. Also disclosed are methods for making a lipid matrix of lysophosphatidylcholine, monoglyceride and fatty acid, and lipid matrices of particular structure.

Abstract: The object of the present invention is to establish a volatile sulfide production inhibitor that can inhibit the production of volatile sulfides from a composition and to provide a method for inhibiting the production of volatile sulfides from a composition by using the inhibitor. The object are solved by providing a volatile sulfide production inhibitor comprising L-ascorbic acid 2-glucoside as an effective ingredient and a method for inhibiting the production of volatile sulfides from a composition by incorporating the volatile sulfide production inhibitor into the composition.

Abstract: Disclosed is a system for delivery of a drug comprising a multiple unit dosing device comprising a chousing and an actuator, said device containing multiple doses of multiparticulates comprising drug particles, said device upon actuation delivering a unit dose of said multiparticulates, said drug particles having a mean diameter of greater than 10 ?m to about 1 mm such that an effective dose of said drug cannot be delivered into the lower lung of a human patient. Also disclosed are novel methods, devices and dosage forms for delivering a drug.

Abstract: The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.

Abstract: The present invention provides a transdermal formulation for the delivery of at least one active agent. The formulation includes (i) a first compound comprising an organic sulfoxide, and (ii) a second compound selected from the group consisting of a fatty acid ester, a fatty acid, an azone-related compound and mixtures thereof.

Abstract: The invention relates to sterile pharmaceutical compositions for parenteral administration which comprise an oil-in-water emulsion in which a free radical scavenging sedative agent dissolved in an omega-3 rich water-immiscible solvent, is emulsified with water and stabilised by means for a surfactant, the composition being suitable either directly or after dilution with a liquid diluent for parenteral administration to a warm-blooded animal; in particular to such compositions comprising propofol, and which optionally further comprise a metal ion chelating agent (such as edetate), and the use of such compositions in improving survival in critically ill patients.

Abstract: Targeted therapeutic delivery systems comprising specially designed nanocarriers for intracellular therapeutic delivery, mediated by acoustic energy, for use either in vivo or in vitro, are described. Nanocarriers comprised of substantially polymersomes, and mixtures thereof, are used to treat a variety of diseases in humans and other species, such as cancer, opthalmological, pulmonary, urinary or other pathologies. Methods for preparing the targeted therapeutic delivery systems are also embodied, which comprise processing a solution comprised of biopolymers or other species and components, with or without targeting moieties, adding said biopolymers and other compounds to a solution containing one or more therapeutic agents, stabilizing or not stabilizing said nanocarriers, adding one or more contrast agents, and resulting in a targeted therapeutic delivery system. Preferred therapeutics for use with the present invention include nucleic acids, proteins, peptides, and other therapeutic macromolecules.