1411 results about "Drug molecule" patented technology

In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful election of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.

Various polymers, including cationic polyamine polymers and dendrimeric polymers, are shown to possess anti-proliferative activity, and may therefore be useful for treatment of disorders characterised by undesirable cellular proliferation such as neoplasms and tumours, inflammatory disorders (including autoimmune disorders), psoriasis and atherosclerosis. The polymers may be used alone as active agents, or as delivery vehicles for other therapeutic agents, such as drug molecules or nucleic acids for gene therapy. In such cases, the polymers' own intrinsic anti-tumour activity may complement the activity of the agent to be delivered.

Methods of implanting, applying, or adhering various drug molecules directly into or onto the surface of medical devices through gas cluster ion beam (GCIB) and / or monomer ion beam surface modification of the medical devices before or after depositing the various drug molecules onto the medical devices.

A composition comprising intact minicells that contain a drug molecule is useful for targeted drug delivery. One targeted drug delivery method employs bispecific ligands, comprising a first arm that carries specificity for a bacterially derived minicell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target drug-loaded minicells to specific mammalian cells and to cause endocytosis of the minicells by the mammalian cells. Another drug delivery method exploits the natural ability of phagocytic mammalian cells to engulf minicells without the use of bispecific ligands.

The invention relates to an amphiphilic block copolymer and a preparation method thereof, and a micelle drug delivery system formed by the copolymer and an anti-tumor drug. The amphiphilic block copolymer comprises a hydrophilic chain segment and a hydrophobic chain segment, and the end of the hydrophobic chain segment is sealed by hydrophobic radicals. According to the amphiphilic block copolymer disclosed by the invention, methoxy polyethylene glycol (or polyethylene glycol)-polyester segmented copolymer with generally recognized safety is taken as a base material, and terminated hydroxyl hydrophobic radicals of the polyester chain segment are modified, thus the compatibility of hydrophobic chain segments in drug molecules and segmented copolymers is improved, and mutual acting force is increased; through a self-assembling method, the drug can be solubilized in micelle hydrophobic cores of the amphiphilic block copolymer, and the drug molecules are limited in the micelle cores so as not to be likely to be dissolved out, thus drug delivery micelle with high stability is obtained.

The invention provides a drug residue competition-type quantum dot-labeled immunochromatography assay test-strip / detection card and an observation device thereof, comprising the following preparation steps of coating the antibody of quantum dot-labeled drug molecule on a fiberglass film, coating the drug-molecular-carrier protein coupler and second antibody on a pyroxylin film or a cellulose acetate film respectively to form a detection belt and a quality control belt; preparing the immunochromatography assay test-strip from the fiberglass film and the pyroxylin film or the cellulose acetate film on a polyester or plastic plate, and assembling a shell. The quantum dots of the detection belt and the quality control belt on the test-strip is triggered by the ultraviolet LED source of the observation device, and the change of the fluorescent intensity of the observation belt and the quality control belt is observed, thus being capable of quantitatively analyzing the content of the drug molecule in the sample. The invention has simple operation, high sensitiveness and quick quantification, is suitable for detecting the drug residue in the food and can be widely applied to the customhouse, airport, health supervising department, household and the like.

The invention discloses chitosan-functionalized metal organic framework materials. The chitosan-functionalized metal organic framework materials comprise at least one metal ion and an organic ligand. A preparation method of the chitosan-functionalized metal organic framework materials comprises the following step of: carrying out hydrothermal reaction on the metal ion and the organic ligand in a certain proportion at high temperature in a reaction kettle or reacting by adopting a microwave process, an ultrasonic process, and the like by taking a surfactant as a template to synthesize the metal organic framework materials in different shapes, and modifying the metal organic framework materials by a biocompatible material chitosan and a derivative thereof, and the like, to functionalize the organic framework materials. In a process of synthesizing nano-scale metal organic frameworks and modifying by using chitosan and the derivative thereof, different drug molecules can be loaded to the internal frameworks of the metal organic frames and external chitosan macromolecular structures. The chitosan-functionalized nano-scale metal organic framework materials disclosed by the invention can be applied to targeted transportation of various drugs and controlled release of drugs in a living body.

In the present invention, a biodegradable bone graft is disclosed, which includes: a scaffold made of a biodegradable material; and a collagen-embedding matrix portion which completely encompasses the scaffold. The above-mentioned bone graft can increase the micro-porosity of the scaffold to enable cells to grow adhesively thereon. Compared with the scaffold only, the above-mentioned bone graft has high hydrophilicity. Hence, the bone graft of the present invention can efficiently retain tissue fluid, cell growth factors, blood and / or bone marrow which are mixed with the bone graft beforehand to achieve osteoinduction. Furthermore, the collagen-embedding matrix portion can also serve as a carrier to encompass other bone graft materials and drug molecules. The present invention also relates to a method for manufacturing the above-mentioned bone graft.

Disclosed herein are novel targeted drug delivery and controlled release methods and compositions where optically absorbing nanoparticles, such as nanoshells, are functionalized on their surfaces with thermolabile molecules that bind the drug molecules to be delivered. The linkage between the thermolabile moiety on the nanoparticles and the drug is deliberately designed or selected to be temperature sensitive, so that upon illumination of the nanoparticle at a wavelength of light, the drug molecules on the nanoparticles will be released. Targeting molecules, such as antibodies, aptamers or other molecules like folic acid, can be concurrently bound to the nanoparticle surface to deliver the nanoparticle to specifically targeted cells or tissues prior to the photothermally induced drug release. In this way the nanoparticles can be advantageously concentrated on the target prior to illumination, which makes the disclosed compositions both a targeted delivery and a controllable drug release vehicle.

The invention discloses a medicine carrying system based on nano graphene oxide, and is characterized in that the surface of the nano graphene oxide contains two hydrophilic potential groups of carboxyl and sulfonic acid group, carboxyl of the nano graphene oxide is subject to coupling with targeted molecules of folacin, polypeptide or antibody with the help of chemical cross-linker, and carbon atoms of nano graphene oxide absorb and load with one or more than one medicine molecules containing aromatic nucleus to form a targeted medicine carrying system. Proved by application in laboratories,the medicine carrying system can practically improve targeted medicine application and targeted cytotoxicity on each disease point where the medicine is applied, and provides a new thought for targeted therapy on tumor, cancer and other pathogeny.

The invention discloses a meso-porous silicon nano-drug carrier with both reduction responsiveness and targeting ability and a preparation method thereof. Firstly, meso-porous silicon nano-particles are prepared with a sol-gel method, and are developed into a nanometer reservoir of drug molecules; then a disulfide bond is introduced into the surface of the meso-porous silicon nanometer reservoir with a simple chemical modification method and is used as a cohesive tie; secondarily, a biocompatible natural extracellular matrix-collagen molecule is creatively fixed to the surface of the meso-porous silicon nanometer reservoir and is developed into a nanometer encapsulator of the meso-porous silicon nanometer reservoir; and finally a lactobionic acid molecule is modified to the surface of a meso-porous silicon / collagen nanometer compounding system and is used as a specificity receptor of a liver cancer cell membrane surface receptor (ASGP-R) so as to construct a meso-porous silicon / collagen-lactobionic acid multifunctional compound type nano-drug carrier system with both cell specificity targeting ability and reducing substance / enzyme responsiveness.

This invention relates to a method and system for improving diagnostic imaging and / or delivering therapeutically active agents for control of hyperlipidemia and infectious diseases (bacterial or viral), comprising nanoscale block copolymer assemblies carrying drug molecules in its core and receptor peptide in the corona surrounding the core, forming larger micelle or vesicle aggregates with target molecules such as LDL molecules and surface lipid of microorganisms.

The invention provides ABA type triblock biodegradable polyurethane with amino side chains and a preparation method and uses thereof, belongs to the field of biomedical materials and solves the problem that the existing biodegradable polyurethane has molecular weight uncontrollable, wide molecular distribution index and complexity in self-assembly. The ABA type triblock biodegradable polyurethane with amino side chains is shown as in a structural formula I or II. The ABA type triblock biodegradable polyurethane is controllable in polymer molecular weight and wide in molecular weight distribution and can serve as a drug carrier; drug molecules, target molecules or fluorescence molecules are grafted to active side groups of the polyurethane by means of physical encapsulation or chemical bonding, so that a carrier drug system having one or multiple of functions such as being untargeted, being targeted, pH sensitivity, photosensitivity, enzyme sensitivity and fluorescence probing is constructed.

This invention provides Chelating Complex Micelles as a drug carrier. The Chelating Complex Micelles can load drugs without changing their structure, and therefore extend the half-life of drugs in the human body. The chelating complex micelles contain a metal ion core, at least one polymer, and at least one drug molecule. The metal ion is considered as a Lewis acid while polymer chain and drug molecules are referred to as Lewis bases. The drug molecule is linked to the polymer via forming coordinate bonds with metal ion, and then self-assembled to form chelating complex micelles as a drug carrier.

A nanotube device comprises a gel matrix that includes microcapsules and functionalized nanotubes, or other functionalized nanostructures incorporated into said gel matrix. Pharmaceutical compositions and methods of treatment comprising same. The pharmaceutical compositions of the present invention enable the specific and targeted delivery of therapeutic agents such as DNA molecules, peptides, including antibodies, drug molecules (e.g. small organic molecules), while offering sufficient resistance towards mucus layer of the intestine and high concentrations of enzymes and other molecules found in the blood stream and the GI tract.

The present invention provides NO and, optionally, drug releasing macromers and oligomers wherein the drug molecule and NO releasing moiety are linked an absorbable macromer or oligomeric chain susceptible to hydrolytic degradation and wherein the macromer or oligomer comprises of repeat units derived from safe and biocompatible molecules such as glycolic acid, lactic acid, caprolactone and p-dioxanone. Furthermore, the present invention relates to controlled release of nitric oxide (NO) and / or drug molecule from a NO and drug releasing macromer or oligomer. Moreover, the present invention also relates to medical devices, medical device coatings and therapeutic formulations comprising of nitric oxide and drug releasing macromers and oligomers of the present invention.

The present invention relates to a conjugate of hydrophilic polymer-multicarboxyl oligopeptide and drug molecule of the following formula: wherein: P is a water soluble polymer; m is an integer of 2˜12; j is an integer of 1˜6; Ri is a group selected from H, C1-12 alkyl, substituted aryl, aralkyl, heteroalkyl and substituted alkyl; X and Z are linking groups; and TA is drug molecule. The conjugate has low toxicity and an ability to carry more than one drug molecule to improve solubility, sustain and control drug release, and has a remarkably enhancing effect especially to antitumor drug such as paclitaxel and camptothecin etc.

The invention relates to a drug-loaded contact lenses and a corresponding preparation method. The drug-loaded contact lenses are obtained firstly through UV-curing or heat-curing and then through drug-liquid immersion. The drug-loaded contact lenses can be particularly defined as a combination of a contact lenses material containing cyclodextrin and drug molecules and comprise the contact lenses formed by combining a crosslinked polymer hydrogel formed by copolymerizing mono-substituted cyclodextrin monomers, polymerization monomers and crosslinkers with one kind or a plurality of acetazolamide, methazolamide, puerarin or prostaglandin. The characteristic of forming inclusion compounds between the cyclodextrin molecules and drug molecules is adopted to increase the quantity of loaded drugs so as to reduce the stimulation to eyes by drugs and control the drug release speed for eye diseases of curing glaucoma, etc.

The invention relates to a novel amphiphilic-block-copolymer-based pro-camptothecin drug, which is a compound of methoxy polyethylene glycol- polylactic acid and camptothecin derivatives (mPEG-X-PLA-T), wherein, mPEG refers to methoxy polyethylene glycol; X refers to linking group, for example, succinic acid; PLA refers to polylatic acid; T refers to drug molecule, that is, camptothecin derivatives such as, camptothecin, 10-hydroxycamptothecine, 7-ethyl-10- hydroxycamptothecine. Polylactic acid is connected with camptothecin derivatives through ester bond.

The invention discloses an aptamer and a new use of derivative thereof. The new use provided by the invention is application of aptamer and the derivative thereof in preparation of target drugs. The invention further protects the target drugs obtained by coupling the drugs with the aptamer or the derivative thereof. The invention has the advantages of screening and preparing specific aptamer or derivative thereof under the condition of not knowing the molecular transformation of the target cell surface related to the disease, and can simultaneously obtain multiple aptamers or derivatives thereof of molecular related to the cell surface cell; the specificity of the obtained aptamer or derivative thereof is strongly combined with the disease cell; the aptamer or the derivative thereof can be chemically synthesized in large scale and can be easily connected with the drug molecules and has low cost; the molecular weight of the aptamer or the derivative thereof is relatively small without immunologic competence and toxicity; the aptamer or the derivative thereof has good stability; and the formed target drugs are stable. The invention has very high application value.

A bioresorbable material is incorporated with bioactive agents to form an implant used for treatment against hard tissue or soft tissue defects and diseases. Antibiotics or anti-cancer agents are incorporated to treat hard or soft tissue infections or cancers. Sustained release of the bioactive agents or drug molecules may be achieved after implantation at the targeted sites. The dosage of the active agents or molecules, the microstructure, morphology, and composition of the bioresorbable material allow control of the release profile. The invented implant may be used for drug delivery, chemotherapy, or gene therapy. Various microstructure and the morphologies of the implants are injectable like putty or shaped with multilayers.

A conjugate of water soluble polymer-amino acid oligopeptide-drug of Formula (I) below and a pharmaceutical composition comprising the conjugate are provided. In the conjugate, P is a water soluble polymer; X is a linking group, wherein the linking group links P and A1; each of A1, A2 and A3 is independently same or different amino acid residue or amino acid analogue residue; each of D1 and D2 is independently same or different drug molecule residue; a is 0 or 1; b is an integer of 2-12; c is an integer of 0-7; d is 0 or 1. The conjugate could improve drug load capacity, water solubility, stability and activity of the drug.

A novel multi-arm polyethylene glycol (PEG) (I) and preparation method thereof. Active derivatives (II) based on the multi-arm PEG. Gels formed of the active derivatives. Drug conjugates formed of the active derivatives and drug molecules and uses thereof in medical preparation. The multi-arm PEG is formed by polymerizing ethylene oxide with pentaerythritol oligomers as initiator, wherein PEG is the same or different and is a —(CH2CH2O)m-, the average value of m is an integer of 3-1000, l is an integer more than or equal to 2. An 8-arm PEG is preferred, wherein l is equal to 3. The active derivatives (II) comprise link groups X attached to PEG and active end groups F attached to X.

The invention provides a brand new drug molecule construction method based on a pharmacophore model which relates to the medicine development assisted by computers. A pharmacodynamic characteristic segment is selected, folded and placed in an appropriate position in the pharmacophore model. The connection of the pharmacodynamic characteristic segment is controlled by a genetic algorithm to construct a new molecule completely fitting for the pharmacophore model. The method thereof comprises the following steps: the pharmacophore model is input; a sub-database of the pharmacodynamic characteristic segment and the connection is built; the pharmacodynamic characteristic segment is reasonably placed in the framework of the pharmacophore model, and the population is initialized; a judgment is made on whether the pharmacodynamic characteristic segment is directly connected or a linker is added; the produced molecule is judged on pharmacophore characteristic, space steric hindrance limitation and pharmacodynamic property; the individual fitness degree is calculated; with the operation of hybridization and mutation, and a new population is generated; a compositionality appreciation is carried out on a new compound produced. The method achieves the beginning design of the molecule under the condition that the three dimensional structure of the Danpabai is unknown, and the constructed molecule completely meets the requirement of the pharmacodynamic characteristic. The method is novel and has significant meaning.

The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.