Abstract: Novel pentablock polymers comprising PGA-PCL-PEG-PCL-PGA or PEG-PCL-PLA-PCL-PEG, wherein PEG is polyethylene glycol, PCL is poly(?-caprolactone), PGA is poly(glycolic acid), and PLA is poly(lactic acid).

Abstract: A composition of matter for use in encapsulating a drug is expressed by formula (1) or formula (2): wherein R1 and R2 are each independently a hydrogen atom or a substituted or unsubstituted, linear or branched alkyl group having 1 to 12 carbon atoms; A is a hydrophilic polymer chain; L1 and L3 are each a linking group; B is a cation-containing group; R3 is a side chain of an amino acid; z is an integer of 5 to 500; x is an integer of 40% or more of z; y is 0 or a positive integer; z-x-y is 0 or a positive integer; p is an integer of 1 to 10; and q is an integer of 1 to 10.

Abstract: The present invention relates to nanoparticles comprising a biodegradable polymer, preferably the vinyl methyl ether and maleic anhydride (PVM/MA) copolymer, and a polyethylene glycol or derivatives thereof. These nanoparticles are easy to produce and provide excellent bioadhesion, size and zeta potential characteristics making them suitable for the administration of active molecules. The selection of the type of polyethylene glycol used in their production allows suitably modulating the characteristics of these nanoparticles, which can be advantageously used according to the type of drug to be carried and/or the method of administration of the pharmaceutical formulation. pegylation is carried out by simple incubation for a short time period of the two macromolecules in question, without needing to have to resort to the use of organic solvents with high toxicity or long and laborious organic synthesis processes.

Abstract: The disclosed method involves preparation of a composition containing a poorly water soluble substance. The composition has a median diameter of not more than 1 ?m, and includes (i) a poorly water soluble substance, (ii) polyvinylpyrrolidone or a vinylpyrrolidone-vinyl acetate copolymer, and (iii) an auxiliary dispersion stabilizer. By employing such constitution, a poorly water soluble substance is sufficiently micronized and a composition containing a poorly water soluble substance showing good absorbability of the poorly water soluble substance can be provided.

Abstract: A biocompatible polymer material is described that exhibits mechanical and physical properties that are fundamental to many medical devices and treatment of many medical diseases and disorders. The material is composed of a combination of acrylate monomers polymerized via a microemulsion polymerization. Multiple applications of the polymer material are presented.

Abstract: A granulate mixture suitable for regenerating a bone contains at least one expandable particle and at least one nondeformable particle. The at least one expandable particle contains a swelling agent. The swelling is enclosed by a biodegradable sheathing or be a biodegradable casing. Three-dimensional callus distraction may be accomplished by introducing the granulated mixture into a bone defect.

Abstract: The present invention relates to a drug-containing polymeric composition comprising at least one therapeutic agent encapsulated in at least one biocompatible polymer, wherein at least a portion of the therapeutic agent in this polymeric composition is crystalline. The at least one biocompatible polymer may form a substantially continuous polymeric matrix with the at least one therapeutic agent encapsulated therein. Alternatively, the at least one biocompatible polymer may form polymeric particles with the at least one therapeutic agent encapsulated therein.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: A controlled release particle includes a core containing an antibiotic compound, and a shell covering the core. The controlled release particle is obtained by a production method including a first step in which a first component containing an antibiotic compound and a polymerizable vinyl monomer is subjected to suspension polymerization to form the core containing the antibiotic compound and a polymer of the polymerizable vinyl monomer; and a second step in which a second component containing a shell-forming component is subjected to interfacial polymerization to form a shell, wherein in the second step, the interfacial polymerization is started simultaneously with the start of the suspension polymerization of the first step, or started after the start of the suspension polymerization of the first step.

Abstract: A controlled release particle includes a core formed by suspension polymerization of a core ingredient component containing an antibiotic compound and a first polymerizable vinyl monomer, and containing a first polymer of the first polymerizable vinyl monomer and the antibiotic compound present in the first polymer; and a shell formed by suspension polymerization of a second polymerizable vinyl monomer having affinity with water of the same or higher than that of the first polymerizable vinyl monomer, containing a second polymer obtained from the second polymerizable vinyl monomer, and covering the core.

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: The present invention relates to a magnetic nanoparticle for tumor therapy, comprising: a magnetic core; a shell encapsulating a surface of the magnetic core, wherein the shell is made of a polymer with carboxylic groups; a poly-nucleotide chain connected to a surface of the shell; an anti-tumor drug connected to the poly-nucleotide chain, wherein the anti-tumor drug comprises at least one functional group, and each of the functional group is independently a pyrimidine group or a purine group; and an antibody connected to the shell, wherein the antibody identifies a target tumor. In addition, the present invention further provides a method for manufacturing the magnetic nanoparticles for tumor therapy and a pharmaceutical composition containing the magnetic nanoparticles. Accordingly, the magnetic nanoparticle for tumor therapy of the present invention can achieve effective treatment of tumor by synergistic effects between hyperthermia and targeted chemotherapy.

Abstract: Polymeric nanoparticles with a hydrophobic core that encapsulates curcumin and a hydrophilic shell with one or more chemotherapeutic agents (e.g., doxorubicin) associated with the shell surface are formed from N-isopropylacryl amide (NEPAAM), acrylic acid (AA), and at least one vinyl monomer selected from the group consisting of vinyl acetate, 4-vinyl benzoic acid, methylmethacrylate, vinylmethacrylate, N-vinylpyrrolidone, N-vinyl piperidone, N-vinyl caprolacum, N-vinyl carbazole, and styrene, where the NIPAAM, the AA, and the vinyl monomer are present at molar ratios of 50-70:10-30:10-30 for NIPAAM:AA:vinyl monomer. These nanoparticles effectively overcome multidrug resistance and ameliorate cardiomyopathy in vivo.

Abstract: The present disclosure provides compositions and methods of treating Breast Cancer. Disclosed is a nanoparticle paired to at least one of W genetic materials that suppress key regulators of fat synthesis (e.g. Rev-erb) to cause a predefined target cell types apoptosis or X predefined targeting moieties that cause predefined target cell types apoptosis and correspond to Y predefined target parameters associated with Z predefined target cell types in connection with treatment of at least one of the following breast cancer, glioblastoma, head and neck cancer, pancreatic cancer, lung cancer, cancer of the nervous system, gastrointestinal cancer, prostate cancer, ovarian cancer, kidney cancer, retina, cancer, skin cancer, liver cancer, genital.

Abstract: Nano-constructs comprising nanoshells and methods of using the nano-constructs for treating or ameliorating a vascular condition are provided.

Abstract: Nanocrystals, compositions, and methods that aid particle transport in mucus are provided. In some embodiments, the compositions and methods involve making mucus-penetrating particles (MPP) without any polymeric carriers, or with minimal use of polymeric carriers. The compositions and methods may include, in some embodiments, modifying the surface coatings of particles formed of pharmaceutical agents that have a low water solubility. Such methods and compositions can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for administration routes involving the particles passing through a mucosal barrier.

Abstract: Nanoparticles gene carriers, particularly nanoparticle gene carriers which exhibit increased rates of diffusion through cystic fibrosis (CF) mucus, as well as methods of making and using thereof, are described herein. The nanoparticle gene carriers are formed from a nucleic acid complexed to one or more biocompatible, polycationic polymers. The nanoparticle gene carriers also contain one or more mucus resistant polymers. In a particularly preferred embodiment, the nanoparticle gene carrier is a nanoparticle formed from one or more nucleic acids, PEI, and a mucus-resistant/diffusive graft copolymer composed of a PEI backbone functionalized by one or more PEG side chains. The nanoparticle gene carriers can efficiently diffuse through CF mucus, and can effectively serve as a vehicle to administer one or more nucleic acids to a patient suffering from CF.

Abstract: A process for forming microspheres is disclosed. The process includes: forming a first plurality microspheres comprising at least one bioactive agent and modified cellulose; contacting the first plurality of microspheres with a solution of a biodegradable polymer to form a discontinuous phase liquid; contacting the discontinuous phase liquid with a continuous phase liquid to form an emulsion; and extracting a second plurality of microspheres from the emulsion, the second plurality of microspheres comprising the first plurality of microspheres.

Abstract: Particles, compositions, and methods that aid particle transport in mucus are provided. The particles, compositions, and methods may be used, in some instances, for ophthalmic and/or other applications. In some embodiments, the compositions and methods may involve modifying the surface coatings of particles, such as particles of pharmaceutical agents that have a low aqueous solubility. Such compositions and methods can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for ophthalmic applications, and may be used for delivering pharmaceutical agents to the front of the eye and/or the back of the eye.

Abstract: The present invention provides a method for forming a multicompartmentalized vesicular structure comprising an outer block copolymer vesicle and at least one inner block copolymer vesicle, wherein the at least one inner block copolymer vesicle is encapsulated inside the outer block copolymer vesicle. The method comprises forming the at least one inner block copolymer vesicle by any method and adding block copolymers dissolved in a suitable solvent to a dispersion of the at least one inner block copolymer vesicle in an aqueous buffer under conditions that allow the block copolymers to form the outer block copolymer vesicle and encapsulate the at least one inner block copolymer vesicle. A multicompartmentalized vesicular structure and its uses are also provided.

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: Particles, compositions, and methods that aid particle transport in mucus are provided. The compositions and methods may include, in some embodiments, modifying the surface coatings of particles including pharmaceutical agents that have a low water/aqueous solubility. In some embodiments, a surface coating includes a synthetic polymer having pendant hydroxyl groups on the backbone of the polymer, such as poly(vinyl alcohol) (PVA). Such compositions and methods can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for administration routes involving the particles passing through a mucosal barrier.

Abstract: Particles, compositions, and methods that aid particle transport in mucus are provided. The particles, compositions, and methods may be used, in some instances, for ophthalmic and/or other applications. In some embodiments, the compositions and methods may involve modifying the surface coatings of particles, such as particles of pharmaceutical agents that have a low aqueous solubility. Such compositions and methods can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for ophthalmic applications, and may be used for delivering pharmaceutical agents to the front of the eye and/or the back of the eye.

Abstract: A pesticide granule is provided that includes a base carrier particle. A liquid pesticide coating is applied to the particle surface. The coating may contain adjuvants. The coating has sufficient tack to adhere a second powdered pesticide to the carrier particle. The usage of tackifying agents to render the particle surface tacky enough to adhere powdered pesticide is reduced or eliminated. The powdered pesticide is sized to a mean diameter of less than 10% of the carrier diameter to promote adhesion. The synergistic rapid acting pesticide delivery associated with the granule results in the usage of less pesticide to control a given pest with reduced environmental impact. Bifenthrin is a representative of the liquid pesticide.

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: Disclosed is an oral dosage form comprising: (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is not released when the dosage form is administered orally intact.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances using core-shell composites and compositions comprising such core-shell composites. In particular, the invention provides core-shell particles and compositions comprising potassium binding polymers, and core-shell particles and compositions comprising sodium binding polymers, and in each case, pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are also disclosed. The compositions and methods of the invention offer improved approaches for treatment of hyperkalemia and other indications related to potassium ion homeostasis, and for treatment of hypertension and other indicates related to sodium ion homeostasis.

Abstract: The present invention provides immediate release and modified release oral dosage forms. Specifically, the invention provides modified and immediate release pharmaceutical dosage forms containing memantine that exhibit an enhanced release profile and provide reliable absorption. The dosage forms may be used to treat mild, moderate or severe Alzheimer's disease or neuropathic pain.

Abstract: Polyarginine-coated nanoparticle, and methods for making and using the nanoparticle. The nanoparticle can have a core that includes a material that imparts magnetic resonance imaging activity to the particle and, optionally, include one or more of an associated therapeutic agent, targeting agent, and diagnostic agent.

Abstract: The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Abstract: A method for treating a subject, such as a human patient, having a vascular disorder. The treatment method administers a therapeutic effective amount of a nanoparticle or a chemical structure to the subject to treat the disorders. The nanoparticle includes a poly L-arginine polymer and a Factor VIIa inhibitor conjugated to, or encapsulated in, the poly L-arginine polymer. The chemical structure includes a Factor VIIa inhibitor that includes at least one nitric oxide (NO) donor. The disorder may be sickle cell disease; stimulated or pathological angiogenesis associated disorders, cancer, ocular angiogenesis-mediated disorders such as diabetic retinopathy and macular degeneration, coagulation and/or platelet activation-associated disorders, pulmonary hypertension, or combinations thereof.

Abstract: A radiopaque particulate material one or more of SiO2, TiO2, La2O3, Na2O and MgO and useful for embolization which optionally includes therapeutic components that are released in vivo.

Abstract: A method of controlling a physical characteristic of polymeric nanocarrier-encapsulated protein particles includes altering or selecting a weight percentage of a hydrophobic polymer block in a total amphiphilic diblock copolymer of a primary emulsion of a double emulsion, freeze-thaw technique. The primary emulsion is formed using a freeze-thaw cycle of the amphiphilic diblock copolymer and a protein having a molecular weight of up to or equal to 300,000 Da. Selection of the hydrophobic polymer block percentage alters one or more characteristics of the resulting nanoparticles, such as shape. Thus, as one aspect, a method of producing filamentous polymeric nanocarrier-encapsulated protein (i.e.

Abstract: Milled nanoparticles comprising a biologically active agent, at least one biopolymer and a coating containing at least one coating which is a polymer or ligand are produced using milling and coating techniques which have not previously been used for these applications.

Abstract: A biomedical implant according to this invention comprises ceramic complex, which includes a surface-modified basic ceramic particles, which are basic ceramic particles modified their surface with first biodegradable polymers, and the second biodegradable polymers. The first and second biodegradable polymer are combined each other and form a stereo complex. The biomedical implant has a superior effect to suppress inflammation caused by degradation of biodegradable polymers with improving its mechanical property.

Abstract: This disclosure relates to an extended release oral dosage form comprising a matrix containing a viscosity modifier (but no lipid) and coated granules containing metoprolol or a pharmaceutically acceptable salt or solvate thereof. The dosage form has alcohol resistance and may also have crush resistance.

Abstract: A method for preparing poorly water soluble drug particles is disclosed. The method comprises dissolving a drug in at least one organic solvent to form a drug/organic mixture, spraying the drug/organic mixture into an aqueous solution and concurrently evaporating the organic solvent in the presence of the aqueous solution to form an aqueous dispersion of the drug particles. The resulting drug particles are in the nanometer to micrometer size range and show enhanced dissolution rates and reduced crystallinity when compared to the unprocessed drug. The present invention additionally contemplates products and processes for new drug formulations of insoluble drug particles having high dissolution rates and extremely high drug-to-excipient ratios.

Abstract: Novel pentablock polymers comprising PGA-PCL-PEG-PCL-PGA or PEG-PCL-PLA-PCL-PEG, wherein PEG is polyethylene glycol, PCL is poly(?-caprolactone), PGA is poly(glycolic acid), and PLA is poly(lactic acid).

Abstract: The present invention relates to a novel effective dry powder vaccine formulation that increases the immune response in the host. The formulation comprises of an antigen entrapped into a polymer particle, coated with alum, finally spray dried into a dry powder. This formulation is used to elicit long lasting higher antibody titers than alum adsorbed antigen or admixture of polymer entrapped antigen and alum.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances using core-shell composites and compositions comprising such core-shell composites. In particular, the invention provides core-shell particles and compositions comprising potassium binding polymers, and core-shell particles and compositions comprising sodium binding polymers, and in each case, pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are also disclosed. The compositions and methods of the invention offer improved approaches for treatment of hyperkalemia and other indications related to potassium ion homeostasis, and for treatment of hypertension and other indicates related to sodium ion homeostasis.

Abstract: Dosage forms having a core having a surface having means for controlling release(s) on an active agent(s); methods of manufacturing, tools used in manufacturing; and uses of the dosage forms are described.

Abstract: The present invention relates to an oral pharmaceutical composition comprising metronidazole, wherein metronidazole is released from the composition generally at the pH 5.0 and above.

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 discloses a magnetic nanodrug for treating thrombosis, which comprises a core formed of magnetic nanoparticles, a shell enveloping the core and made of carboxyl-functionalized polyaniline, and a thrombosis-treatment drug covalently bonded to the shell. The magnetic nanodrug of the present invention is non-toxic to vascular endothelial cells, has superior stability, features superparamagnetism, and can be uniformly dissolved in water. Therefore, the magnetic nanodrug for treating thrombosis can be guided by an external magnetic field to concentrate on a specified region and increase the effect of thrombosis treatment.

Abstract: The present disclosure is directed to compositions comprising encapsulated particles of diethylenetriaminepentaacetate (DTPA) and a zinc salt such as zinc acetate, and to pharmaceutical compositions comprising such encapsulated compositions. The present disclosure is also directed to methods of treatment by administering an effective amount of the compositions and pharmaceutical compositions of the present disclosure, to methods of making such encapsulated particle compositions, and to methods of making the corresponding pharmaceutical compositions.

Abstract: Disclosed is a method for preparing a longer sustained-release formulation containing bioactive substances. More particularly, the present invention provides a method for preparing longer sustained-release microcapsules comprising: adding an emulsion including bioactive substances, biocompatible polymer and polyvinylpyrrolidone to an aqueous solution.

Abstract: The present provides amphiphilic block copolymer coated surfaces (e.g., nanoparticles, medical devices, etc.) and methods of preparing such surfaces. In certain embodiments, the present invention provides amphiphilic block copolymer coated single dispersed nanoparticles, which are stable in buffer (e.g., PBS) and have neutral but functionable surfaces, and methods of preparing the same.

Abstract: The present invention relates to pharmaceutical formulations for the controlled delivery of threo-3-(3,4-dihydroxyphenyl)serine (threo-DOPS) and derivatives of it. Such formulations can contain an extended or slow release component that maintains therapeutic concentration of threo-DOPS in the blood plasma over a prolonged time period. They can be further combined with an immediate release formulation to produce a product that, when administered to a patient in need thereof, results in substantially steady levels of active drug, eliminating the sharp peaks and troughs in blood plasma drug levels experienced with the existing threo-DOPS formulations.

Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.