44results about How to "Overcoming multidrug resistance" patented technology

The invention provides an anticancer intermediate based on PKI-587 and a polyethylene glycol coupled anticancer drug, and preparation methods and application thereof, belonging to the field of treatment of cancers. The anticancer intermediate has a general structural formula as described in the specification, and at least one AC in the general structural formula is the anticancer drug PKI-587. Thepolyethylene glycol coupled anticancer drug has a general structural formula as described in the specification. The above two drugs can realize combined medication of the targeting anticancer drug PKI-587 and a plurality of other anticancer drugs, so toxic response caused by mutual influence and pharmacokinetics of a plurality of other anticancer drugs can be prevented during individual administration of the anticancer drugs, multidrug resistance of cancers is overcome, and synergistic effect is exerted; and the two drugs can be used for preparing anticancer drugs with targeting effect and have critical clinical value and wide market prospects.

The invention discloses hyaluronic acid modified mitochondria target liposome and a preparation method thereof. The mitochondria target liposome disclosed by the invention is prepared from drug carrying liposome and outer-layer modifying hyaluronic acid, wherein the drug loading liposome is liposome covered by hydrophobic drug and dequalinium chloride, and the hydrophobic drug is any one chosen from adriamycin, taxol, 10-hydroxycamptothecine, irinotecan or cis-platinum. The hyaluronic acid modified mitochondria target liposome disclosed by the invention has the beneficial effects that receptors are effectively targeted, uptake of tumor cells to liposome is improved, cell mitochondria is further targeted in the tumor cells, a function of damaging the mitochondria is achieved, tumor cell apoptosis is promoted, tumor cell growth is inhibited, and ability of overcoming multidrug resistance of the tumor cells is achieved.

The invention belongs to the field of pharmaceutical preparations and the technical field of breast cancers, and discloses a preparation method and application of a soluble nano drug delivery system inhibiting multidrug resistance breast cancer growth. According to the preparation method and application, water-soluble super-molecular organic framework (SOF) nano particles server as carriers for the first time, the system is obtained through self-assembly of tetrahedral molecules obtained through tetraphenylmethane derivatization and CB[8] in a water phase, and chemotherapy drugs such as neutral drug doxorubicin and anionic drug pemetrexed disodium, folate derivatives, targeted integrin specific ligands such as RDG peptide derivatives and infrared probe molecules such as IR-820 can be loaded simultaneously; the SOF nano-drug carrier has the release characteristic of pH dependence, is accumulated in tumor tissue at high concentration, has a specific growth inhibiting effect on tumor cells with drug resistance in the tumor tissue due to P-glycoprotein overexpression and can obviously increase the retention volume of a chemotherapy drug in multidrug resistance breast cancer tissue, effectively inhibit the multidrug resistance breast cancer growth and significantly improve the curative effect on a multidrug resistance breast cancer.

The invention relates to a preparing method of a nanometer polymer micelle carrier integrating diagnosis and treatment. The method includes following steps of: (1) dissolving 0.1-1 part by weight of a hydrophobic anticancer medicine, 1-10 parts by weight of a magnetic resonance sensitive molecular probe, 4-40 parts by weight of polyethylene glycol-polycaprolactone end-capped with methoxy, 0.8-8 parts by weight of a polymer micelle with an active targeting group and 0.8-8 parts by weight of FITC-PEG-PCL into 1-100 parts by weight of tetrahydrofuran to obtain a mixture; (2) adding the mixture prepared in the step (1) into 5-800 parts by weight of deionized water, dialyzing and volatilizing to remove the organic solvent to obtain a targeted FA-NP/SPIO/PTX nanometer polymer micelle; and (3) subjecting the targeted FA-NP/SPIO/PTX nanometer polymer micelle prepared in the step (2) to filter membrane filtration and centrifugation to remove the unloaded or uncovered antitumor medicine so as to prepare the nanometer polymer micelle carrier integrating diagnosis and treatment, wherein the inner core of carrier carries the hydrophobic medicine and the magnetic resonance sensitive molecular probe, and the outer shell of the carrier is provided with the active targeting group.

The invention discloses a pH response type curcumin and succinic anhydride prodrug nanometer micelle and a preparation method and application thereof. The nanometer micelle consists of the following components in percentage by mass of 63.5%-91.9% of carrier auxiliary materials and 8.13%-39.5% of curcumin medicines. A nanometer micelle monomer is an amphiphilic block, and consists of a hydrophilicblock and a lyophobic block, wherein the hydrophilic block is succinic anhydride modified methoxyl polyethylene glycol, the lyophobic block is curcumin molecules, and the weight ratio of the hydrophilic block to the lyophobic block is (1 to 1) to (12 to 1). The pH response type curcumin and succinic anhydride prodrug nanometer micelle disclosed by the invention has the advantages that succinic anhydride sensitive to acid is designed and introduced at the end of the polyethylene glycol and is bonded with a lyophobic medicine namely the curcumin, and the formed amphiphilic polymer is self-assembled in an aqueous solution to form the nanometer micelle, so that the water solubility and the stability of an original medicine are increased; and the nanometer micelle monomer can degrade to releaseout cancer resisting medicines namely curcumin body medicines under the action of acid in cancer cells, so that pinpoint controlled release effects can be achieved.

The invention discloses composite micelle carrying an anti-tumor medicine and a preparation method thereof. The composite micelle is prepared from the following raw materials: pluronic, an amphiphilic block copolymer, an anti-tumor medicine, an organic solvent and water, wherein the mass ratio of the pluronic to the amphiphilic block copolymer is 1-1000:10; the mass ratio of the total mass of the pluronic and the amphiphilic block copolymer to the anti-tumor medicine is 2-100:1. The invention combines the advantages of the pluronic and the amphiphilic block copolymer, and the prepared composite micelle has uniform particle diameter and can overcome a multidrug resistance action. Fluorescent HPLC proves that the composite micelle can obviously increase the intracellular accumulation of the medicine and can be applied to the field of the reversion of the multidrug resistance of tumors. The invention has simple preparation method and very good application prospect.

The invention discloses a gold medicinal nano-carrier with double functions of overcoming and preventing P-glycoprotein-mediated tumor multidrug resistance. The gold medicinal nano-carrier is prepared by connecting a synergistic hydrophilic ligand for enhancing intake of nano-materials and a medicine-carrying ligand for carrying hydrophobic medicines to a gold nano-material by a ligand exchange method, wherein the synergistic hydrophilic ligand is a thiolated PEG 5000 (polyethylene glycol 5000) molecule with electropositive amino group at the terminal, and the medicine-loading ligand is a thiolation modified beta-cyclodextrin molecule; the gold medicinal nano-carrier is of a spherical shape. Experiments prove that a paclitaxel-loaded gold medicinal nano-carrier prepared by adsorbing the gold nano-carrier to paclitaxel can be used for effectively killing cells with P-glycoprotein drug resistance, can avoid drug resistance generation while killing cells without P-glycoprotein drug resistance, and provides a new thought and new direction to nano-medicine loading methods in overcoming tumor multidrug resistance.

The invention discloses a cationic polymer for co-loading drugs and genes and application of the cationic polymer. A constructed cationic PCL-ss-P (GHA-co-PEGMA) polymer is rich in side chains, so that the polymer has good biocompatibility and water solubility; in addition, a shell layer is rich in hydroxy groups, which can promote transmembrane transport of a drug/gene complex and improve the transcription and expression of the genes in cells. Under the condition of higher glutathione, cracking of a main chain in the drug/gene complex is caused, and the release of drugs in polymeric micellesis caused, thereby achieving the purpose of inhibiting tumor cell proliferation. The release of the drugs and the transcription and expression of the genes can be combined to treat the lung cancer, and the drug resistance of anti-cancer drugs in the cells is effectively overcome. The cationic polymer for the co-loading drugs and genes and the application of the cationic polymer have the advantagesthat the used experimental conditions are milder, the structure of the cationic polymer is easy to control, the operation is simple, the raw materials are easy to obtain, purification is easy, and the cationic polymer is suitable for industrial production; therefore, the cationic polymer can be used as a common carrier of the anti-cancer drug and cancer suppressor genes, and has a larger market application prospect in the future.

The invention relates to the technical field of medical nano-materials, in particular to a magnetic nano-drug carrier based on a porous gadolinium-doped iron oxide nano-cluster and a preparation method of the magnetic nano-drug carrier. The magnetic nano-drug carrier is characterized in that the gadolinium-doped iron oxide nano-cluster serves as a core, the surface area of the gadolinium-doped iron oxide nano-cluster is large, the surface of the gadolinium-doped iron oxide nano-cluster is rich in hydroxyl, and particularly, the gadolinium-doped iron oxide nano-cluster synthesizing a mesoporousstructure can load high-content anti-cancer drugs. According to the drug carrier, a peripheral degradable shell layer can effectively prevent non-specific release of the anti-cancer drug, and after the drug reaches a target site, the shell layer material is degraded through pH value and external near-infrared light stimulation, the gadolinium-doped iron oxide nano-cluster loaded with the drug isexposed, and the drug release is realized; and meanwhile, the gadolinium-doped iron oxide nano-cluster shows excellent magnetization intensity due to the characteristic that sub-nanoparticles of the gadolinium-doped iron oxide nano-cluster are closely integrated, and can be applied to a T1-T2 magnetic resonance image contrast agent.

The invention provides an application of jervine to preparation of a multidrug resistance reversal agent for a tumor. When jervine is jointly used with other tumor chemotherapeutic drugs, the killing effect of the chemotherapeutic drugs on drug-resistant tumor cells can be improved obviously, dosage of the tumor chemotherapeutic drugs can be reduced, and the toxic effect of the chemotherapeutic drugs is reduced. The unique action mechanism of jervine is as follows: jervine can inhibit transport of ABCs (ATP-bindingcassette transporters) such as P-gp, ABCG2 and the like, reduce efflux of the chemotherapeutic drugs by the tumor cells, increase concentration of the chemotherapeutic drugs in the cells and induce apoptosis of the drug-resistant tumor cells, so that the multidrug resistance of the tumor cells is overcome. Jervine can be combined with other chemotherapeutic drugs for preparation of a compound drug for overcoming multidrug resistance of the tumor and has broad application prospect.

The invention discloses a medicine for assisting in treating a breast cancer and a preparation method of the medicine. The medicine comprises the following raw materials in parts by weight: 25-60 parts of centipede extract, 12-35 parts of angelica sinensis, 18-29 parts of selfheal, 12-30 parts of akebiaquinata, 11-28 parts of ormosia, 8-19 parts of codonopsis pilosula, 7-22 parts of glycyrrhiza uralensis, 6-21 parts of rhubarb, 8-22 parts of astragalus mongholicus, 9-23 parts of ginseng, 7-20 parts of nightshade and 6-19 parts of oolong tea. The prepared medicine for assisting in treating thebreast cancer can assist in western medicine treatment of the breast cancer, particularly can effectively eliminate or inhibit tumor development for late-stage patients incapable of undergoing surgery, chemotherapy and radiotherapy, improves clinical symptoms of the patients, reduces toxic and side effects of the chemotherapy and the radiotherapy, overcomes multidrug resistance of tumor cells, regulates immunologic mechanisms of bodies, improves curative effects of the surgery, the chemotherapy and the radiotherapy, improves the life quality of the patients, and prolongs the life time.

The invention discloses a metal organic framework coated nano-particle capable of automatically supplying H2O2/O2 and consuming GSH and a preparation method and application of the metal organic framework coated nano-particle. The metal organic framework coated nano-particle is a core-shell structure compound and comprises a calcium peroxide nano-particle inner core, a calcium peroxide nano-particle outer core and a metal organic framework coated nano-particle inner core, the periphery of the calcium peroxide nanoparticle core is coated with the metal organic framework shell, and pores of the metal organic framework are loaded with a photosensitizer; and the phase change material is modified on the peripheral surface of the metal organic framework shell. The prepared nano-particles automatically supply H2O2/O2 and consume GSH, can effectively enhance the PDT/CDT curative effect, can be combined with chemotherapy drugs to amplify chemotherapy, avoids multi-drug resistance, and realizes multi-mode synergistic therapy of tumor photothermal therapy, photodynamic therapy, chemical dynamic therapy and chemotherapy.

The invention discloses a preparation method of TiO2 nanoparticles capable of overcoming multidrug resistance of tumor. The preparation method comprises the steps of forming empty TiO2 nanoparticles with effective pH gradient, encapsulating anthracycline antitumor drugs into the TiO2 nanoparticles, and thus preparing the anthracycline anti-tumor drug TiO2 nanoparticles. The preparation method hasthe advantage of simple preparation, can significantly improve the encapsulation efficiency of the anthracycline antitumor drug, and effectively omits recognition, binding and discharging of multidrugresistance related proteins of drug-resistant cells through the encapsulation technology, so as to effectively enhance the drug amount of drugs in the drug-resistant cells, prolong the drug retentionin the drug-resistant cells and indicate relatively good tumor MDR-overcoming effect. Compared with other methods, the method provided by the invention is simple and convenient, can delay the releaseof the drugs in a culture medium, and can co-carry other tumor MDR-overcoming drugs, has low requirements for preparation materials, has high encapsulation efficiency, and can effectively overcome multi-drug resistance.