165 results about "Drug targetting" patented technology

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.

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 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.

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 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 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.

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.

The invention relates to compounds that have been identified as CDK4 (cyclin-dependent kinase enzyme) inhibitors for the first time, for use as a medication, in particular, for the treatment of cancers e.g. those with overexpression of the enzyme CDK4, and to pharmaceutical compositions comprising same. Said compounds target the interaction interface between CDK4 and its activating cyclin, whereas those drugs already approved for the treatment of cancers with overexpression of the enzyme CDK4 target the ATP-binding site.

This application relates to the biomedical technology field, and more specifically to a tumor therapy method combining recombinant oncolytic viruses and small molecule anticancer drugs. Specifically, it includes the step of treating a tumor using recombinant oncolytic viruses and small molecule anticancer drugs in combination, wherein the small molecule anticancer drugs include ALK-targeting small molecule anticancer drugs, BTK-targeting small molecule anticancer drugs, EGFR-targeting small molecule anticancer drugs, FGFR-targeting small molecule anticancer drugs, HER2-targeting small molecule anticancer drugs, Parp-targeting small molecule anticancer drugs, PI3K-targeting small molecule anticancer drugs, VEGFR-targeting small molecule anticancer drugs, CDK4 / 6-targeting small molecule anticancer drugs, and KRAS-targeting small molecule anticancer drugs, and the recombinant oncolytic viruses include site-directed mutagenesis of M protein, G protein, N protein, P protein, and L protein. In this application, it is possible to achieve an effect greater than 1+1 by using recombinant oncolytic viruses and low-molecular-weight anticancer drugs in combination to attack and kill tumor cells.

The present invention relates to a micro-nano robot, and more specifically, a micro-nano robot that is targeted to dissolve tophi. The micro-nano robot consists of a head and a tail, and the head and the tail form a rigid-flexible composite structure. The rigid-flexible composite structure is a rigid head and a flexible tail. The rigid head has a plurality of cavities. The cavity is provided with a nano switch and an acidity response module. The flexible tail of the micro-nano robot is a flexible spiral drill structure tail, and the flexible spiral drill structure tail is covered with magnetic particles. The rigid head of the micro-nano robot is an ultrasonic sensitive structure head, that is, the front end of the ultrasonic sensitive structure head is an asymmetric structure. The flexible tail of the micro-nano robot is a flexible spiral drill structure tail. The micro-nano robot can be loaded with a variety of composite drugs for targeted transportation, and the amount of drug release can be regulated in the lesion area, so that tophi can be dissolved accurately and efficiently.

The invention belongs to the technical field of biological medicine, and particularly relates to a drug-loaded nano-selenium particle and a preparation method and application thereof, the drug-loaded nano-selenium particle uses tea polysaccharide modified nano-selenium particle as a carrier to load doxorubicin hydrochloride, and the drug-loaded nano-selenium particle is encapsulated by a metal zeolite imidazole skeleton. DOX is loaded to the surfaces of the particles by utilizing physical adsorption and functional groups on the surfaces of the tea polysaccharide nano-selenium particles. Due to the porous structure and the self-assembly characteristic of the metal zeolite imidazole skeleton, the DOX-loaded tea polysaccharide nano-selenium particles are wrapped to form the drug-loaded nano-selenium particles. The tea polysaccharide nano-selenium particles serve as a drug carrier, ZIF-8 serves as a shell, the tea polysaccharide nano-selenium particles internally loaded with DOX can be protected, and drug targeted delivery can be achieved through the acid-sensitive characteristic of the tea polysaccharide nano-selenium particles. DOX is modified through the process, toxic and side effects generated by DOX are reduced, and it is not found that the drug-loaded nano-selenium particles have liver and kidney toxicity, the bone marrow hematopoiesis inhibiting function, delayed cardiotoxicity and toxic and side effects causing alopecia.

According to the selective organ targeting endoplasmic omentum fusion nano delivery platform and the application thereof, the platform realizes bidirectional regulation and control of organ targeting selectivity and cell membrane fusion efficiency through reasonable design of components and proportions on the basis of the synergistic effect of functional lipid combination, and the delivery efficiency of the endoplasmic omentum fusion nano delivery platform is improved. The problems that the organ specificity accumulation of a traditional delivery system for delivering drugs is insufficient, the release efficiency of intracellular drugs after delivery is low and the accumulation of organelles is limited are solved, and the drugs are delivered to specific organs in a targeted manner and are highly fused with endoplasmic reticulum membranes of cells in the organs; the method can be widely applied to the treatment of organ specificity and endoplasmic reticulum related diseases, such as lung intracellular bacterial infection treatment, pulmonary fibrosis treatment, anti-tumor vaccine construction and the like. The raw materials for construction of the platform are easy to obtain, and the platform is prepared by adopting a scalable simple process and has a good clinical transformation prospect.

The invention belongs to the technical field of bioengineering, and provides a drug-loaded targeted nano platform for targeted delivery of ZIF-8 drug-loaded nanoparticles by macrophages, a preparation method and an application, aiming at the technical problem that complications are easily caused by the existing treatment means of endometriosis, so that the invention provides a drug-loaded targeted nano platform for targeted delivery of ZIF-8 drug-loaded nanoparticles by macrophages, and a preparation method and application of the drug-loaded targeted nano platform. According to the invention, the ZIF-8 nano-particles and the drugs aiming at the energy metabolism level are combined to be used as the carrier, so that endometriosis cells with acidic cell microenvironment can be targeted, drug controlled release can be realized in the acidic environment of lesions, and the effective uptake of the endometriosis cells to the drugs is enhanced, thereby effectively increasing the uptake rate and the drug concentration at the target position, and improving the curative effect of the drug on the endometriosis cells. Meanwhile, the distribution of the medicine in normal tissues or cells is reduced, and the toxic and side effects of the medicine are reduced; and through the design of combining the macrophages with the ZIF-8 nano-particle carrier, the drug targeting property of the ZIF-8 nano-particle carrier can be obviously improved.

The invention relates to the technical field of nano-drug delivery systems, in particular to an oleuropein-loaded core-shell structure drug delivery system as well as a preparation method and application thereof. The invention relates to an oleuropein-loaded core-shell structure drug delivery system, which comprises an inner core and an outer shell, the inner core is an oleuropein nanoparticle formed by self-assembly of oleuropein; the oleuropein nanoparticles are cross-linked and modified with sodium tripolyphosphate and covalently connected with folic acid; the shell is formed from ferulic acid derived lignin. According to the scheme, efficient targeted delivery and collaborative treatment of the oleuropein in treatment of sepsis-related intestinal dysfunction are achieved, the technical problems that when the oleuropein is applied to treatment of sepsis, the drug targeting property is not high, the bioavailability is not ideal, and target site release cannot be achieved can be solved, and the application of the oleuropein to treatment of the sepsis is promoted. The invention opens up a new way for developing a novel efficient targeting drug delivery system, provides an innovative strategy for clinical conversion of natural products, and has ideal application and popularization values.

The application provides a drug delivery system for targeted treatment of inflammatory diseases and a preparation method and application thereof, and belongs to the technical field of biological drugs. The drug delivery system for targeted treatment of inflammatory diseases is M2 type macrophages phagocytizing drug-loaded nanoparticles, wherein the drug-loaded nanoparticles comprise a biodegradable high molecular material for coating drugs. The drug delivery system prepared by the application realizes lung targeted delivery through the natural inflammatory chemotaxis characteristics of M2 type macrophages, and in combination with the drug slow-release effect of the drug-loaded nanoparticles, the drug targeting and availability are significantly improved, so that the drug efficacy is improved, the biological safety is good, and a new effective means is provided for the clinical treatment of various inflammatory diseases including carbapenem-resistant Klebsiella pneumoniae (CRKP) pneumonia.

According to the invention, a polymer prodrug is designed and prepared, and a dasatinib (DAS) and triphenylphosphine-adriamycin (TPP-DOX, TD) co-loaded nano-micelle is constructed; the preparation method has the advantages that 1) the optimal preparation process of the polymer micelle is determined by a single factor investigation method, namely the optimal nano-micelle is prepared by using a dialysis method and taking DMF (Dimethyl Formamide) as a solvent according to the mass ratio of a prodrug material to a carried drug being 15: 1, and the preparation method is simple and clear and is easy to industrialize; 2) the particle size is small and uniform, so that the nanoparticles can be enriched at a tumor part through an EPR effect; 3) the amphiphilic micromolecule prodrug improves the water solubility of DAS, improves the drug stability, has high drug loading capacity, and avoids adverse reactions possibly caused by carriers and auxiliary materials; and 4) the polymer nano-micelle co-loaded with the DAS and the TPP-DOX has good MMP-2 sensitive responsiveness, enhances the drug targeting delivery capability, has good blood compatibility and safety, improves the drug curative effect, reduces the toxic and side effects, and has a good tumor MDR reversing effect.

The invention relates to the technical field of radiopharmaceutical research and development, and discloses a radiotargeted nuclide drug molecule design method based on a first principle, comprising: screening a high-specificity target based on a preset demand, and screening candidate nuclides according to drug functions and ligand types corresponding to the high-specificity target; the method comprises the following steps: setting a difunctional chelating agent adaptive to candidate nuclides, setting a ligand for a high-specificity target, setting a linker for connecting the difunctional chelating agent and the ligand, calculating and optimizing the difunctional chelating agent, the ligand and the linker according to a first principle, and assembling according to a nuclide-chelating agent-linker-ligand sequence to obtain an initial molecular complex; and for alpha nuclide in the initial molecular complex, calculating and optimizing through a first principle to obtain a target molecular complex. According to the method, by constructing collaborative design logic, the drug targeting property, stability and the balance capacity of the curative effect and safety are improved, special optimization is carried out for alpha nuclide risks so as to reduce toxicity, and extensive expandability is achieved.

The invention relates to the technical field of radiopharmaceuticals, and discloses a targeted GPC3 polypeptide ligand, which has a structural general formula: C-L-P, wherein C is a chelating group; l is a linker; p is a targeted phosphatidylinositol proteoglycan-3 (GPC3) polypeptide pharmacodynamic group; the linker is a covalent linker or a reversible non-covalent linker. The invention has the following technical effects: by introducing the covalent linker or the reversible non-covalent linker, the chemical structure of the targeted GPC3 polypeptide ligand is optimized, the targeting property of the targeted GPC3 polypeptide radiopharmaceutical is improved, and the pharmacokinetic characteristics are improved; the defects that an existing targeted GPC3 polypeptide radiopharmaceutical is low in tumor uptake, short in tumor residence time, poor in pharmacokinetic characteristic and the like are overcome. The invention further discloses a targeted GPC3 polypeptide radiopharmaceutical as well as a preparation method and application of the targeted GPC3 polypeptide radiopharmaceutical.