66results about How to "Achieve targeted drug delivery" patented technology

The invention relates to a multifunctional double-layer core-shell structure magnetic nano particle. In the invention, a magnetic nano particle with a particle size of 1-300 nm is used as a core and coated with a double-layer shell consisting of a SiO2 layer with a thickness of 1-200 nm and a hydrolyzed silane coupling agent layer is 1-100 nm thick and comprises one or more multifunctional groups; the particle size and the shell layer thickness can be controlled through regulating the volumes, the weight ratios and the reaction time of the magnetic core, a silicon dioxide precursor, a silane coupling agent and a catalyst in a preparation process; the total particle size of the nano particle can be as small as 5-50 nm and as large as 700-800 nm; the nano particle can have superparamagnetism, paramagnetism and ferromagnetism according to the change of the magnetic core particle size; and one or more bioactive molecules can be connected into the shell layer of the magnetic nano particle or to the surface of the shell layer through a chemical method or a physical method. The invention also provides a preparation method of the multifunctional double-layer core-shell structure magnetic nano particle and application thereof. The particle preparation method has the advantages of simplicity, moderate condition, low cost and easy realization of industrial production. The nano particle can obtain different functions through connecting different bioactive molecules and can be applied to the fields of protein enrichment, biological detection, separation and purification, targeted drug carriers, cell imaging and medical imaging.

The invention discloses a double aptamer modified mesoporous silica targeted drug-loading nanoparticle and preparation and application thereof. The targeted drug-loading nanoparticle is composed of mesoporous silica nanoparticles, anti-cancer drugs coated and carried in the pore channels of the mesoporous silica nanoparticles and two types of nucleic acidaptamers modified on the surfaces of the mesoporous silica nanoparticles and capable of specifically identifying specific proteins on the surfaces of cancer cells. The targeted drug-loading nanoparticle can identify tumor sites and cancer cells circulated in blood in a targeted mode and can be used for preparation of drugs for preventing and treating tumor metastasis.

The invention belongs to the field of preparation of targeted therapeutic microspheres of slow release formulation and in particular relates to a preparation method of taxol-loading polylactic acid-hydroxyacetic acid (PLGA) microspheres. The preparation method comprises the following steps: dissolving a polylactic acid-hydroxyacetic acid copolymer in an organic solvent, and adding a taxol drug, wherein the polymer and the taxol drug are uniformly dissolved to obtain an organic phase; dropwise adding the organic phase into a fresh polyvinyl alcohol aqueous solution and curing and forming microspheres; and performing centrifugal separation on the cured drug-loading microspheres to obtain the uniformly dispersed taxol-loading polylactic acid-hydroxyacetic acid (PLGA) microspheres. The taxol-loading targeted therapeutic PLGA microspheres prepared by the preparation method have an ideal drug loading ratio and encapsulation efficiency while guaranteeing the drug stability of taxol, can reach an effect of slow release, maintain the optimum drug concentration in vivo, prolong the action time of the drug and reduce the side effects brought by burst release of the drug, and have important theoretical value and actual application prospect.

The invention relates to a natural pullulan nano drug carrier, which is made of carboxymethylation pullulan and hydrazine under condensation reaction, wherein the condensation reaction degree of carboxyl of the carboxymethylation pullulan with amino of the hydrazine is 60-90%. The carriers with drug are automatically combined in water to form nano particles with particle size ranging from 60nm to 200nm. The preparation method includes the steps: firstly, preparing carboxymethylation pullulan; and secondly, using deionized water to make the carboxymethylation pullulan into solution with concentration being 0.01-0.10g/ml, using deionized water to make hydrazine into solution with concentration being 0.1-0.5g/ml, mixing while adding carboxymethylation pullulan aqueous solution into the hydrazine solution at room temperature and normal pressure, well mixing, adding 1-(3-dimethylamino propyl)-3-ethyl carbodiimide hydrochloride aqueous solution with concentration being 0.5-1g/ml, mixing for reaction for two to six hours, using deionized water for dialyzing to remove micromolecular impurities after reaction is completed, and freeze drying to obtain the natural pullulan nano drug carrier.

A biodegradable polyester microparticle or microsphere for controlling the release of medicine is prepared from levo-and dextro-cubic polyblock polylactide through cooling method, solvent voltilizing method, or non-solvent depositing method.

The invention relates to the technical field of polymer materials, and particularly relates to preparation and application of a mixed structure PLGA-PLL-PEG (Polylactide Acid Glycolic Acid-Polylysine-Polyethylene Glycol) targeting polymer carrier. The preparation is characterized in that polylactide acid glycolic acid and side chain protected polylysine are acted by a dehydrating agent and then connected in the block way to form a midbody; the midbody is deprotected and then connected with activated polyethylene glycol in the grafting manner, so that the polylactide acid glycolic acid-polylysine-polyethylene glycol polymer having the molecular weight of 4*10 <4> to the power of 4 to 5*10<5> is obtained. The polymer is used for carrying various medicines and also capable of being coupled with various ligands to realize targeted medicine delivery. The preparation of the polymer carrier provided by the invention is few in synthesis steps, mild in reaction conditions, available in materials and convenient for product purification.

The invention relates to a tumor cell active targeting drug delivery system based on nanometer particles and a construction method thereof. The tumor cell active targeting drug delivery system is characterized by using the nanometer particles with photocatalytic performance as carriers to obtain targeted molecule/nanometer particle/chemotherapy drug compounds in a physical absorption or chemical bonding mode, the mole ratio of the nanometer particles and targeted molecules is 50:1-20:1, the mole ratio of the nanometer particles and chemotherapy drugs is 50:1-10:1. The tumor cell active targeting drug delivery system integrates the chemotherapy drugs, the targeted molecules and the nanometers particles with photocatalytic performance, enables a nanometer particle dry carrying system to have active tumor cell targeting capacity, effectively reduces side effects of the chemotherapy drugs, can realize controllable release of the chemotherapy drug and reverse multiple drug resistance of the tumor cell, and is simple and easy in construction method, low in cost, and favorable to industrialized production and market popularization.

The invention provides a carfilzomib prodrug with a structural formula (I). The invention uses a short-chain PEG molecule as a hydrophilic end, and carfilzomib as a hydrophobic end; and the two parts are connected by L-leucine in the form of imine, so as to prepare a novel carfilzomib prodrug. The carfilzomib prodrug improves the water solubility, is easy for preparation into high-concentration solution, and can be produced into a finished product with enhanced stability by freeze-drying. At the same time, the carfilzomib prodrug is a compound sensitive to acid, maintains stability in blood (alkaline) circulation, and can quickly release carfilzomib drug once arriving in the tumor tissue (acidic), in order to achieve targeted drug delivery, enhance curative effect of chemotherapy and reduce side effects.

The invention relates to a method for preparing sulfuric (sulfonic acid) esterification PEG liposome derivate, and relative application in drug transmitter, especially the application of novel polyethylene glycol dimethyl ether cholesterol sulfate derivate in medical aera. The inventive sulfuric (sulfonic acid) esterification PEG liposome derivate is sulfuric (sulfonic acid) esterification PEG cholesterol, sulfuric (sulfonic acid) esterification PEG sterol, sulfuric (sulfonic acid) esterification PEG tocofecol, sulfuric (sulfonic acid) esterification PEG vitamin D, sulfuric (sulfonic acid) esterification PEG phosphatide, or sulfuric (sulfonic acid) esterification PEG-DSPE. And the drug transmitter comprises a gel beam, a nanometer gel beam, an emulsifier, a micro emulsifier, a nanometer emulsion, a liposome, and nanometer particles. The invention esterificates and connects the PEG sulfuric (sulfonic acid) with cholesterol to prepare derivate, to protect drug, reduce degradation, and prolong the circulation time in body, and realize the combination with gp120 specificity at the surface of HIV, to transmit drug targeted.

The invention discloses a method for preparing targeted controlled release aspirin powder. The preparation process comprises the following four steps: preparing a magnetic core-shell nano-silica drug carrier, partially dissolving a magnetic core, loading aspirin on the magnetic drug carrier and performing secondary coating of the aspirin. According to the invention, the magnetic core is partially dissolved by adopting an acid-soluble mode, the cavity diameter of the magnetic core-shell nano-silica is enlarged, and the drug loading capacity is improved. The aspirin-loaded drug is subjected to secondary coating by using polyvinylpyrrolidone polymer sol, and the pore density on the silica shell is reduced. The problem that the conventional slow release aspirin drug is extremely high in release speed is solved, and long-lasting release and controlled release can be realized. The drug carrier has magnetic property, the drug can reach the target tissues under guide of a magnetic field, targeted drug delivery is realized, and the treatment efficiency is improved.

The invention relates to a Bola type ribavirin compound. A structure is shown as a general formula I. Through studying the characteristics of the special structure of the Bola type amphiphilic molecules, the structure optimization is performed by aiming at 1, 2, 4-ribavirin; the water solubility and the cancer cell growth inhibition rate of the compound are improved. Further, the compound has the capability of forming nanometer scale particles through self assembly in a water solution, so that the compound can be more easily gathered into the tumor tissues to realize the targeted medication through high permeability of the solid tumor and the retention effect. Meanwhile, as a nanometer medicine carrier, the compound can also encapsulate and seal other micromolecular medicine to reach the combined medication effect. In the general formula, n, R1, R2, R3 and R4 are defined as the patent claim. The formula I is shown as the accompanying drawing.

The invention provides a combination of autologous blood activating transfusion medicine, microecologics and nano-traditional Chinese medicine.The autologous blood activating transfusion medicine is adopted once or twice every half month, 1-2 g of the microecologics are taken twice every day, 1-3 g of the nano-traditional Chinese medicine is taken twice or three times every day, and each course lasts for 10-15 days.The autologous blood activating transfusion medicine can activate hemocyte metabolism, the immune system and the antioxidase system, improve the state of the blood vessel wall and enhance the physiological function of hemocytes; the microecologics can regulate the balance of intestinal flora, maintain normal physiological metabolism of a human body, accelerate normal metabolism of the human body, promote discharge of toxins in the intestinal tract and decompose blood fat waste accumulated in the human body; the nano-traditional Chinese medicine has high solubility, absorbance, adsorption strength, bioavailability and permeation strength, and fast, efficient, long-acting and targeted treatment can be realized; the autologous blood activating transfusion medicine, the microecologics and the nano-traditional Chinese medicine are applied in a combined mode to jointly achieve the purposes of preventing and treating cardiovascular and cerebrovascular diseases and enhancing immunity.

The invention relates to a preparation method of urushiol-loading pH responsive amphiphilic copolymer micelle. The preparation method comprises the following steps: firstly, dissolving a certain amount of mPEG, hydrophobic amine monomer, 5-amino-1-pentanol and 1,4-butanediol diacrylate in DMSO to prepare a reaction solution with a certain concentration, performing polyreaction for 20-48h, then adding a certain amount of 1,3-pentanediamine, and continuing the reaction for 24h to synthesize polyethylene glycol-poly-beta-amino ester amphiphilic copolymer (mPEG-PBAE); and then taking and dissolving a certain amount of mPEG-PBAE and urushiol in DMF, performing uniform ultrasonic mixing, and performing dialyzing, centrifuging and filtering to obtain the urushiol-loading pH responsive amphiphiliccopolymer micelle. The drug-loading micelle has an average particle diameter of 140-160nm, good stability, obvious pH responsive drug-release property, good biocompatibility, and good targeting anti-tumor activity, can be applied to clinical targeting anti-tumor drugs, has very high added value, and can become a new technique for clinically developing urushiol targeting anti-tumor drugs.

The invention relates to a reduced response-type amphiphilic polymer prodrug and a preparation method and an application thereof. The prodrug has a molecular structure as a formula I, wherein X is O or NH, ROH is a hydrophobic antitumor drug, n is from 5 to 1,000, and m is 1 or 2. The prodrug provided by the invention can achieve targeted administration, which not only retains the advantages of anano drug-loading system, but also exhibits the characteristic of specific degradation of a disulfide bond at the tumor site. Compared with conventional 2,2'-disulfanediyldiacetic acid, 3,3'-dithiodipropionic acid and other connecting arms, the prodrug and the preparation method thereof have the advantage that an anticancer drug with an original drug molecular form can be obtained without furtherhydrolysis.

The invention discloses an imidacloprid and moxidectin dihydric alcohol plastid and a preparation method and application thereof. An insect repellent preparation is prepared from the following components: imidacloprid, moxidectin, soybean lecithin, dihydric alcohol (including ethanol and propylene glycol), polysorbate-80 and a phosphate buffer solution. It is confirmed by animal experiments that the imidacloprid and moxidectin dihydric alcohol plastid preparation has the effect of resisting in-vivo and in-vitro parasite infection in dogs and cats. Meanwhile, compared with an imidacloprid and moxidectin compound transdermal agent, the toxicity of the imidacloprid and moxidectin dihydric alcohol plastid preparation is greatly reduced, and the advantages such as good skin permeability, biologically slow release, longer action time and comparatively excellent treatment effect are achieved.

The invention provides a digoxin lipid microbubble. The digoxin lipid microbubble comprises a lipid bilayer membrane, gas and digoxin-loaded albumin nanoparticles, wherein the gas and the digoxin-loaded albumin nanoparticles are packaged in the lipid bilayer membrane. The digoxin lipid microbubble has relatively high drug loading capacity and encapsulation efficiency, the plasma concentration of a target position can be increased, the action time of drugs at the target position can be prolonged, the degradation of drugs can be reduced, the stability of the drugs can be improved; furthermore, by virtue of the nanoparticles, the selective distribution of the drugs can be promoted, the drugs is beneficially transferred into diseased tissues, the pesticide effect can be increased, and toxic and side effects can be reduced. The invention further discloses a preparation method of the digoxin lipid microbubble. The preparation method is simple in process and easy to industrialize, chemical reactions are not involved in the preparation process, and high-toxicity organic solvents are not utilized, so that the preparation method is high in safety and environmental friendliness.

The invention relates to bola type quercetin derivatives and a preparation method thereof. A bola type amphiphilic molecule is formed by connecting two polar head groups by using a hydrophobic chain; and unique natures such as better stability and compatibility in a plasma membrane are given to the bola type amphiphilic molecule through the special structure. The bola type quercetin derivatives shown as general formulas I-V are developed by utilizing bola type characteristics to increase the water solubility and the bioavailability of the derivatives; meanwhile, proved by research results, compared with non-bola type quercetin lipid derivatives, the bola type quercetin derivatives are capable of better inhibiting the growth activity of tumor cells; the bola type quercetin derivatives are transformed into nanometer drugs through micromolecule self-assembly on the basis of the structure to improve the physicochemical property of compounds; the ability of targeting focal tissues is enhanced and the damage of the drugs to normal tissues and cells is reduced; and R and n in the general formulas are defined as the claim.

The invention provides a liposome drug carrier combined with a blood cell membrane as well as a preparation method and application of the liposome drug carrier, and belongs to the technical field of biological materials. The liposome drug carrier disclosed by the invention is obtained by mixing liposome and blood cells; the lipidosome is adhered to the surface of a blood cell membrane or the lipidosome is fused with the blood cell membrane. The liposome drug carrier combined with the blood cell membrane is prepared, the liposome drug carrier can carry different kinds of drugs, the drug encapsulation efficiency and the drug loading capacity are high, and the delivery efficiency of the drugs can be effectively improved. Meanwhile, according to the drug carrier disclosed by the invention, the liposome is combined with cell membranes of blood cells with biological activity, and the combined blood cells can still keep complete morphology and good activity and functions, so that the half-life period of the drug can be effectively prolonged, and the elimination of an autoimmune system can be better avoided; more effective drug sustained release and clinical treatment effects are achieved with a lower drug dosage, and good application prospects are achieved.

The invention relates to a novel electrostatic spinning drug administration device, belongs to the technical field of drug administration devices, and provides the novel electrostatic spinning drug administration device with good use effect. The novel electrostatic spinning drug administration device includes a shell, a liquid supply drug administration system, a gas generation device and a high-voltage power supply generation device 17, and is characterized in that the shell is provided with an air outlet 10, an air inlet 9 and a spinning nozzle 14, the air inlet 9 is connected with the air outlet 10 through the gas generation device, and the air outlet 10 is formed in the periphery of the spinning nozzle 14; and the high-voltage power supply generation device is connected with a power supply port of the spinning nozzle 14, and the liquid supply drug administration system is connected with a drug administration input port of the spinning nozzle 14.

The invention discloses a traditional Chinese medicine composition with an anti-cancer effect and an anti-cancer traditional Chinese medicine implant, and relates to a traditional Chinese medicine composition and an implant. The problems that an existing traditional Chinese medicine composition is low in lung cancer cell proliferation inhibition rate and unstable in implant release rate are solved. The traditional Chinese medicine composition is prepared from a traditional Chinese medicine extract, atractylenolide I and crocin. The preparation of the implant comprises the steps: dissolving the PLGA and the mannitol in an organic solvent, adding the traditional Chinese medicine composition, performing drying, performing forming, performing sub-packaging and performing sterilizing. The auxiliary release device containing the anti-cancer traditional Chinese medicine implant is composed of a medicine storage bin, foamed plastic, the flaky anti-cancer traditional Chinese medicine implant and a mesh, the traditional Chinese medicine composition can inhibit proliferation of tumor cells and has low toxic and side effects, and the auxiliary release device ensures that the release rate is constant.

The invention provides a vincristine lipid microbubble. The vincristine lipid microbubble comprises a lipid bilayer membrane, gas, albumin nanoparticles for carrying vincristine; and the gas and the albumin nanoparticles for carrying the vincristine are wrapped by the lipid bilayer membrane. The vincristine lipid microbubble has the higher medicine loading capacity and the higher encapsulation efficiency; the blood concentration of target positions can be improved; the action time of medicines at the target positions is prolonged; the medicine degradation is reduced; and the medicine stability is improved. In addition, the nanoparticles have the beneficial effects that the selective distribution of the medicines is promoted; the medicines are better transmitted to enter lesion tissues; the pesticide effect can be improved; and the toxic and side effects can be reduced. The invention further discloses a preparation method of the vincristine lipid microbubble. The preparation process is simple; industrialization is easily achieved; the preparation process does not relate to chemical reactions; organic solvents with high toxicity are not adopted; the safety performance is high; and the environment friendliness is high.

The invention discloses a nano drug carrier targeting to a central nervous system. The nano drug carrier includes nano-micelles, nano-lipidosomes, nano-particles and the like, takes apamin or an apamin derivative exposed on the surface of the carrier as a targeting ligand, can carry a small-molecule chemical drug to cross blood brain barrier and blood spinal cord barrier, thereby realizing the central nervous system targeting drug administration, wherein the apamin derivative has a peptide chain C end without amidation.