236 results about "Drug targetting" patented technology

The invention discloses a cationic polymer-based proteolysis targeting chimera as well as preparation and application thereof, and belongs to the fields of targeting protein degradation and nanotechnology. According to the chimera, a cationic polymer is used as a connecting arm to connect a target protein ligand and an E3 ubiquitin ligase ligand to form a ternary complex, so that efficient degradation of target protein is realized. By adjusting the ligand proportion, chimeras with different degradation efficiencies can be synthesized, and accurate regulation and control are realized. The pH-responsive nano-drug obtained by hydrolyzing the targeting chimera by using the targeting protein can respond to an acidic tumor microenvironment, specifically release the chimera, and improve the targeting property and the treatment effect of the drug. Compared with the traditional PROTACs, the compound has higher bioavailability and tumor permeation effect; the preparation method of the nano-drug is simple and easy to implement, provides possibility for preparation of high-performance nano-drugs, shows potential in preparation of anti-tumor cell drugs, provides new thoughts and methods for tumor treatment, and has important clinical application value.

The invention discloses a nanometer delivery device for a gastric cancer targeted drug and a use method of the nanometer delivery device, and belongs to the technical field of drug targeted delivery. The device comprises a molecular recognition and optimization module which is responsible for accurately recognizing a tumor cell specific molecular marker and providing personalized treatment strategy recommendation; the nano-carrier design module is used for designing multifunctional lipid-polymer hybrid nano-particles and carrying out surface targeting ligand modification; the intelligent drug loading module is used for improving the stability and controllability of drug loading based on a pH / temperature sensitive release mechanism and effectively reducing the toxic influence of non-targeted tissues; the molecular imaging and monitoring module integrates a nanoprobe imaging technology and a quantum dot tracing technology, constructs a treatment-imaging integrated system, realizes real-time dynamic monitoring of a treatment process, and provides instant feedback of a molecular level; and the risk assessment module is used for establishing a safety database and providing dynamic risk assessment of the treatment process through a biological safety assessment system and long-term tracking management.

The invention provides a medicine composition for treating cancer. The medicine composition comprises an inhibitor for inhibiting FOXRED2 protein expression and application of Paraprevir in preparation of a medicine for treating cancer. According to the application disclosed by the invention, the new indication of the hepatitis C medicine paritaprevir for inhibiting the malignant process of the liver cancer HCC is found for the first time, the treatment field of the medicine in the liver cancer is expanded, and a theoretical basis is provided for developing a new target spot for treating the liver cancer.

A drivable drug-release and sampling integrated capsule, which falls within the technical field of medical instruments, and can achieve targeted release of a drug of an exact dose and nearly non-invasive tissue sampling at a precise position in the human intestinal tract. The capsule comprises a shell (1), wherein the shell (1) is provided with a first external thread (11) and an internal thread (12) having the same rotation direction, and is provided with a first drug outlet at the tail and a sampling needle (4) at the head; a sleeve (2) and a plunger (3) are provided in the shell (1); the sleeve (2) is a cylinder having an opening at one end; the plunger (3) comprises a threaded section (31) and a plain shaft section (32), the threaded section (31) being provided with a second external thread (33) adapted to the internal thread (12), the plain shaft section (32) extending into the sleeve (2) and capable of axially sliding in the sleeve (2), and the bottom surface of the plain shaft section (32), the bottom surface of the sleeve (2) and the inner side wall of the sleeve (2) enclosing a drug storage cavity (5); a second drug outlet is provided in a side wall of the drug storage cavity (5); the plunger (3) can push the sleeve (2) to move in the axial direction of the shell (1); when the sleeve (2) moves to the bottom of the shell (1), the first drug outlet is in communication with the second drug outlet; and both the first external thread (11) and the second external thread (33) have magnetic properties.

The invention provides an ergosterol-loaded brain-targeted nano preparation and a preparation method and application thereof, and relates to the field of nano materials and nano biological medicine.The active ingredient ergosterol of the nano preparation is entrapped in a DSPE-PEG-pinacol borate nano material, and the nano material has the ROS response characteristic and can be used for preparing a brain-targeted nano preparation. The ergosterol-loaded nano preparation is in the shape of a regular sphere, is uniform in particle size, has good dispersibility and stability, has good ability of targeted therapy of cerebral arterial thrombosis diseases, effectively solves the problems of poor targeting property, low bioavailability and the like of common drugs, enhances the therapeutic effect of ergosterol on cerebral arterial thrombosis, and has good application prospects. The ergosterol can effectively improve brain injury caused by the cerebral arterial thrombosis and has a good treatment effect, meanwhile, the ergosterol serving as the active ingredient plays a role in treating the cerebral arterial thrombosis by activating a PI3K / AKT / mTOR pathway, and a new direction is provided for treatment of the cerebral arterial thrombosis.

Described herein are compositions, systems, and methods for targeted and controlled drug release. In some embodiments, the compositions, systems, and methods may comprise magnetoelectric silica nanoparticles for targeted and controlled release of chemotherapeutic drugs for cancer treatment. In some embodiments, an external magnetic field may be used to release one or more drugs from the magnetoelectric silica nanoparticles. The disclosed compositions, systems, and methods may improve drug targeting and reduce systemic drug toxicity.

The invention discloses a nano-drug delivery method for enhancing LGP kidney targeted release and application of the nano-drug delivery method, and relates to the technical field of nano-drugs. According to the nano-drug delivery method for enhancing LGP kidney targeted release and the application thereof, a hydrophobic modified chitosan polymer is synthesized; preparing HCS nanoparticles; and constructing a drug loaded nanoparticle, namely, HCS-LGP NPs. According to the invention, the solubility of the medicine is increased, the distribution of the medicine in vivo is changed, and the targeting of the medicine is improved, so that the treatment effect is improved, and adverse reactions are reduced. Due to good biocompatibility and modifiability, chitosan is widely used as a nano delivery carrier of anti-tumor and antibacterial drugs.

The invention relates to the technical field of biology, and particularly provides a targeting carrier, a targeting drug, a preparation method and application. The targeting carrier comprises (a) a metal-polyphenol compound particle and (b) a targeting structure, and the targeting structure is connected with the outer surface of the metal-polyphenol compound particle. Under the condition that the effectiveness of the LNP based on the cationic lipid and / or the ionizable lipid is not lower than that of the LNP based on the cationic lipid and / or the ionizable lipid, the targeting carrier provided by the invention does not use the cationic lipid and the ionizable lipid, so that the toxicity is greatly reduced, the biological safety is remarkably improved, negative charge drugs are more favorably carried in a living body, the application range is wide, and the targeting carrier can be used for drugs with different sizes. The targeted drug can achieve high expression quantity of nucleic acid drugs, the biological safety is remarkably improved, the targeting property is good, and efficient treatment of various diseases can be achieved.

The invention discloses an oral colon-targeted silicon nano-drug and application thereof, and belongs to the technical field of drug targeted delivery. According to the oral colon targeting delivery system based on biodegradable nano-silica, entrapment of drug molecules can be synchronously achieved in the preparation process, and the targeting effect of the system on inflammatory endothelial cells and macrophages is enhanced through surface modification of hyaluronic acid. In order to ensure the stability of the delivery system in the gastrointestinal tract and avoid the influence of strong acid environment, enzyme and the like in the stomach on the protein, the surface of the delivery system is further modified with chitosan and sodium alginate through electrostatic interaction. The hyaluronic acid, the chitosan and the sodium alginate are used as natural polymer materials and have good biocompatibility. A novel neurotrophic factor MANF is used as a model protein, the MANF protein is successfully delivered to a colon part by constructing an oral colon targeting delivery system, and it is proved that the MANF protein can improve ulcerative colitis injury through oral administration on the animal level.

The invention relates to the technical field of biology, in particular to application of synaptic binding protein 11 serving as a marker to preparation of products for diagnosis, auxiliary diagnosis, screening or auxiliary screening of schizophrenia and application of the synaptic binding protein 11 and / or a dopamine D2 receptor serving as a core target to treatment of schizophrenia. The application of the synaptic binding protein 11 or the transcriptional product mRNA or the mRNA fragment of the synaptic binding protein 11 as the marker in any one of the following items: 1) application in preparation of products for diagnosis or auxiliary diagnosis of schizophrenia of human or non-human mammals; 2) application in preparation of products for screening or auxiliary screening of schizophrenia of human or non-human mammals; 3) application in diagnosis or auxiliary diagnosis of schizophrenia of human or non-human mammals to be detected; and 4) application in screening or auxiliary screening of schizophrenia of human or non-human mammals to be detected. Meanwhile, the invention also provides application of treating three symptoms of schizophrenia through a brain region specific targeting dopamine D2 receptor. Researches find that synaptic binding protein 11 or a transcription product mRNA or mRNA fragment thereof can be used as a brand new functional schizophrenia diagnosis marker, and a chemical molecule or gene therapy drug targeting synaptic binding protein 11 or a dopamine D2 receptor can effectively improve three symptoms of schizophrenia.

Disclosed are drug conjugates comprising a targeting moiety conjugated to a drug molecule, wherein the targeting moiety binds to a cell adhesion moiety and / or receptor expressed on a Schwann cell to mediate targeted delivery of the drug conjugate to the Schwann cell, and wherein the drug molecule modifies expression or activity of a disease-associated molecule, and / or confers a cytotoxic effect, in the Schwann cell. Further disclosed herein are methods of targeted delivery of a drug to the Schwann cells.

The invention relates to the technical field of medicines, and provides a synergetic nano chemotherapy preparation for treating pancreatic cancer and a preparation method of the synergetic nano chemotherapy preparation. According to the synergistic nano chemotherapy preparation, an RGD peptide modified lipid-mesoporous silica nano delivery system is used for simultaneously encapsulating a ferroptosis inducer Erastatin and a chemotherapy drug gemcitabine hydrochloride hcGEM. The nano synergistic treatment system not only can actively deliver the drug to the pancreatic tumor tissue with high expression of the integrin receptor in a targeted manner through the surface-modified RGD peptide, but also can realize drug synergistic treatment, and improves the killing effect of the drug on pancreatic cancer cells while reducing the toxic and side effects.

Disclosed in the present invention is a compound represented by formula (I), or a pharmaceutically acceptable salt, ester or solvate thereof. Such a PSMA compound has higher tumor uptake and / or lower or substantially equivalent kidney uptake, can improve the drug targeting effect and / or reduce the kidney injury risk, and is conducive to better meeting the medication needs of patients.

The invention relates to a nano drug delivery system for delivering at least one drug and a preparation method of the nano drug delivery system. The nano drug delivery system is formed by assembling a recombinant fusion protein and hydrophobic degradable polyester or a derivative thereof with an albumin hydrophobic structural domain in the recombinant fusion protein through weak acting force and loading at least one drug, the medicine is a small molecule medicine used clinically. The hydrophobic degradable polyester or the derivative thereof is selected, different drug molecules and specific recombinant fusion protein are prepared into the nano drug delivery system for targeted delivery of at least one drug, the stability is excellent, the efficiency of targeted delivery of the drug to a tumor site can be improved, the anti-tumor curative effect is enhanced, and toxic and side effects are reduced. The preparation method of the nano drug delivery system is mild and controllable, and has high clinical application potential. The nano drug delivery system delivers at least one drug to different types of tumors in a targeted manner, and can be applied to tumor treatment.

The invention relates to the technical field of medicines, and discloses a drug delivery bionic carrier as well as a preparation method and application thereof. Most of anti-tumor drugs are low in delivery efficiency through intravenous injection, the anti-tumor drugs are'inactivated 'by lysosomes after entering cells and fail, and the drug failure approach is a main reason for reduction of the effectiveness of most of the anti-tumor drugs delivered through intravenous injection. In order to improve the efficiency of targeted delivery of anti-tumor drugs through intravenous injection, a bionic carrier formed by wrapping chalk with a cell membrane is provided to load the anti-tumor drugs, and specifically, chalk releases carbon dioxide in lysosome to break through the lysosome and promote the drugs to escape from the lysosome, so that targeted delivery and intracellular positioning release of the drugs are realized; the anti-tumor effect of the medicine is remarkably improved while the biocompatibility of the carrier is not influenced, and a scientific basis is provided for targeted delivery of the medicine and tumor treatment.

The invention relates to an application of a CAR exosome drug carrier in tumor treatment. The application of the CAR exosome loaded medicine in tumor treatment is based on the strategy of CAR exosome coupling medicine, so that the completeness of the exosome and the controllability of the medicine loading capacity are greatly protected, the purpose of accurately delivering the medicine to tumors in a targeted manner is achieved, and a new direction is provided for tumor treatment.

The invention discloses folate receptor mediated manganese ion coordination type cabazitaxel-loaded albumin nanoparticles as well as a preparation method and application thereof. Human serum albumin is covalently linked with folic acid through an amide condensation reaction to obtain a folic acid-albumin modifier with folic acid targeting; further combining with manganese ions through metal coordination to form a folic acid-albumin-manganese ion modifier with a targeting function; finally, efficient loading of cabazitaxel is achieved through a simple heating polymerization method, and the folate receptor mediated cabazitaxel-loaded albumin nanoparticles are formed. According to the nanoparticles provided by the invention, the particle size is about 140 nm, the stability is good, and the drug loading capacity and the encapsulation efficiency of cabazitaxel are high; the compound has a slow release effect, is good in in-vitro release behavior, and has important application value in the aspect of targeted delivery of drugs to tumors. Compared with other traditional nanoparticles, the nanoparticles show a remarkable anti-tumor effect.

The invention discloses a preparation method of a metal ruthenium hydrogel drug delivery system, which comprises the following steps: mixing a PDA-IR780 nanocapsule with a metal ruthenium hydrogel solution, quickly stirring, washing with distilled water, and freeze-drying to obtain the metal ruthenium hydrogel drug delivery system Ru (fmb) 3-HAADH (at) PDA-IR780. According to the invention, the drug targeting is improved, the pharmacokinetics of active ingredients is enhanced, a plurality of treatment modes are integrated, a photoresponse type metal ruthenium hydrogel drug loading system is constructed, and the killing effect on tumors is improved through photothermal and photodynamic combined treatment.

The invention provides a high-definition vascular structure reconstruction and blood flow function evaluation method and system, and the method comprises the steps: constructing a high-dimensional feature manifold space based on an ultrasound contrast image, carrying out the recognition to obtain a vascular subgroup with different blood flow function modes, and finally obtaining a high-definition rainbow vascular structure video and a vascular heterogeneity index in an ultrasound scanning region. A powerful tool can be provided for evaluating tumor microvascular structures, blood flow functions and time-space heterogeneous characteristics, abundant parameters for quantitatively describing tumor complex vascular systems are provided for early evaluation of drug curative effects, and a target blood flow perfusion area can be specifically recognized according to functional characteristics; and a target prompt and feedback intervention basis is provided for drug targeted release.

The invention provides a universal drug targeting delivery system for constructing pathological fibroblast-like synovial cells in osteoarthritis and application of the universal drug targeting delivery system. According to the drug targeting delivery system, vasoactive intestinal peptide is modified to the surface of polydopamine-coated large-aperture calcium ion-doped silicon dioxide; the vasoactive intestinal peptide specifically targets a VPAC1 receptor, and targeted delivery of the nano-drug to pathological fibroblast-like synovial cells in osteoarthritis is successfully realized. The vasoactive intestinal peptide provided by the invention is a polypeptide, has abundant amino groups and carboxyl groups, and can be connected to a drug delivery carrier through a simple chemical reaction, so that efficient targeted delivery of drugs and accumulation of pathological cells are realized.

The invention discloses a compound as shown in a formula I or pharmaceutically acceptable salt, ester or solvate thereof. The PSMA compound has higher tumor uptake and / or lower kidney uptake, the risk of renal injury can be greatly reduced while the drug targeting effect is improved, and the drug use requirements of patients can be better met. # imgabs0 #

The present invention discloses a nano-thermosensitive assembled gel for nasal administration, a preparation method thereof and its use, namely, mitochondrion-targeted puerarin nanoparticles, a thermosensitive gel, a preparation method thereof and its use. The nano-thermosensitive assembled gel for nasal administration of the present invention uses chitosan modified with SS-31 peptide having mitochondrion-targeting and transmembrane properties as a carrier material, and uses a thioketal cross-linking agent sensitive to reactive oxygen species (ROS) to cross-link the modified chitosan to prepare nanoparticles loaded with puerarin. Through a poloxamer thermosensitive gel system, a thermosensitive nanogel drug reservoir encapsulating the nanoparticles is constructed, and its application in the preparation of drugs for treating nervous system diseases realizes the targeting of the drug to the mitochondria of cerebral ischemic stroke injury, responsive cleavage in an environment rich in ROS, release of the drug, increase of the drug concentration in the mitochondria, and improvement of the brain bioavailability of puerarin, providing a more suitable and effective new dosage form for the treatment of stroke.

The invention relates to the field of biological medicine, and discloses application of bionic high-density lipoprotein nanoparticles in preparation of drugs for targeting hepatitis virus receptor-1. The bionic high-density lipoprotein nanoparticle disclosed by the invention is composed of phospholipid and apolipoprotein mimetic peptide, wherein the apolipoprotein mimetic peptide is ApoA-I mimetic peptide. According to the invention, the bionic high-density lipoprotein nanoparticles can target hepatitis A virus receptor-1 for the first time, and can deliver drugs to cells of high-expression hepatitis A virus receptor-1 to play a therapeutic role. The biomimetic high-density lipoprotein nanoparticles co-loaded with anti-inflammatory and anti-fibrosis drugs can deliver the drugs to damaged renal tubules in a targeted manner especially for damaged renal tubule epithelial cells with selective high expression of KIM-1, so that kidney injuries are effectively relieved, chronic kidney diseases are treated, disease progression is relieved, and a new solution is provided for treatment of the chronic kidney diseases.

This invention relates to the field of nanomedicine delivery systems, specifically to an ultrasound-enhanced synergistic immunotherapy drug delivery system, its preparation method, and its applications. The ultrasound-enhanced synergistic immunotherapy drug delivery system includes a lipid shell and a fluorocarbon gas encapsulated within the lipid shell. The lipid shell is made from cancer cell membranes and a lipid membrane formed from synthetic phospholipids. The lipid shell integrates a protein degradation-targeting chimera for degrading PD-L1. This invention combines targeted drug delivery, PD-L1 targeted degradation, and ultrasound enhancement technology to construct an integrated synergistic immunotherapy drug delivery system. Through multi-mechanism synergistic action, it overcomes the bottlenecks of existing PROTAC delivery systems, achieving a highly efficient anti-tumor immune response. This technical solution solves the technical problems of limited tumor tissue penetration and cellular uptake efficiency of PROTAC degrading agents targeting PD-L1, resulting in unsatisfactory delivery effects and promising prospects for widespread application.

The present disclosure relates generally to (CRISPR) RNA (crRNA) for the precision silencing of transcripts. In some embodiments, the crRNA are enriched for guanosine (G) nucleotides at key spacer positions, which is useful in enhancing the silencing efficacy of otherwise inefficient crRNA, thereby expanding the targeting spectrum of Cas13 endonucleases, e.g., Cas13b and Cas13d. In other embodiments, the crRNA comprise a spacer sequence having at least one nucleotide mismatch relative to the target RNA sequence, wherein the target RNA sequence is a wild-type transcript and / or a variant transcript (e.g., a transcript comprising a single nucleotide variant (SNV)). The present disclosure also provides RNA editing systems comprising the crRNA described herein in complex a Cas13 effector protein and a target RNA sequence, methods for the selective targeting of transcripts encoding proteins that are difficult to target, or are not amenable to pharmacological targeting, e.g., oncogenic fusion transcripts or oncogenic transcripts comprising single nucleotide variant(s), and methods for the design and selection of potent crRNA.

The application discloses an albumin nano-drug based on HSP90 inhibitor and a preparation method and application thereof, and belongs to the technical field of medicines.The short peptide A6 is modified to human blood albumin through a connecting chain, and the human blood albumin modified by the A6 is self-assembled with geldanamycin derivative G2111 in the presence of an organic solvent, so that the G2111 is combined to the hydrophobic region of the human blood albumin through a non-covalent bond, effective loading of the G2111 is realized, the solubility of the geldanamycin derivative is improved, the drug is targetedly released into cancer cells with high expression of CD44, the targeted accumulation of the drug in tumor tissues is enhanced, damage to other normal tissues and cells caused by off-target effects of the drug is avoided, the albumin nano-drug can be simultaneously used for chemotherapy of leukemia and solid tumors, and has important practical significance.

The application discloses a DDI prediction method based on a Siamese structure and graph contrast learning, comprising the following steps: collecting drug-drug interaction text data and physical and chemical property data files and targeting relationship data files of drugs; extracting the physical and chemical property characteristics and the targeting relationship characteristics of the drugs, fusing the characteristics to obtain initial characteristics based on the physical and chemical properties and the targeting relationship; calculating a drug-drug interaction adjacency matrix, combining the initial characteristics to construct a drug-drug interaction heterogeneous graph; inputting the heterogeneous graph into a Siamese structure-based graph contrast learning model to learn and obtain embedding characteristics of drug nodes; and using a link prediction method to calculate the score of edges between any two drug nodes. The application can alleviate the problem that the drug targeting relationship characteristics and the drug-drug interaction text data are difficult to be used alone when the data are sparse and have an impact on the performance of the model, improves the accuracy of drug-drug interaction prediction, and can be applied to identifying potential interactions between drugs.

A polypeptide-modified liposome for targeted drug delivery and a use thereof, relating to the technical field of biomedicine. The raw materials for the preparation of the liposome comprise a polypeptide-modified lipid material. The polypeptide-modified lipid material is obtained by coupling a polypeptide to a lipid material containing a polyethylene glycol chain; the polypeptide is Cys-(X)n, wherein X is any one or any two of Arg, Asp, His, Glu or Thr, n is the total number of X and is an integer in the range of greater than 1 and less than 11; and the polypeptide is coupled to the polyethylene glycol chain by means of a thiol group on a cysteine residue of the polypeptide. The provided polypeptide-modified liposome can achieve targeted delivery of drugs to organs, tissue and cells in the body. The provided polypeptide-modified lipid material has a certain degree of universality, and can be used in combination with multiple currently commercially available liposome excipients; and the type of an ionized lipid material and the type of a phospholipid can be adjusted arbitrarily.

The present invention belongs to the field of biological probe technology, and in particular relates to a small molecule probe HBAPE-Ac3ManNAz based on sugar metabolism labeling and its application in improving the targeting of platinum drugs. The present invention provides a small molecule probe HBAPE-Ac3ManNAz based on sugar metabolism labeling. The probe can selectively label tumor cells or tissues in vivo or in vitro as a metabolic precursor, and provide new targets for refractory tumors such as triple-negative breast cancer that lack specific targeting receptors; a pharmacodynamic molecule DBCO-PEG8-Oxp(IV) complex that reacts orthogonally with the probe is synthesized. The complex reacts with an azide tag marked on the tumor cell membrane through a bioorthogonal reaction, thereby improving the targeted transport ability of platinum drugs to tumors and reducing toxic side effects, providing a new theoretical basis for the targeted treatment of tumors in organisms.