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.

An application of (-)-epigallocatechin gellate (EGCG) extracted from tea in preparing the medicines for treating tumor is disclosed, which features that said EGCG can be used as sensitizer and synergistic of antineoplastic medicine.

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 relates to a TPGS modified docetaxel liposome nano-drug delivery system, a preparation method and an application thereof. The TPGS modified docetaxel liposome nano-drug delivery system uses phospholipid and cholesterol as membrane materials, Surfactant TPGS modified liposomes and docetaxel (DTX) as anticancer drug were prepared by membrane dispersion ethanol injection ultrasonic dispersion reverse evaporation and freeze drying. The particle size of nano-doxetaxel liposomes modified by TPGS is 80-200 nm, the zeta potential is 0+30 mV or 0-30 mV, the encapsulation efficiency is 75-99%, with a drug loading of 3-15%. The in vitro cell experiment and in vivo pharmacodynamic experiment of the TPGS modified docetaxel liposome nano-drug delivery system prepared by the invention showthat the nano-drug delivery system can inhibit P. Overexpression of gp, decrease of drug efflux, increase of drug enrichment in tumor cells, increase of cytotoxicity and apoptosis rate, increase of tumor therapeutic effect and reversal of multidrug resistance.

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 relates to a preparation method and an application of a pH-sensitive mixed micelle. An anti-cancer drug, namely DOX, is in covalent linkage with mPEG by virtue of acid-sensitive Cbm, an obtained material, as a polymer prodrug, is mixed with TPGS, and self-assembling is conducted in a water solution, so that the mixed micelle, which is of a core-shell structure, is formed. The pH-sensitive mixed micelle provided by the invention can, in response to a special low-pH environment of tumor tissues, can achieve specific release of the DOX, so that the excretion of the drug can be effectively inhibited and the multi-drug resistance of tumor cells can be reversed; and the mixed micelle is good in biocompatibility and long in drug circulating time, and the preparation method is convenient for operation and popularization and has a good development prospect.

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 an application of pH sensitive type amphiphilic graft polyphosphazene for preparing a pH response type amphiphilic graft polyphosphazene administration vesicle. The administration vesicle contains pH response type amphiphilic graft polyphosphazene and drugs, wherein metered by the total weight of the drugs and the pH response type amphiphilic graft polyphosphazene, the weight percent of the drugs is 0.001%-30%, and the weight percent of the pH response type amphiphilic graft polyphosphazene is 70%-99.999%. The pH response type amphiphilic graft polyphosphazene is a graft polymer which is characterized in that a polyphosphazene chain segment is taken as a framework, a first graft group and a second graft group are connected on a phosphorus atom, and a third graft group is selectively connected on the phosphorus atom. The administration vesicle can load one or two water-soluble drugs and hydrophobic drugs, has pH responsiveness in drug release, can quickly release drugs near tumor tissues or in tumor cells at the fixed time, and has a function of reversing the multidrug resistance of tumor cells.

The invention discloses a targeted antitumor nano drug inhibiting expression of multi-drug resistance genes and a preparation method application thereof, and in particular relates to preparation, synthesis and application of the nano drug. The nano drug is prepared as follows: a polylactic acid-glycolic acid copolymer is used as a carrier material, curcumin-loaded nanoparticles are prepared by a solvent evaporation method, and pluronic F127 and hyaluronic acid are used for surface modification. The particle size of the nanoparticles is about 260nm, and the drug loading is about 6.6%. More importantly, the nanoparticles not only can be used for targeted delivery of drugs to tumor cells, but also can effectively inhibit the expression of the multi-drug resistance genes, thereby enhancing the efficacy of chemotherapy and reducing the side effects of the chemotherapy.

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 an HA (hyaluronic acid)-mediated targeted double-drug-loading cationic liposome coating, which is a cationic liposome coating co-modified by HA (hyaluronic acid), TPGS (tocopheryl phosphate synthase) and polylysine-deoxycholic acid (PLL-DA), and is used for co-delivering PTX (paclitaxel) and SOR (sorafenib) so as to treat multidrug resistance cancers. And the liposome coating adopts a lipid membrane hydration-ultrasonic method to prepare the drug-loaded TPD-CL-PTX / SOR liposome of the HA coating. The multifunctional liposome (HA-TPD-CL-PTX / SOR) can be preferentially gathered at a tumor part through a passive targeting effect and a CD44 mediated active targeting effect after intravenous injection. PTX and SOR are released from tumor cells and have a synergistic anti-tumor effect. Besides, TPGS can further interfere with the mitochondrial function and prevent energy supply of a P-gp efflux pump so as to reduce efflux of PTX or SOR to the maximum extent, so that drugs with high treatment concentration are maintained in cancer cells, multi-drug resistance is effectively reversed, and the method is promising.

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 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 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 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 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 relates to a preparation method and an application of a pH-sensitive mixed micelle. An anti-cancer drug, namely DOX, is in covalent linkage with mPEG by virtue of acid-sensitive Cbm, an obtained material, as a polymer prodrug, is mixed with TPGS, and self-assembling is conducted in a water solution, so that the mixed micelle, which is of a core-shell structure, is formed. The pH-sensitive mixed micelle provided by the invention can, in response to a special low-pH environment of tumor tissues, can achieve specific release of the DOX, so that the excretion of the drug can be effectively inhibited and the multi-drug resistance of tumor cells can be reversed; and the mixed micelle is good in biocompatibility and long in drug circulating time, and the preparation method is convenient for operation and popularization and has a good development prospect.

The invention discloses a pH-sensitive and active oxygen-sensitized Planic polymer. The structure of the polymer is shown in formula VI: at the same time, the invention also discloses the preparation method of the above-mentioned polymer, which specifically includes step S1: shown in formula III Preparation of compound; step S2: preparation of compound shown in formula IV; step S3: preparation of pH-sensitive and active oxygen-sensitized pluronic polymer shown in formula VI; at the same time, the present invention combines the polymer prepared above with antitumor Drug compounding is applied to the drug delivery system, and the above-mentioned polymer is prepared into drug-loaded micelles. The above-mentioned polymer disclosed in the present invention uses Pluronic P123 as the core, and is designed according to the principle of drug combination. On both sides of Pluronic P123 Orthoester and vitamin E succinate groups are sequentially combined at the end of the chain. The polymer prepared by using the above drug combination theory not only shows significant reversal of multidrug resistance of tumor cells but also has ideal drug release. relatively stable.

The invention provides the use of schisandra fruit in preparing medicament for treating tumors, wherein the schisandra is a plant of Schisandra chinesis(Turcz.)Baill. belonging to Magnoliales, it can effectively inverse the multi-drug tolerance of the tumors. The extracts of schisandra fruit can be acted on P-glucoprotein, MRP1 and MXR.

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.