37results about How to "Reverse multidrug resistance" patented technology

The invention discloses an application of nanometer structure lipid carrier administration system in the antineoplastic drug to reverse the multiple-drug tolerance of tumour cell, which comprises the following parts: solid lipid material, liquid lipid material and antineoplastic drug, wherein the rate of the liquid lipid (such as oleic acid) is 0-30wt%; the solid lipid is selected from monoglyceride; the liquid lipid is oleic acid; the antineoplastic drug is Paclitaxel or adriablastina. The invention has highly effective cell uptaking and cytolymph condensing function with packing molecular target in the antineoplastic drug of cell, which avoids P-glucoprotein in the drug tolerant cytolymph from identifying the antineoplastic drug to reduce exclusion.

The invention relates to the field of nanometer drug carriers, and concretely relates to an asymmetric magnetic mesoporous silica rod supporting chemotherapeutic and gene drugs and application thereof to tumor diagnosis and treatment. The asymmetric magnetic mesoporous silica rod is prepared by employing spherical magnetic ferrite nanoparticles and ethyl orthosilicate through a sol-gel method, and the asymmetric magnetic mesoporous silica rod is subjected to surface functionalization modification, and is successively loaded with a chemotherapeutic drug, coated by a positive high-molecular polymer and loaded with a gene drug, so that a target product is obtained. The chemotherapeutic drug is connected with the silica rod through functionalization of the mesoporous surface, and the silica rod is endowed with the pH-responsive drug release characteristic, also the biocompatibility of the composite material is increased and the in-vivo cycling time is prolonged, and gene is supported in an electrostatic adsorption mode. The composite material is injected into a living body via an intravenous route, the characteristics of nanoparticle in-vivo passive targeting, gene guiding and pH-responsive drug release of the composite material are utilized, also the cooperativity of the multidrug resistant gene and the chemotherapeutic drug is utilized, and in-vitro magnetic targeting, NMR imaging and other technologies are applied to diagnosis and treatment of malignant tumors.

The invention discloses an adriamycin nano drug delivery system as well as a preparation method and application thereof. The drug delivery system comprises the following components in percentage by weight: 0.02%-1.5% of active ingredient containing adriamycin, 1%-20% of solid lipid, 0.1%-20% of liquid lipid, 0.5%-20% of emulsifier and 0.1%-5% of isoosmotic adjusting agent, wherein the solid lipid and the liquid lipid form nanoparticles to cover the active ingredient containing the adriamycin. The preparation method comprises the following steps: (1), uniformly dispersing the active ingredient containing the adriamycin, the solid lipid, the liquid lipid and fat-soluble emulsifier in an organic solvent, evaporating the organic solvent to obtain an oil phase; (2), uniformly dispersing other emulsifiers and the isoosmotic adjusting agent in water to obtain a water phase; (3), adding the water phase into the oil phase for emulsifying drop by drop; (4), homogenizing under high pressure; (5), cooling and degerming. The adriamycin nano drug delivery system disclosed by the invention can be used for realizing co-transporting of the adriamycin and a chemosensitizer, so that the killability of the adriamycin on liver cancer cells is strengthened.

The invention belongs to the field of pharmacology, and discloses new application of brevifolin used for preparing a sensitizer or a reversal agent of an antitumor drug. The invention discloses the new application of the brevifolin in improving the sensibility of tumor to the antitumor drug, and can effectively reverse multi-drug resistance of the tumor to the anti-tumor drug. Furthermore, the brevifolin has low toxicity and abundant resource, and has excellent medicinal prospect.

The present invention relates to compounds, compositions for use in reversing multidrug resistance in cancer cells, process for the preparation thereof and their uses in treating cancers. More particularly, the present invention relates to 3′,4′-aromatic acyloxy substituted 7,8-pyranocoumarins compounds for use in reversing P-glycoprotein overexpression mediated multidrug resistance in cancer cells, pyranocoumarins containing compositions, process for the preparation thereof and their uses in treating cancers.

The invention belongs to the technical field of pharmaceutical chemicals and discloses segmented copolymer - docetaxel combination, a preparation thereof and a preparation method thereof. The combination is combined by bonding polyoxyethylene - polypropylene oxide - polyoxyethylene (PEO- b - PPO - b - PEO with a product name as Pluronics (BASF company)) triblock copolymer and docetaxel through ester bond, and the Pluronics - docetaxel combination is obtained. By utilizing amphipathy of the combination and adopting physical methods to prepare micelle aqueous solution, a freeze-dried preparation can also be prepared. Nanomicelle is capable of gathering at tumor parts through 'enhanced permeation and retention effects (EPR effects)', and tumor targeting of docetaxel is enhanced. Besides, an active targeting factor is connected on Pluronics polymer so as to have the function of active targeting. The segmented copolymer - docetaxel combination overcomes the defects that existing docetaxel injection is poor in water-solubility and severe in allergic reaction and the like.

The invention provides an oxaliplatin chitosan-stearic acid grafting micelle which comprises 0.5 percent of chitosan-stearic acid grafting, 0.009-0.02 percent of oxaliplatin, 0-0.2 percent of lecithin and the balance of water. The oxaliplatin chitosan-stearic acid grafting micelle is respectively prepared by using a probe ultrasonic method, a film dispersion method and a lecithin mediated film dispersion method. The oxaliplatin chitosan-stearic acid grafting micelle has rapid ingestion function of passive targeting and cancer cells in a polymer micelle, can greatly improve the intracellular medicine concentration of a molecular target in the oxaliplatin in the cancer cells by encapsulating the oxaliplatin chitosan-stearic acid grafting micelle on the oxaliplatin, improves the cytotoxicity and shifts the multidrug resistance, and enhances the clinical anti-tumor efficacy of the oxaliplatin. The oxaliplatin chitosan-stearic acid grafting micelle can be applied to preparing an anti-tumor medicine.

The invention discloses a folic acid targeted modified co-loaded doxorubicin hydrochloride and gambogic acid nanostructure lipid carrier preparation. In the embodiment, the preparation is prepared from 0.01 to 1 part of doxorubicin hydrochloride, 0.01 to 1 part of gambogic acid, 0.01 to 2 parts of phospholipid-polyethylene glycol-folic acid, 0.1 to 10 parts of solid lipid, 0.1 to 5 parts of liquidlipid, 0.1 to 3 parts of a lipid-soluble emulsifier and 1 to 10 parts of a water-soluble emulsifier. The invention further discloses a preparation method of the preparation. The nano preparation prepared by the method has the advantages of smaller particle size, even distribution, good stability and higher encapsulation efficiency; furthermore, the nano preparation improves water insolubility ofgambogic acid, prolongs drug residence time and has better active targeting; two drugs synergistically play curative effects, so that antineoplastic activity is enhanced, chemotherapeutic medicine dosage is reduced, and bioavailability is improved; meanwhile, multidrug resistance generated by the doxorubicin hydrochloride is inverted.

The invention discloses a pH response type amphipathic stem-grafting polyphosphazenes feeding micelle containing 70%-99.999% of pH response type amphipathic stem-grafting polyphosphazenes and 0.001%-30% of at least one hydrophobic medicament by the total weight of the medicament and the pH response type amphipathic stem-grafting polyphosphazenes, wherein the hydrophobic medicament is a hydrophobic anti-tumor medicament or a hydrophobic chemotherapeutic medicament. The micelle can be prepared by using a film hydration method or a dialysis method and can exist in a state of aqueous dispersion or frozen dry powder. The medicament of the micelle has pH response when released, the micelle can rapidly release the medicament nearby tumor tissues or in tumor cells at fixed points to reverse the multi-medicament resistance of the tumor cells, and meanwhile, the amphipathic stem-grafting polyphosphazenes has good biocompatibility and less toxicity and is suitable for being used as a targeting carrier of the anti-tumor medicament.

The invention discloses a medicine carrier system. Prussian blue modified by carbon quantum dots and beta-cyclodextrin is used as a substrate; a product is obtained through the combination with NO donor 5-chloro-2-nitrophenyl trifluoromethane grafted polylysine after the modification by folic acid. The medicine carrier system provided by the invention can realize the effective enriching in the tumor positions through folic acid targeting and tumor position EPR effect; under the near infrared laser irradiation, Prussian blue nanometer particles can melt tumor cells through high photothermal conversion efficiency. Meanwhile, the medicine carrier system can control the release of nitric oxide under the illumination condition of the wavelength being 400nm, so that the enrichment of the nanometer particles in the tumor positions through the EPR effect can be improved; meanwhile, NO can achieve the effect of inhibiting the tumor growth through inducing the tumor cell apoptosis, reversing multidrug resistance and the like.

The invention discloses a biologically responsive nitric oxide donor type polymer prodrug and a preparation method thereof, wherein the polymer prodrug is obtained by connecting a hydroxyl-containing chemotherapeutic drug and a nitric oxide donor type polycarbonate macromolecule through a tumor microenvironment acid responsive acetal bond, and then the polymer prodrug nano-drug is obtained through self-assembly. According to the invention, chemotherapeutic drugs are modified, and a nitric oxide donor is introduced to a polymer carrier material, so that the nitric oxide donor type polymer prodrug with high drug loading capacity, high stability and biological response is prepared, drug sensitization and synergistic treatment effects are realized, and the prodrug has a wide application prospect in the aspect of efficient anti-tumor.

The present invention relates to a preparation extracted from Stephania tetrandra S. Moor and its use for manufacture of medecine for enhancing the sensitivity or effect of chemotherapy, enhancing the sensitivity of radiotherapy, improving the level of leukocytes in body, and having antineoplastic and antianaphylaxis effects. Said preparation is mainly composed of tetrandrine and fangchinoline with the ratio of 9:1 to 8:2 (moles), which is obtained by the following process: (1) the powder or piece of Stephania tetrandra S. Moor is extracted with dilute acid with the cool acid extract being collected; and washed with water with the aqueous extract being collected; then the cool acid extract and aqueous extract are combined, adjusted with base pH 10 to 12, kept overnight; (2) the fluid of Step (1) is filtered, the solid dried, pulverized to give Powder 1; (3) Powder 1 is heated under reflux in alcohol for 30 min.; (4) the alcohol extract from Step (3) is concentrated, kept, filtered to give Solid 2; (5) Solid 2 is dissolved in warm ammoniac ethanol, kept for crystallization. The present invention also relates to the use of tetrandrine and the pharmaceutically acceptable salt thereof for manufacture of medecine for improving the level of leukocytes in body.

The invention discloses a targeted drug co-delivery nano system. The nano system is characterized in that a nano co-carrier with relatively strong drug loading capacity is formed by coating gold nanorods with mesoporous silica, and targeted co-delivery of a chemotherapeutic drug PTX and a gene drug miR let-7alpha is realized by combining modification of amino, PEG and HA. The invention also discloses a preparation method of the targeted drug co-delivery nano system. The method is simple to operate, and the size of the prepared product is controllable. The invention also discloses application of the targeted drug co-delivery nano system in preparation of drugs for treating ovarian cancer. The co-delivery nano system realizes effective delivery of chemotherapeutic drugs and gene drugs, can target tumor tissues, increases permeability of tumor parts, promotes drug uptake of cancer cells, and is beneficial to improvement of drug effect, reversal of multidrug resistance of ovarian cancer tissues and enhancement of PTX treatment effect, thereby improving treatment efficiency. A new thought is provided for treating the ovarian cancer.

The invention belongs to the field of biological medicine, and particularly relates to a pharmaceutical composition containing a PI3K inhibitor and application of the pharmaceutical composition. The composition comprises an effective quantity of the PI3K inhibitor, an effective quantity of an HSP90 inhibitor and a pharmaceutically acceptable carrier. The pharmaceutical composition containing the PI3K inhibitor has a remarkable treatment effect on esophageal cancer cells, lung cancer cells, gastric cancer cells and liver cancer cells, is low in toxicity to normal cells, has a remarkable inhibition effect on proliferation and migration of the esophageal cancer cells, and can remarkably improve expression of Cleaved-PARP and promote apoptosis at the same time. According to the pharmaceutical composition containing the PI3K inhibitor, the bioavailability of drugs is improved, the drug effect can generate a synergistic interaction effect, and the drug resistance treatment effect on tumors is obviously superior to that of a single drug.

The invention discloses a detoxication preparation which is prepared from the following raw materials (by weight portions): astragalus root 12-30 parts, sun-dried ginseng 1.5-12 parts, fleece-flower root 6-15 parts, white atractylodes rhizome 6-30 parts, rhizome smilacis glabrae 15-60 parts, campeachy wood 3-10 parts, bistorta 4.5-15 parts, psoralea fruit 6-12 parts, golden buckwheat rhizome 6-30 parts, Marsdenia tenacissima 6-30 parts, licorice 3-12 parts.The invention also discloses its preparation.

The invention belongs to the technical field of medicine application, and discloses an application of trametinib in preparing a medicine for reversing multi-medicine resistance of tumors. Trametinib can be used for significantly reversing the multi-medicine resistance of the tumors mediated by membrane transport protein to ensure that the sensitivity of P-glycoprotein high expression cells to anti-cancer medicines can be restored. According to the medicine for reversing the multi-medicine resistance of the tumors, disclosed by the invention, trametinib and the anti-cancer medicines can be combined to ensure that the effects of treating and controlling resistant tumors can be achieved by restoring the sensitivity of resistant cells to the anti-cancer medicines.

The invention discloses application of KU55933 in preparation of drugs for reversing multidrug resistance of tumors, and belongs to the technical field of drug application. According to the invention, KU55933 is found to be capable of remarkably reversing tumor multidrug resistance mediated by membrane transporter for the first time, so that ABCG2 high-expression cells recover sensitivity to anti-cancer drugs. The drugs for reversing the multidrug resistance of the tumors can contain KU55933, anti-cancer medicines, carriers and auxiliary agents, can be prepared into a tablet, a particle, a capsule, an oral liquid or an injection form, and can be used for treating and controlling resistant tumors.