Abstract: A process for producing a compacted rumen-protected nutrient pellet and the resultant pellet. The process includes the steps of (i) blending a C4-24 fatty acid and a biologically active ingredient to form solid central core particles, (ii) compacting the core particles to form pellets, and (iii) sequentially coating the pellets with an organic solvent and a fatty acid alkali metal or alkaline earth metal salt.

Abstract: Articles, compositions, kits, and methods relating to nanostructures, including synthetic nanostructures, are provided. Certain embodiments described herein include structures having a core-shell type arrangement; for instance, a nanostructure core may be surrounded by a shell including a material, such as a lipid bilayer, and may include other components such as oligonucleotides. In some embodiments, the structures, when introduced into a subject, can be used to deliver nucleic acids and/or can regulate gene expression. Accordingly, the structures described herein may be used to diagnose, prevent, treat or manage certain diseases or bodily conditions. In some cases, the structures are both a therapeutic agent and a diagnostic agent.

Abstract: The present invention provides methods and liposomal compositions useful in therapeutics, and diagnosis, prognosis, testing, screening, treatment and/or prevention of various disease conditions. The present invention provides imaging methods for various conditions. The present invention is a multi-layered drug delivery pathway, inclusive of nanoparticle liposomal formulations and mechanisms of localized action via unzipping upon delivery to the affected tissue site. The nano-encapsulation methodology allows maximization of a potent antioxidant's biocompatibility, increased target cell penetration and uptake, reduced off-target effects and retention of high anti-oxidative activity for promising therapeutic potential.

Abstract: The present invention relates to a controlled-release pharmaceutical composition which, when administered in the evening, promotes rapid sleep onset and makes it easy to wake up in the morning in a refreshing way. The composition comprises: a first portion having sleep-inducing activity, which is able to be degraded and absorbed in vivo within 5 minutes to 1 hour after administration; and a second portion having cognition-enhancing activity, which is able to be released in vivo after 4 to 8 hours from the start of absorption of the first portion. The composition, when administered in the evening, promotes rapid sleep onset and makes it easy to wake up in the morning in a refreshing way.

Abstract: The present invention is directed to microcapsules for reliably modified release and adapted to industrial reproduction of an active principle hardly water-soluble, other than anti-hyperglycemia agents. Each of said microcapsules comprises a core of hardly soluble active principle and a coating film applied on the core. Their mean diameter is less than 1000 microns. The coating film contains a film-forming polymer (PI) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said coating film represents at least 4% p/p of dry matter of their total weight, and its components P1, P2, PL satisfy the following characteristics: dry weight mass fraction of PI relative to the total coating weight ranging between 40 and 90%; dry matter weight fraction of PL/P1+P2 ranging between 15 and 60%; dry matter weight fraction of PL/P1+P2 ranging between 1 and 30%.

Abstract: The present patent application relates to a novel coating system, coated compositions with such a coating system, as well as to the use of such compositions in the production food, feed, dietary supplements and/or pharmaceutical products, as well as to food, feed, dietary supplements and/or pharmaceutical products comprising such compositions.

Abstract: Metal-bisphosphonate nanoparticles are disclosed. Also disclosed are pharmaceutical compositions including the metal-bisphosphonate nanoparticles, methods of preparing the metal-bisphosphonate nanoparticles and materials comprising the nanoparticles, and methods of using the compositions to treat cancer or bone-related disorders (e.g., bone-resorption-related diseases, osteoporosis, Paget's disease, and bone metastases) and as imaging agents.

Abstract: A nano-carrier comprising an antiproliferative drug encapsulated by a lipophilic enhancement agent.

Abstract: The present invention provide compositions and methods for treating a dermatological disorder or disease.

Abstract: The present invention relates to the field of polymer chemistry and more particularly to encapsulated peptides and uses thereof.

Abstract: Nanolipidic Particles (NLPs) having average mean diameters of 1 nm to 20 nm are made from a precursor solution. NLPs can be loaded with a desired passenger molecule. Assemblies of these particles, called NLP assemblies, result in a vehicle population of a desired size. Single application or multifunction NLP assemblies are made from the loaded NLPs and range in size from about 30 nm to about 200 nm. A method of using preloaded NLPs to make larger carrier vehicles or a mixed population provides increased encapsulation efficiency. NLPs have application in the cosmetics, pharmaceutical, and food and beverage industries.

Abstract: Nanolipidic Particles (NLPs) having average mean diameters of 1 nm to 20 nm are made from a precursor solution. NLPs can be loaded with a desired passenger molecule. Assemblies of these particles, called NLP assemblies, result in a vehicle population of a desired size. Single application or multifunction NLP assemblies are made from the loaded NLPs and range in size from about 30 nm to about 200 nm. A method of using preloaded NLPs to make larger carrier vehicles or a mixed population provides increased encapsulation efficiency. NLPs have application in the cosmetics, pharmaceutical, and food and beverage industries.

Abstract: The present invention provides nucleic acid-lipid particles comprising siRNA molecules that silence genes expressed in cancer (e.g., Eg5, EGFR or XIAP) and methods of using such nucleic acid-lipid particles to silence Eg5, EGFR or XIAP gene expression.

Abstract: The disclosure is directed to a nanoparticle comprising a porous framework core including a porous framework material and a compound, and a lipid layer disposed on the surface of the porous framework core.

Abstract: An oral dosage form has the following: an amount of minocycline selected from the group consisting of 55 mg, 80 mg, and 105 mg; an amount of lactose monohydrate; an amount of hydroxypropylmethylcellulose. The hydroxypropylmethylcellulose is at least 8.3 to about 9.8% hydroxypropoxylated. The minocycline in the oral dosage form has a dissolution profile or release rates about 35% to about 50% in 1 hour, about 60% to about 75% in 2 hours, and at least about 90% in 4 hours. There is also provided a method of treating acne in a human and a method of assisting a physician in prescribing a dose of minocycline for the treatment of acne.

Abstract: The present invention is a solventless method of producing polymer coated active pharmaceutical ingredient that is taste-masked and may be released in relatively short time. It employs high energy vibrations or acoustic mixing of API particles, water soluble coating material particles and hydrophobic polymer particles, with or without use of other pharmaceutically relevant powders as media. Additionally the method is capable of producing individually coated drug particles without agglomeration or the long drying times associated with solvent based coating methods.

Abstract: The present invention describes a process for the manufacture of a solid composition comprising a microorganism, which process comprises a first step of blending and/or compacting the microorganism with a salt of a medium or long-chain fatty acid to prepare a powderous mixture or compacted granulate, and a second step of providing said powderous mixture or compacted granulate with a coating. The microorganisms are preferably probiotics. The invention also relates to the solid composition obtained by said process and to its use in food.

Abstract: Microcapsules possessing Lewis acid-Lewis base salt walls incorporate water-immiscible materials, such as N,N-di-ethyl-m-toluamide (DEET), as a core component. Such microcapsules, or similar microcapsules incorporating other core components, may be made by emulsifying a water-immiscible core component in an aqueous solution of one wall-forming reactant, such as the Lewis base, and then mixing that solution with the other wall-forming reactant, such as the Lewis acid. Various adjuvants may be included with the core component to contribute additional characteristics, such as enhancement of a controlled release characteristic or improved mechanical stability.

Abstract: An object of the present invention is to provide a drug delivery carrier that is free from the drug leakage problem and has an easily controllable particle size, and that can be used to deliver water-soluble drugs such as genes and proteins in a wide range of applications, including delivery of water-soluble drugs that do not have high anionic properties, and also can be used as a non-viral gene vector. The invention also provides a process for production of such drug delivery carriers. The drug delivery carrier of the present invention includes a water-soluble drug double-coated with two types of inner and outer surfactants 1 and 2.

Abstract: The invention relates to microencapsulated colorant granules consisting of a core (A) and a shell (B), whereby the core (A) has a diameter of between 1 and 1000 micrometer and comprises a) a colorant (I), b) microcrystalline cellulose, c) a polyol; and whereby the shell (B) has a thickness of between 1 to 500 micrometer and comprises d) a polymer selected from the group consisting of polycarboxylic acids, vinyl polymers, styrene-(meth)acrylic copolymers, cellulose and cellulose derivatives. The invention further relates to cleansing compositions, such as hand soaps, containing said microencapsulated colorant granules.

Abstract: The subject of this invention is a controlled release composition for zootechnical use. In particular, the subject of this invention is a composition comprising micro-pellets that are able to release the physiologically active substances they contain in a controlled manner. In addition, this invention refers to a procedure for preparing said composition as well as the use of said composition in the zootechnical sector.

Abstract: The present invention relates to solid microparticulate oral pharmaceutical forms whose composition and structure make it possible to avoid misuse of the pharmaceutical active principle (AP) they contain. The object of the present invention is to prevent solid oral drugs from being misappropriated for any use other than the therapeutic use(s) officially approved by the competent public health authorities. In other words, the object is to avoid the voluntary or involuntary misuse of solid oral drugs. The invention relates to a solid oral pharmaceutical form which is characterized in that it contains anti-misuse means, in that at least part of the AP it comprises is contained in coated microparticles for modified release of the AP, and in that the coated microparticles of AP have a coating layer (Ra) which assures the modified release of the AP and simultaneously imparts crushing resistance to the coated microparticles of AP so as to avoid misuse.

Abstract: The invention relates to drug-free or drug-loaded lipid particles of a mixed matrix made of solid and liquid lipids, and to a method for producing highly concentrated lipid particle dispersions of solid-liquid particles having a lipid content of from 30% to 95% or a solids content of from 30% to 95% (lipid and stabilizer), which in contrast to biamphipileic cremes are integer particles, and/or which upon dilution of the highly concentrated particle dispersions with the outer phase result in free-flowable particle dispersions.

Abstract: Novel macromolecules for filtering contaminants from water and non-aqueous solutions. Molecules such as polyethyleneimine (PEI) may be functionalized, cross-linked, and/or quaternized to improve their binding capacity or selectivity with particular water contaminants such as bromide, nitrate, and sulfate. The macromolecules may be either recyclable or non-recyclable, and may be recovered or separated from water using means such as ultrafiltration, flocculation, or immobilization on a substrate.

Abstract: The invention concerns microcapsules with prolonged release of active principles with low solubility, consisting of a core containing the active principle and coated with a polymer layer which controls the release of the active principle. The aim is that said oral microcapsules containing hardly soluble active principles, should have a coating film of sufficient thickness to ensure controlled permeability and should be adapted to industrial reproduction. This is achieved by the inventive microcapsules of mean diameter less than 1000 microns, and whereof the coating film contains a film-forming polymer (P1) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA).

Abstract: A method of producing solid composite lipid/drug nanoparticles that includes the steps of: (1) dissolving a lipid and a drug in a suitable organic solvent to form a solution; (2) emulsifying the solution in a liquid to form an emulsion having a discontinuous phase of micelles comprising the organic solvent, the drug and the lipid, and a continuous phase comprising the liquid; and (3) contacting the emulsion with a supercritical fluid under conditions suitable to keep the supercritical fluid in a supercritical state, whereby the supercritical fluid extracts the organic solvent from the micelles, causing them to precipitate as organic-solvent free solid composite lipid/drug nanoparticles suspended or dispersed in the liquid.

Abstract: The present invention relates to a pasty composition, at least containing particles of at least one calcium salt, whereby the particles of the at least one calcium salt are at least partly coated with at least one saturated fatty acid ester (a) that has a melting temperature of at least 45° C., and said particles that are at least partly coated with the saturated fatty acid ester (a) are mixed with at least one saturated fatty acid ester (b) that has a melting temperature below 25° C. to form a pasty composition. The invention also relates to a method for producing a pasty composition, the pasty composition obtainable through said method, and the use of a pasty composition as bone replacement material.

Abstract: The invention relates to compositions and methods for the preparation, manufacture and therapeutic use of polynucleotides, primary transcripts and mmRNA molecules.

Abstract: An abuse-resistant controlled release pharmaceutical composition comprising a pharmaceutically effective amount of discrete particles of an active capable of abuse, wherein surfaces of said particles are wetted with a water insoluble coating material, and preferably wherein said composition comprises a matrix, in which said particles are distributed, and which renders the abuse-capable compound within the matrix difficult to separate from the matrix; and a method for the preparation of a controlled release pharmaceutical composition having a reduced potential for abuse, comprising applying a pressure force to a mixture comprising a water insoluble material, and particles of a pharmaceutically active compound capable of inducing in a subject a reaction that is physiologically or psychologically detrimental if administered in an immediate release dosage form, thereby resulting in surface coated particles, and incorporating said surface coated particles into a pharmaceutical composition.

Abstract: The invention provides microparticles for use in a pharmaceutical composition for pulmonary administration, each microparticle comprising a particle of an active substance having, on its surface, particles of a hydrophobic material suitable for delaying the dissolution of the active substance. The invention also provides a method for making the microparticles.

Abstract: Formulation of acoustically activatable particles having low vaporization energy and methods for using same are disclosed. According to one aspect, a method of producing particles of materials includes, with a first substance that includes at least one component that is a gas at room temperature and atmospheric pressure, performing one of: causing the first substance to condense to a liquid phase, and extruding or emulsifying the first substance into or in the presence of a second substance to create a droplet or emulsion in which the first substance is encapsulated by the second substance; or extruding or emulsifying the first substance into or in the presence of a second substance to create a bubble in which the first substance is encapsulated by the second substance and wherein at least some of the first substance is in a gaseous phase, and causing the first substance to condense to a liquid phase, which causes the bubble to transform into a droplet or emulsion.

Abstract: A process for the production of an n-butyric acid compound in microencapsulated form comprises the stages of:—providing a granular material based on the n-butyric acid compound, —mixing the granular material with a matrix having a content of long-chain C14-C22 saturated fatty acids of from 40% to 95%, and an amount of between 1% and 20% of a mineral agent in which an effective amount of calcium sulphate dihydrate is present, heating the mixture to a temperature higher than the melting temperature of the lipid component of the matrix, —spraying the mixture into a cooling chamber having a temperature lower than the melting temperature of the lipid component of the matrix, so that the latter solidifies around the granular material, forming a covering thereof.

Abstract: Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes.

Abstract: A particle includes an aqueous core; a first amphiphilic layer surrounding the aqueous core; and a polymeric matrix surrounding the first amphiphilic layer.

Abstract: Provided is a surface-treated powder, in which a powder is treated with a surface-treating agent composed of a mixture A+B including A: an alkyl alkoxy silane of a general formula (1): (CnH2n+1)aSi(OCmH2m+1)b and B: one kind of a compound or two or more kinds of compounds selected from a reactive organo silicone of the following general formula (2): (R13SiO)(R12SiO)p(SiR23) and a C12 to C22 saturated or unsaturated branched fatty acid. In the general formula (1), n is an integer of 1 to 18, m is an integer of 1 to 3, a, b represent an integer of 1 to 3, and a+b=4. In the general formula (2), R1s mutually independently represents a lower alkyl group having 1 to 4 carbon atoms or a hydrogen atom or a hydrogen atom, respectively, R2 is any of an amino group, a hydrogen atom, a hydroxyl group and a C1-C4 lower alkoxy group, and p is an integer of 1 to 300.

Abstract: Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.

Abstract: A cholesterol efflux assay probe formulation having a core comprised of a biocompatible hydrophobic material at least partially coated with a sphingomyelin/cholesterol layer, methods of making and methods of using are described.

Abstract: The invention relates to an aqueous dispersion comprising microcapsules, the capsule wall of which is formed from radically polymerized monomers and the capsule core of which comprises at least one oil, in which the capsule core comprises at least one lipophilic surfactant and the continuous phase of the dispersion comprises at least one agrochemical. In addition, the invention relates to a process for the preparation of an aqueous dispersion by (i) providing an aqueous dispersion comprising microcapsules, the capsule wall of which is formed from radically polymerized monomers and the capsule core of which comprises at least one oil and at least one lipophilic surfactant (microcapsule crude dispersion), and (ii) mixing with at least one agrochemical.

Abstract: The present invention relates to a method for “hot melt coating” of pharmaceutical active ingredients characterized by organoleptic or physicochemical properties that it is desirable to mask. The invention also relates to the resulting medicinal active ingredients with masked organoleptic or physicochemical properties and the compositions comprising same.

Abstract: Disclosed are multi-compartmental nanoparticulate systems for imaging as well as the diagnosis, monitoring, and treatment of inflammation and/or disease. These multicompartmental nanoparticulate systems can be used to target specific cells or ceullular structures. Furthermore, these systems are capable of simultaneous delivery of hydrophilic and lipophilic compositions. Finally, these systems also allow for temporal control of drug delivery.

Abstract: Biocompatible intraocular implants, such as microparticles, include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the prostamide component may be encapsulated by the ploymeric component. The present implants include oil-in-oil emulsified implants or microparticles. Methods of producing the present implants are also described. The implants may be placed in eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma.

Abstract: A livestock feed supplement in which a core particle containing sodium metabisulfite and at least one binder is enrobed with an enteric coating, wherein the thickness and composition of the coating protects the sodium metabisulfite from decomposition to sulfur dioxide in an aqueous acid stomach environment. Also disclosed are a method of delivering sodium metabisulfite to the lower gastrointestinal tract of an animal, and a method of delivering an antidote to relieve the toxic effect of vomitoxin in an animal, by administering to the animal the livestock feed supplement.

Abstract: The invention consists of a method for manufacturing an aqueous formulation containing at least one oil, and comprising the steps of mixing at least one associative polymer, one oil, and water, encapsulating the oil by increasing the pH to a value greater than 8, potentially precipitating the mixture by reducing the pH to a value less than 6, and potentially isolating the resulting particles by removing the water. The aqueous formulations, as with the aqueous dispersions, and the resulting solid particles constitute other objects of the invention.

Abstract: The present invention relates to novel nanocell compositions and their use in imaging, diagnostic and treatment methods. In one embodiment, nanocells tailored for imaging methods comprise a nanocore surrounded by a lipid matrix, and are modified to contain a radionuclide core or a nanocore with an emission spectra. The nanocells may be size restricted such as being greater than about 60 nm so that they selectively extravasate at sites of angiogenesis (e.g. tumor) and do not pass through normal vasculature or enter non-tumor bearing tissue. In this way, angiogenic sites can be both detected and treated. In another embodiment, nanocells are tailored for various treatment methods, including the treatment of brain cancer, asthma, Grave's Disease, Cystic Fibrosis, and Pulmonary Fibrosis.

Abstract: The invention relates to methods of targeted drug delivery of antiviral compounds, including, chemical agents (like nucleoside analogs or protease inhibitors) and nucleic acid based drugs (like DNA vaccines, antisense oligonucleotides, ribozymes, catalytic DNA (DNAzymes) or RNA molecules, siRNAs or plasmids encoding thereof). Furthermore, the invention relates to targeted drug delivery of antiviral compounds to intracellular target sites within cells, tissues and organs, in particular to target sites within the central nervous system (CNS), into and across the blood-brain barrier, by targeting to internalizing uptake receptors present on these cells, tissues and organs. Thereto, the antiviral compounds, or the pharmaceutical acceptable carrier thereof, are conjugated to ligands that facilitate the specific binding to and internalization by these receptors.

Abstract: The present invention relates to a novel crosslinked polyethylenimine (PEI) nanoparticle based nucleic acid transfection agent wherein the crosslinker is having carbon chain in the range of C2 to C8, ranging between 3.27-19.8%, having the size of nanoparticle ranging between 20-600 nm and zeta potential ranging from +5 to 50 mV.

Abstract: A powder composition, includes: (A) an oil-soluble antioxidant substance powder; (B) a water-soluble antioxidant substance powder; and (C) at least one of zinc, selenium, manganese and copper.

Abstract: Antibodies that bind to c-Met are provided herein, as well as related compositions and methods of use. Methods of use encompass cancer therapies and diagnostics. In certain embodiments, antibodies bind mammalian cell surface antigen (e.g., cancer cell surface antigen). The antibodies can also be endocytosed upon binding to cells. Cells that can be targeted by the antibodies include carcinomas, such as those in lung, kidney, liver, stomach, breast, and brain, etc.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for coating a particle comprising a pharmaceutically active ingredient (API) comprising the steps of providing a composition comprising carbonate ions, phosphate ions, or a mixture thereof, providing a particle comprising an API, and precipitating a carbonate salt, a phosphate salt or a mixture thereof onto said particles. The present invention is also directed to a particle comprising an API, wherein the particle is coated with a coating comprising a carbonate salt, phosphate salt, or mixture thereof, and to a pharmaceutical composition comprising said particles. Moreover, the present invention is also directed to the use of said particles for preparing a medicament.

Abstract: The present invention relates to hydrogel particles coated with lipid, which are made from dispersing hydrogel particles in an organic solvent in which lipids are dissolved, and to a method for manufacturing same. Unlike the existing method for manufacturing hydrogel core vesicles, the present invention can effectively manufacture same by using an emulsification method, without involving the steps of chemical treatment of the surface of hydrogels or dilution, thereby facilitating mass production and preventing the decrease of drug encapsulation efficiency.