57 results about "Drug accumulation" patented technology

The invention relates to a targeted lipidosome drug-loading system containing aptamers and a preparation method of the system. The targeted lipidosome drug-loading system containing the aptamers comprises the aptamers, an antitumor drug and nano-liposomes prepared from sphingomyelin, wherein the antitumor drug is wrapped with the nano-liposomes and the aptamers are connected onto the nano-liposomes through chemical bonds for specifically identifying tumor cells. The nano-liposomes are prepared from sphingomyelin and are connected with an appropriate quantity of the aptamers after the antitumor drug is wrapped with the nano-liposomes, sphingomyelin contains more amido bonds and can resist chemical and biological degradation better, protect stability of a lipidosome structure and increase the drug accumulation content of the tumor cells, and accordingly, the antitumor effect is improved.

The invention belongs to the field of medical technology and relates to an integrin targeting drug loaded albumin nanoparticle formulation and its preparation method. According to the invention, a gemcitabine-carried albumin nanoparticle target administration system is prepared by gemcitabine raw medicine, bovine serum albumin BSA, a RGD polypeptide, injection water, a dehydrating agent, a cross-linking agent and sodium hydroxide. The drug-loaded albumin nanoparticles have good dispersibility with a distribution range of particle size being 94-166nm, average particle size being 130nm, Zeta potential being -30.77mV, an encapsulation efficiency being 92.16%, a drug loading capacity being 12.8%, 30min burst release rate being 53.25+ / -2.23% and 8 hours in vitro cumulative release rate reaching 90%. It is verified through experiments that the targeted nanoparticles provided by the invention can significantly increase the drug accumulation in the target sites, have good slow release and tumor targeting effects, can improve therapeutic effects and relieve toxic and side effects of chemotherapeutic drugs and enhance the tolerance of patients to treatment.

The invention relates to a pH (potential of hydrogen) responsive graphene oxide nano-sheet coated mesoporous silicon dioxide drug double-loaded composite nanoparticle and a preparation method. The pHresponsive graphene oxide nano-sheet coated mesoporous silicon dioxide drug double-loaded composite nanoparticle comprises a mesoporous silicon dioxide nanoparticle, cinnamyl aldehyde, a graphene oxide nano-sheet and adriamycin, wherein the cinnamyl aldehyde is loaded inside the mesoporous silicon dioxide nanoparticle, the surface of the mesoporous silicon dioxide nanoparticle is coated with the graphene oxide nano-sheet, and the adriamycin is loaded in the structure of the graphene oxide nano-sheet. The preparation method includes the steps: loading the cinnamyl aldehyde and the adriamycin inthe amination mesoporous silicon dioxide nanoparticle and the graphene oxide nano-sheet by physical load and pi-pi conjugate; performing electrostatic adsorption to obtain the pH responsive grapheneoxide nano-sheet coated mesoporous silicon dioxide drug double-loaded composite nanoparticle. The prepared composite nanoparticle is good in biocompatibility, high in drug loading capacity and less indrug release within a neutral pH range, a surface covering layer is rapidly removed by surface charge variation of the graphene oxide nano-sheet in a low-pH environment in a tumor cell, drugs are released in a responsive manner, drug accumulation in the cell is finally improved, drug treatment effects are enhanced, and toxic and side effects are reduced.

Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.

The invention provides a focusing vortex acoustic tweezers control system and a method with an obstacle avoidance control function. The active phase control and passive structure phase modulation of aplanar fan-shaped transducer array are utilized to construct the focusing vortex acoustic tweezers with a controllable obstacle avoidance cavity, and object control behind an obstacle is realized. The curvature radius of a self-bending wave beam arc track is regulated and controlled through the order and the wave number of a semi-Bessel sound beam, the hollow radius of a phase modulation disc isdetermined according to the size of an obstacle, and regulation and control over the shape and the size of an arc track obstacle avoidance cavity and the axial distance of the acoustic tweezers are achieved. The capture radius and the capture capability of the focusing vortex acoustic tweezers are further regulated and controlled through the vortex topological charge of the transducer. According to the invention, sound waves emitted by the transducer array can be guided to bypass bones and important organs to form the focusing vortex acoustic tweezers, rotary capture of drug particles is realized, the thermal therapy effect of a focal region can be enhanced by utilizing drug accumulation, and a new method is provided for application of the focusing vortex acoustic tweezers in biomedicine.

Albumin and doxorubicin are bonded through reaction. The bonded albumin and doxorubicin are added with a gold-nanoparticles solution for reaction. After being purified with water in a column, the liquid phase of gold-nanoparticles is changed into a phosphate buffer for obtaining an anticancer drug having doxorubicin bonded with gold nanoparticles. Thus, with the high biocompatibility and the big surface areas, gold nanoparticles are used in biological applications and used as carriers for increasing drug accumulation on tumor. The bonding between gold nanoparticles and doxorubicin increases stability of doxorubicin. Besides, doxorubicin has tumor-killing effect for cancer therapy.

The invention discloses an application of liquiritin in preparing an escherichia coli fluoroquinolone efflux pump inhibitor. Research results indicate that, the liquiritin can obviously reduce the minimal inhibitory concentration of fluoroquinolone of drug-resistant escherichia coli (fluoroquinolone active efflux phenotype and acrA gene high expression strain), obviously increase drug accumulation concentration in a thallus, and obviously reduce expression quantity of an efflux pump gene acrA, so that susceptibility of the drug-resistant escherichia coli to the fluoroquinolone is increased, usage amounts of drugs are reduced, treatment cost is reduced, and food safety problems such as drug residues are decreased. Simultaneously, the liquiritin is a natural compound existing in plants, has no side effects such as teratogenesis and carcinogenesis, and is safe and nontoxic. The invention not only broadens application fields of the liquiritin and improves market value of the liquiritin, but also provides an efficient and safe bacteria efflux pump inhibitor for anti-infective therapy.

The invention discloses a polyethylene glycol-gambogic acid liposome, which is composed of a polyethylene glycol-gambogic acid conjugate, polyethylene glycol, vitamin E, cholesterol and phospholipid in a weight ratio of 1-10:0.5-2:0.05-0.2:1-4:10-30. According to the invention, an amphiphilic polymer PEG and an antitumor drug gambogic acid are connected with an ester bond into a conjugate amphipathic PEG-GA, and the PEG-GA is inserted into a liposome bimolecular layer to construct a nano targeted drug delivery system, the water solubility of the drug can be improved, also the drug stability and antitumor effect can be enhanced, drug accumulation in normal tissue can be reduced, the survival time of tumor-bearing mice is prolonged, the treatment efficacy is improved and the toxic and side effects are reduced. The invention also provides a preparation method and application of the liposome, and the liposome can be applied to treatment of lung cancer, ovarian cancer, breast cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma or brain tumors.

The invention provides a polymer shown as formula (I) in the description and a preparation method of the polymer. The prepared polymer has narrower polydispersity index. The invention further discloses a polymer-antitumor drug conjugate and a preparation method thereof. The prepared polymer-antitumor drug conjugate has longer blood circulation time and can obtain more drug accumulation at a tumorpart, so that a drug has better antitumor effect and has broad market application prospects.

The invention belongs to the technical field of high polymer material and pharmaceutical preparations, and particular to preparation of a p-hydroxybenzoic acid mediated polymer micelle drug delivering system with brain targeting function and application of the polymer micelle drug delivering system in the treatment of brain tumors. The polymer micelle drug delivering system with the brain targeting function is prepared by mixed construction of a brain targeting functional material and an amphipathic r polymer material, in-vivo and in-vitro activity evaluation results show that the p-hydroxybenzoic acid mediated polymer micelle drug delivering system can step over blood brain barrier to deliver drugs into the brain, can significantly increase the drug accumulation in the brain, and has the obvious antitumor effect, and compared with a common polymer micelle drug delivery system, the treatment effect of anticancer drugs on the brain tumor can be significantly improved.

The invention relates to a preparation method of strychnine immune nanoparticles, and the preparation method comprises the following specific steps: step 1, dissolving carboxylated poly(ethylene glycol)-polylactic acid block copolymer and strychnine in an organic solvent, and then mixing with a polyvinyl alcohol aqueous solution to form a primary emulsion; step 2, removing the organic solvent andimpurities to obtain a strychnine nanoparticle concentrate; and step 3, sequentially adding a carbodiimide salt used as a carboxyl activation reagent and an anti-human-AFP (alpha-fetoprotein) monoclonal antibody to the strychnine nanoparticle concentrate, thus linking the carboxyl group on polyethylene glycol and the amino group of the anti-human-AFP monoclonal antibody by chemical coupling to obtain the strychnine immune nanoparticles. The preparation method provided by the invention has the advantages of simple process, high encapsulation rate, stable drug release and good drug ballability;and the obtained strychnine immune nanoparticles are used for preparing anti-tumor immune targeting drugs, and have the advantages of precise targeting drug accumulation in tumor tissue cells, stabledrug release, good anti-cancer effect, safety and the like.

The present invention describes the use of radio-labeled antitumor drugs in the treatment of solid tumors by the method of administering a radio-labelled anticancer drug to a patient and imaging at least a part of the patient using Positron Emission Tomography imaging. The method is used to monitor delivery of antitumor drugs to tumors and may be used to predict the effectiveness of therapy with a particular antitumor drug or combination of antitumor drugs, to assess the effectiveness of modulators of cellular accumulation, to individualize therapy and to evaluate the effectiveness of antitumor drugs with respect to particular cancers. Particularly preferred drugs are labeled taxanes, e.g., 11C-paclitaxel and 11C-docetaxel, labeled anthracyclines, e.g., 11C-doxorubicin and 11C-epirubicin, and other radio-labeled drug, e.g. 11C-topotecan and 11C-mitoxantrone. The invention further describes antitumor drugs labeled with the radioactive label 11C and methods of preparing radio-labeled drugs.

The invention discloses a drug combination, in particular to a traditional Chinese medicine combination used for treating vitiligo, pertaining to the traditional Chinese medicine field. The traditional Chinese medicine combination is mainly made from psoralen as the raw material. And through improving the psoralen injection formulation, the disadvantages existing in the prior art are overcome. An external gel is also provided by the invention, which has a simple preparation technology, novel formulation, high biological utilization and stable property and convenient use; the effect can be fast and good when the invention is directly used in the surface of affected skin; besides, drug accumulation on affected skin can be enhanced, thereby, the dosage can be reduced and adverse reaction caused by whole body absorption can be decreased.

The invention discloses a topiroxostat controlled-release granule. An inner core is prepared from topiroxostat through an inclusion technology, then controlled-release coating is conducted, and the topiroxostat controlled-release granule is obtained. The invention further discloses a preparation method of the topiroxostat controlled-release granule. Compared with the prior art, the topiroxostat controlled-release granule can slowly release a drug at a constant speed in a specified release medium, the release rate and bioavailability of topiroxostat are effectively increased, rapid release can be achieved at the preliminary stage of taking to produce drug efficacy, slow release at a constant speed can be achieved at the later stage of taking, normal plasma concentration can be maintained, the drug efficacy can be maintained for a long time, toxic and side effects do not occur, drug accumulation poisoning is not caused, the curative effect is improved, and safety and rapidness are achieved. Meanwhile, the preparation method of the topiroxostat controlled-release granule is suitable for expanded production.

The invention discloses a water solubility platinum complex containing deoxyglucose and a preparation method and application. The water solubility platinum complex containing the deoxyglucose is shown as the formula (1) (please see the formula in the specifications). The water solubility platinum complex containing the deoxyglucose has an excellent tumor selective drug accumulation effect, and drug resistance formed by a repulsive effect of a tumor to drugs is overcome through targeting performance transmission to tumor cells. Compared with clinical drugs, the water solubility platinum complex containing the deoxyglucose has higher water solubility and is capable of achieving clinical preparation easily. Compared with the clinical drug, namely, oxaliplatin, the water solubility platinum complex containing the deoxyglucose has superiority in the aspect of cytotoxicity. In conclusion, according to the water solubility platinum complex containing the deoxyglucose, not only is the problem of poor preparation stability and the shortcoming of inconvenient clinical using in existing platinum drugs because of lacking in water solubility solved, but also targeting performance of the drugs to tumor cells can be improved, and the deficiency of the existing clinical drugs in the aspects of the tumor therapy effect, the drug resistance and toxic and side effects is solved.

The invention discloses a fluorine-containing water-soluble platinum complex and its preparation method and use. The fluorine-containing water-soluble platinum complex is shown in the formula (I). The fluorine-containing water-soluble platinum complex has excellent tumor-selective drug accumulation effects and prevents rejection-caused tumor resistance to drugs by targeting delivery to tumor cells. Compared with clinical drugs, the complex has high water solubility and is suitable for clinical preparation. Compared with a clinical drug oxaliplatin, the complex has superiority in cytotoxicity. The fluorine-containing water-soluble platinum complex solves the problem the existing platinum drug has poor water solubility, poor stability and clinical use inconvenience, improves drug targeting effects on tumor cells, and solves the problem that the existing clinical drugs has deficiency in tumor treatment effects, resistance to drugs and toxic or side effect.

This invention is about a cell-penetrating drug carrier and the application thereof. The mentioned cell-penetrating drug carrier can approach the target cell through using a proper recognizable sequence, so that the cell-penetrating drug carrier can be used to specifically delivery wanted drug to target cell. Through carrying wanted drug into the cytoplasm of the target cell by cell-penetrating peptide, the drug accumulation volume in the target cell can be efficiently increased. Preferably, through using proper bioinert polymer, the cell-penetrating peptide and the recognizable sequence can be kept from been digested before approaching the target cell.

The invention discloses a drug application device for the gynaecology department. The drug application device for the gynaecology department at least comprises an infrared lighting lamp, a supporting rod, a tube body, a piston, a core bar, symmetrical finger rings, a battery case and a drug application tube, wherein the infrared lighting lamp is fixed to the front end of the supporting rod and is connected with a control button arranged on the battery case through a wire arranged in the supporting rod, the piston is arranged in the tube body, the core bar penetrate through the tube body to be connected with the piston, the battery case is fixed to the rear end of the core bar, a battery bin is installed in the battery case, a battery is arranged in the battery bin, and the control button arranged at the outer end of the battery case is connected with a binding post wire of the battery bin in series. By the adoption of the device, the working difficulty of medical staff is reduced, drugs are evenly applied to a wounded part of a patient, and the technical problem of local drug accumulation caused by existing single-point drug application can be solved; due to the fact that the infrared lighting lamp is arranged on the supporting rod of the drug application device, the lighting effect can be achieved.

The invention belongs to the technical field of polymers and medicinal preparations and relates to a myristic acid-mediated brain-targeting polymer micelle drug-delivery system and its preparation method and use. The myristic acid-mediated brain-targeting polymer micelle drug-delivery system is an antitumor drug-loading polymer micelle drug-delivery system comprising a brain-targeting functional material (I), an amphiphilic polymer material (II) and an antitumor drug. An in-vitro and in-vivo activity evaluation experiment proves that the myristic acid-mediated brain-targeting polymer micelle drug-delivery system is obviously superior to a common polymer micelle drug-delivery system, can go through a blood-brain barrier and delivery the drug into the brain, can substantially improve drug accumulation in the brain, has obviously antineoplastic effects and can be used for improving antineoplastic drug effects of treating brain tumors. The myristic acid-mediated brain-targeting polymer micelle drug-delivery system has a good application prospect.

A magnetic microparticle drug carrier comprising mesoporous iron oxide is described. The drug carrier has an average diameter in a range of 0.5-1.2 μm, a BET surface area ranging from 50-300 m2 / g, and a pore volume ranging from 0.15-0.65 cm3 / g. The drug carrier is made using a hard mesoporous silica template which is completely removed from the deposited iron oxide. The drug carrier may be loaded with high amounts of hydrophilic anticancer chemotherapeutic drugs and / or hydrophobic hormonal anticancer drugs, and released in a pH-controlled manner inside cancerous cells. Compared to free drugs, the drug microparticle carrier displays enhanced drug accumulation inside tumor tissues, deeply penetrates into a tumor region and kills the tumor cells inside. The designed carriers described here entrap and release different kinds of anticancer drugs in a controlled manner for synergistic combinatorial chemo / hormonal cancer therapy.

The invention belongs to the field of biological medicine technology, and relates to an application of polypeptides using RGD as an active site to preparation of a targeted medicament for treating depression, and especially relates to the polypeptides which use RGD as the active site and can be used as target heads for constructing an anti-depression brain-targeting drug delivery system. The RGD peptide is a tripeptide sequence (Arg-Gly-Asp) which is composed of arginine, glycine and aspartic acid; polypeptides which use the RGD tripeptide as the active site comprise pentapeptide, heptapeptide, and cyclopeptide or peptide analogue compounds. Tests show that linear peptides and cyclic peptides using RGD as the active site are used for modifying a nanometer drug delivery system, so that drug accumulation of the system in brain is substantially improved, and brain-targeting drug delivery characteristics are obvious; the system can be applied to entrapment of anti-depression medicaments, so that anti-depression effects of trefoil factor are obviously improved.

The invention belongs to the technical field of protein, and discloses an MdrP mutant gene, amino acid, and protein function and drug accumulation activity detection. According to the invention, CCCPis added to the Buffer containing cations (Na<+>, K<+>) to remove the transmembrane H<+> gradient, only transmembrane cation gradient is retained to drive protein translocation, or Monensin or Nigericin is added in the buffer to remove the cation gradient, and only the transmembrane H<+> gradient is retained to drive the protein translocation, and a relative quantitative comparison between different driving effects can be realized. The important function of highly conserving amino acid site of the MdrP protein can be clarified, and the MdrP protein can be proved as an H<+> and Na<+> driven drug efflux protein; N146 is the H<+> binding site, D223 and Q242 are Na<+>, H<+> competitive binding sites, or can be a favorable theoretical support for understanding the MFS family of drug resistanceproteins.

The invention discloses application of pazopanib, a pharmaceutical composition, an injection, a preparation method and application. The pharmaceutical composition comprises the following components: pazopanib, a cyclodextrin solubilizer and a solvent, wherein the mass ratio of pazopanib to the cyclodextrin solubilizer is 1: (13-100); and based on 1mL of the pharmaceutical composition, the concentration of the cyclodextrin solubilizer in the pharmaceutical composition is 6-330mg / mL. The pharmaceutical composition prepared by the invention can be used for treating diseases such as acute lung injury, pulmonary fibrosis and acute respiratory distress syndrome, and the treatment aim can be achieved by using a small amount of pazopanib; and moreover, the pharmaceutical composition is high in bioavailability, high in stability and low in impurity content, and the phenomenon of drug accumulation is avoided.

The invention is applicable to the technical field of fragrance products, and provides a fragrance spray for helping sleep and a preparation method and application thereof. The fragrance spray comprises the following components: herba selaginellae, caulis polygoni multiflori, herba lophatheri, herba mimosae pudica, radix valerianae and lotus plumule. The fragrance spray provided by the invention takes herbal traditional Chinese medicine extract essence as a main component, achieves the purpose of improving sleep by improving the sleep environment, has no toxicity, no harm and no side effects on a human body, overcomes the defects of drug accumulation, drug dependence, drug resistance and other side effects on the human body caused by oral administration of traditional hypnotic drugs, and also overcomes the inconvenience of decoction and administration of traditional Chinese medicines. At the same time, compared with products with sleep improvement, such as aromatherapy products, sachetsachets, medicine bags and medicine pillows on the market, the fragrance spray has the characteristics of no need of heating, no mildew and no breeding of microorganisms, and realizes the product characteristics of portability, convenient use, no side effects, safety, reliability and outstanding effect at home, in travel, in the field and the like.

The present application relates to a series of redox-sensitive albumin-bound prodrugs specifically responsive to tumor tissue, and in particular, to three small-molecule docetaxel-maleimide prodrugs. A maleimide ring in the prodrug structure is used as a target for binding a free thiol group at position 34 of a plasma albumin in the body, such that the drug rapidly and specifically binds to the albumin after intravenous injection into the body and forms an albumin-drug complex, thereby enhancing drug stability and significantly prolonging the circulation time of the drug in the body. Furthermore, the EPR effect is leveraged to achieve drug accumulation in tumor tissue.

The invention discloses a topiroxostat controlled-release capsule, which is prepared by preparing a core from topiroxostat through an inclusion technology and conducting controlled-release coating. The invention also discloses a preparation method of the topiroxostat controlled-release capsule. Compared with the prior art, the controlled-release capsule disclosed by the invention can achieve slow constant-speed release of the drug (the topiroxostat) in a specified release medium, so that the release degree and bioavailability of the topiroxostat are effectively improved; the drug can be rapidly released to generate efficacy in the initial period of administration and can be slowly released at a constant speed in the late period of the administration, so that a normal blood concentration is kept, and the efficacy is kept for a long time, without the problems of toxic and side reactions or poisoning due to drug accumulation; therefore, the efficacy is improved, and the drug is safe and rapid to take the efficacy. Meanwhile, the preparation method disclosed by the invention is applicable to expanded production.

The invention relates to the field of pharmaceutical preparations, and in particular relates to a compound drug controlled-release preparation containing topiroxostat and febuxostat. The invention also discloses a preparation method of the compound drug controlled-release preparation containing topiramate and febuxostat. Compared with the prior art, the compound drug controlled-release preparationprovided by the invention can release a drug slowly at a constant speed in a prescribed release medium, so that the release rate and bioavailability of the compound drug controlled-release preparation are effectively improved, the preparation can be rapidly released in the early stage of medication to produce drug effects and can be slowly released at a constant speed in the later stage to maintain a normal blood drug concentration, and the preparation maintains the drug effects for a long time without producing toxic and side effects or causing drug accumulation and poisoning, improves the efficacy, and is safe and quick; and at the same time, the preparation method provided by the invention is suitable for scale-up production.