177 results about "Drug targetting" patented technology

A solid drug solution perforator (SSP) system and an associated drug reservoir are provided for delivering therapeutic, prophylactic and / or cosmetic compounds, for nutrient delivery and for drug targeting. For drug delivery, the SSP system includes an active drug ingredient and a matrix of perforator material that biodegrades or dissolves quickly upon contact with a patient's body. The SSP system provides a skin barrier perforator and a controller for prompt initiation and cut-off drug delivery. In a preferred method of transdermal drug delivery, an SSP system containing a selected drug penetrates into an epidermis or dermis, and the drug is promptly released from the (dissolving) SSP system perforator. An additional drug is optionally delivered from a patch reservoir through skin pores created by insertion of the perforator. Formulation and fabrication procedures for the SSP and associated reservoir are also provided. An SSP system can be fabricated with variety of shapes and dimensions.

A composition comprising intact minicells that contain a drug molecule is useful for targeted drug delivery. One targeted drug delivery method employs bispecific ligands, comprising a first arm that carries specificity for a bacterially derived minicell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target drug-loaded minicells to specific mammalian cells and to cause endocytosis of the minicells by the mammalian cells. Another drug delivery method exploits the natural ability of phagocytic mammalian cells to engulf minicells without the use of bispecific ligands.

The present invention provides methods and compositions related to the fields of chemoinformatics, chemogenomics, drug discovery and development, and drug targeting. In particular, the present invention provides subcellular localization signals (e.g., chemical address tags) that influence (e.g., direct) subcellular and organelle level localization of associated compounds (e.g., drugs and small molecule therapeutics, radioactive species, dyes and imagining agents, proapoptotic agents, antibiotics, etc) in target cells and tissues. The compositions of the present invention modulate the pharmacological profiles of associated compounds by influencing the compound's accumulation, or exclusion, from subcellular loci such as mitochondria, endoplasmic reticulum, cytoplasm, vesicles, granules, nuclei and nucleoli and other subcellular organelles and compartments. The present invention also provides methods for identifying chemical address tags, predicting their targeting characteristics, and for rational designing chemical libraries comprising chemical address tags.

The invention is an apparatus and method for treatments and targeted drug delivery into a living patient, particularly but not exclusively using magnetic resonance (MR) imaging. The apparatus and method are useful in delivery to all types of living tissue and uses MR Imaging to track the location of drug delivery and estimating the rate of drug delivery. An MR-visible drug delivery device positioned at a target site (e.g., intracranial delivery) delivers a diagnostic or therapeutic drug solution into the tissue (e.g., the brain). The spinal distribution kinetics of the injected or infused drug agent are monitored quantitatively and non-invasively using water proton directional diffusion MR imaging to establish the efficacy of drug delivery at a targeted location.

Disclosed is a conjugate comprising a biologically active agent (drug) linked to a subcellular targeting moiety that targets a drug specifically to the nucleus. Targeting is achieved by attaching a steroid hormone (or an analog) to the drug. The steroid hormone attached to the drug binds its corresponding receptor, the formation of the receptor-ligand complex results in the internalization of the complex into the nucleus, thus resulting in nuclear translocation of the drug. Also disclosed is a conjugate (comprising the complex of the drug and the steroid hormone) bound to a polymer by spacers allowing for concurrent passive targeting to the tumor cell (afforded by attachment to the polymer by the EPR effect) and nuclear targeting of the conjugate (due to the presence of the steroid). Using a suitable degradable spacer allows for the release of free drug in the tumor and enhances nuclear targeting efficacy. The polymer can be further linked to a cellular targeting molecule, where the targeting molecule directs the polymer to specific cells. One may thus be able to effectively target drugs to the nucleus of tumor cells. With little or modifications, several therapeutic agents can be targeted using the invention.

Cyclic-GMP-AMP synthase (cGAS) and cyclic-GMP-AMP (cGAMP), including 2′3-cGAMP, 2′2-cGAMP, 3′2′-cGAMP and 3′3′-GAMP, are used in pharmaceutical formulations (including vaccine adjuvants), drug screens, therapies and diagnostics.

The present invention relates to therapeutic conjugates with the ability to target various antigens. The conjugate contains a targeting antibody or an antigen-binding fragment thereof and an anthracycline chemotherapy drug. The targeting antibody and the anthracycline chemotherapy drug are linked via a linker that includes a hydrazide moiety.

The invention discloses functional albumin and a preparation method of a nano preparation of the functional albumin. The nano preparation of the functional albumin consists of the functional albumin, metal ions and a drug; the metal ions can simultaneously form coordination bonds with the functional albumin and the drug, and can form nanoparticles through induced self-assembly. The nano preparation, through an endocytosis mediated by an albumin receptor (SPARC) on the surface of tumor cells, can deliver the drug into the drug-resistant tumor cells, so as to effectively avoid the exocytosis effect of a p-gp pump on the drug, and then as the coordination bonds break in an acid tumor cell environment through a pH responsibility, the drug releases in cytoplast, enters cell nucleus and inlays in DNA so as to inhibit the synthesis of nucleic acid; and therefore, the growth of the tumor cells is inhibited. Through in vitro characterization, the nano preparation can achieve the relatively good pH responsibility; and through activity evaluation on a cellular level, the system is capable of effectively delivering the drug into the cells, so as to achieve relatively good pH responsive release.

The invention belongs to the field of pharmaceutic preparation, and relates to a targeted drug-carrying liposome of a tumor associated fibroblast. The surface of the targeted drug-carrying liposome is modified with a high-affinity ligand of a specific expression protein of the tumor associated fibroblast. The targeted drug-carrying liposome is capable of realizing targeted delivering of drugs into the tumor associated fibroblast, realizing intervention on tumor microenvironment via action on the tumor associated fibroblast, and realizing tumor treatment. And in addition, the tumor associated fibroblast targeted preparation can be combined with routine tumor cell targeted nano preparations so as to improve antitumous effects of the routine tumor cell targeted nano preparations.

The invention discloses an mRNA nucleic acid drug delivery system, a preparation method and application. The system comprises lipid nanoparticles used for loading one or more mRNAs, and the lipid nanoparticles are prepared from raw materials including ionizable cationic lipid, phospholipid auxiliary lipid, cholesterol and phospholipid polyethylene glycol derivatives. According to the non-viral-vector mRNA nucleic acid drug targeting intracellular delivery system, mRNA is concentrated and loaded through the electrostatic interaction of ionizable cationic lipid and the mRNA, the phospholipid auxiliary lipid component-mediated pH sensitivity and advanced inclusion escape can enable an mRNA nucleic acid drug to be efficiently delivered to target cells, and the mRNA nucleic acid drug is released to cytoplasm of the target cells to play a pharmacodynamic role. The phospholipid auxiliary lipid increases the advanced inclusion escape ability of the mRNA / lipid nanoparticles, and increases the stability of the mRNA / lipid nanoparticles and the mRNA transfection efficiency. The system has efficient and stable mRNA drug intracellular delivery efficiency, and significantly improves the prevention and treatment effects of mRNA nucleic acid drugs.

The invention discloses a novel lipid material. The novel lipid material is used for prolonging the circulating time and increasing the transfer amount of medicine to brain tumor tissues in a target way. The novel lipid material is characterized in that polyethylene glycol is used as a bridge, one side of the bridge is connected with cholesterol, and one side of the bridge is connected with glucose and RGD (arginine-glycine-aspartic acid) peptide, so that the lack of brain tumor targeting ability by the lipid modified by the single glucose or the RGD peptide is overcome, and the brain tumor can be effectively targeted after blood brain barrier crossing. The novel lipid material can be used for different preparation types of lipids, nanoparticles, micelles and the like; the prepared paclitaxel-carrying lipid has obvious brain tumor targeting function, and broad application prospect.

The invention relates to an intracellular triggering reduction sensitive drug linked gene targeted co-carrier which is a gene and drug double-loaded system and comprises disulfide bond cross-linked polyethylene imine, a poly-lactide glycolide copolymer and a surface modified targeted micromolecule. According to the invention, the surface modified active targeted group of a carrier can target drugs to a tumor part and enrich the drugs; a disulfide bond cross-linked in a polymer can be broken in a cell under the condition of high reduction, and the structure of the carrier is disassembled so that the drugs are released. The intracellular triggering reduction sensitive drug linked gene targeted co-carrier disclosed by the invention can effectively load the gene and the hydrophobic micromolecular drug, ensure the stability of the gene and is degraded and releases the gene and the micromolecular drug under the condition of reduction. An in-vivo experiment shows that the intracellular triggering reduction sensitive drug linked gene targeted co-carrier disclosed by the invention has outstanding targeting on tumors.

The present invention provides tumor homing molecules, which selectively home to a tumor. The invention also provides methods of using a tumor homing molecule to target an agent such as a drug to a selected tumor or to identify the target molecule expressed by the tumor. The invention also provides methods of targeting a tumor containing angiogenic vasculature by contacting the tumor with a molecule that specifically binds an alphav-containing integrin. The invention further provides molecules that can selectively home to angiogenic vasculature. In addition, the invention provides a target molecule, which is specifically bound by a tumor homing molecule and is expressed by angiogenic vasculature. The invention also provides antibodies that bind to the target molecule and peptidomimetics that competitively inhibit binding of a ligand to the target molecule.

This invention relates to a highly efficient artificial low-density lipoprotein (LDL) carrier system for the targeted delivery therapeutic agents across the blood-brain barrier (BBB). In particular, this invention relates to artificial LDL particles comprised of three lipid elements: phosphatidyl choline, fatty-acyl-cholesterol esters, and at least one apolipoprotein. The present invention further relates to compositions, methods and kits comprising artificial LDL particles for targeting drugs to and across the BBB for the prevention and treatment of brain diseases.

Disclosed herein are drug delivery devices and methods for the treatment of ocular disorders requiring targeted and controlled administration of a drug to an interior portion of the eye for reduction or prevention of symptoms of the disorder. In several embodiments, the devices are capable of controlled release of two or more drugs, the release of each drug into a different ocular space (e.g., an ocular compartment versus an ocular fluid outflow pathway).

The invention discloses a method for predicting drug targeting protein-to-protein interaction (PPI) based on multivariate data. According to the method, with the judgment whether a drug is targeted to protein-to-protein interaction as the research object, an integrated classifier algorithm for predicting the drug targeting protein-to-protein interaction based on eleven characteristics such as the structure, function and amino acid sequence of protein is developed. The prediction method can be used for predicting whether interaction exists between protein and protein or not and whether the interaction target of a drug and protein occurs in the protein binding interface (PPI interface) or not.

The invention relates to a target drug feeding system with combination of nano-silver and curcumin or a curcumin derivative and belongs to the technical field of biological medicines. The nano-silver target drug feeding system particularly takes an aptamer as a target point; the curcumin or the curcumin derivative or the nano silver is used as a combined anti-tumor drug and is polymerized to the outer surface of a biodegradable high-molecular polymer nano-system (PNS) by the aptamer to synthesize an aptamer-PNS polymer which is used as a shell; the PNS simultaneously encapsulates the curcumin or the curcumin derivative and the nano silver, so as to prepare the nano-silver target drug feeding system which is loaded with active components including the curcumin or the curcumin derivative and improve the solubility and bioavailability of the curcumin and the curcumin derivative; meanwhile, drugs can be targeted into non-small-cell lung cancer cells or prostate cancer cells; the anti-tumor effects of the curcumin or the curcumin derivative and the nano silver are expressed so that the target drug feeding and drug slow releasing effects are realized; the nano-silver target drug feeding system is used for preventing and treating lung cancers and prostatic cancers, the treatment effect is improved and the toxic side effect is reduced.

The invention discloses a nano cell membrane drug-loaded vesicle, a preparation method and application thereof. The preparation method is characterized in that through a physical extrusion technology,drug coating is carried out in the process of forming nanoscale cell membrane vesicles, no influence is generated on the activity of a coated drug, the in-vivo circulation time of the drug can be prolonged, the drug targeting ability is improved, and directional slow release of the drug is realized. The preparation method comprises the steps of cell membrane acquisition and cell membrane nano-vesicle preparation. Specific cell delivery of the drug targeting specific part can be realized, so that the drug fully plays a therapeutic role, and liver and kidney injury caused by one-time massive drug aggregation in the liver or kidney is prevented. Dynamic changes in a drug body can be tracked through probe wrapping.

The present invention discloses a new type medicine target slowly-releasing carrier material and its preparation process. Said medicine target slowly-releasing carrier material is made up by utilizing attapulgite and Fe3O4. Its principle lies in that it utilizes the large specific surface area and adsorbability of ultrafine high-purity attapulgite and uses it as carrier material of medicine to prolong action time of medicine in interior of human body, raise concentration of local medicine, raise therapeutic effect of medicine and reduce toxic side effect of the medicine, and utilizes magnetization treatment so as to attain the goal of making target administration and controlling release of medicine.

The invention discloses a novel lipid material which is used for prolonging the circulation time and increasing drug targets to be transmitted to the brain. According to the novel lipid material, polyethylene glycol is used for bridging, one side of polyethylene glycol is connected with cholesterol, and the other side of polyethylene glycol is connected with glucose and vitamin C, so that the defect of the targeting capability of lipidosomes modified by single glucose or vitamin C is made up for, transfer for crossing a blood-brain and blood-brain spinal fluid dual barrier is achieved, the brain targeting of drugs is improved, and the central concentration of the drugs is increased. The novel lipid material can be used for different dosage forms including liposomes, nanoparticles and micelles, and paclitaxel liposomes prepared from the material have an obvious brain targeting function and wide application prospects.

The present invention provides tumor homing molecules, which selectively home to a tumor. The invention also provides methods of using a tumor homing molecule to target an agent such as a drug to a selected tumor or to identify the target molecule expressed by the tumor. The invention also provides methods of targeting a tumor containing angiogenic vasculature by contacting the tumor with a molecule that specifically binds an alphav-containing integrin. The invention further provides molecules that can selectively home to angiogenic vasculature. In addition, the invention provides a target molecule, which is specifically bound by a tumor homing molecule and is expressed by angiogenic vasculature. The invention also provides antibodies that bind to the target molecule and peptidomimetics that competitively inhibit binding of a ligand to the target molecule.

The site-specific expression of selectins on endothelial cells of blood vessels during angiogenesis provides an opportunity to target anti-cancer drugs to the vascular endothelium to extend the range of the therapeutic effect. This invention describes an innovative drug targeting strategy for the selective delivery of the anticancer drugs to endothelial cells by means of polymer-drug conjugates modified with a carbohydrate ligand for the vascular selectins. A model chemotherapeutic drug, doxorubicin, and the E-selectin ligand, sLex, are attached to a biocompatible polymer (HPMA). The selective binding, cellular uptake, intracellular fate, and cell cytotoxicity of the polymer-bound drug are investigated in human endothelial cells.

The invention discloses a high-molecular material containing cholic acid and a drug-loaded nanoparticle modified by the same. The material has a structural formula as represented by formula III, and n in the formula is equal to 25 to 40. Monomers of the material are obtained by reacting hydroxy groups at C3 position of cholic acid methylester with 4-vinylbenzyl chloride and are initiated by an initiator so as to obtain a polymer precursor; ester groups at C24 position of the polymer precursor are hydrolyzed and turn into carboxyl groups so as to obtain the material in the invention. The material has amphipathy and is capable of assembling and of modifying the surface of the nanoparticles in the process of preparing the nanoparticles by using the method of emulsification-solvent evaporation. The molecular structure of cholic acid in the material can specifically bind to bile acid transporters on the surface of parenchymal hepatic cells; under the mediation of the bile acid transporters, the nanoparticles are absorbed by the parenchymal hepatic cells, and therefore, a drug is targetedly delivered to the parenchymal hepatic cells. Thus, the material provided in the invention can be used as an ideal surface modification material for development of a liver-targeting nanometer drug loading system.

The invention discloses a nucleic acid medicine loading system for targeted therapy and a preparation method of the nucleic acid medicine loading system. The system is adduct consisting of DNA (deoxyribonucleic acid) aptamers as medicine carriers and targeted probes and anticancer medicine loaded onto the DNA aptamers. The targeted identification specificity, high stability and easy modification of the DNA aptamers are utilized, and the DNA aptamer-anticancer medicine adduct is prepared, so small molecule medicine is modified onto the DNA aptamers. The DNA aptamers are very stable at the solid state or low temperature liquid state (such as the temperature below 10 DEG C) and is suitable for being stored for a long time. The adduct maintains the identification specificity of the original DNA aptamers to targeted cancer cells, medicine can be conveyed to cancer cells in a targeted way and can be gradually released at the physiological temperature, the special killing and injury effect on the targeted cancer cells is generated, the side effect is reduced, and the curative effect is improved. The nucleic acid medicine loading system and the preparation method have the advantages that the preparation process is simple, economy is realized, the efficiency is high, and the preparation process is suitable for mass production and is particularly suitable for being used for preparing the targeted medication anticancer medicine.

The invention relates to a preparation method and application of a drug delivery system of a targeting gold-silver alloy nanocage, in order to effectively solve the problems of an existing tumor treatment medicines which are high in side effect and poor in treatment effect; the system is a drug delivery system formed by loading a gene drug on a targeting gold-silver alloy nanocage gene vector, wherein the mass ratio of the targeting gold-silver alloy nanocage gene vector to the gene drug is at ((1-12)*106) to 1; and the targeting gold-silver alloy nanocage gene vector is formed by linking targeting tumor molecule folic acid and a cationic polymer, namely polyethyleneimine (PEI), to the surface of a gold-silver alloy nanocage by virtue of a chemical bond or an electrostatic interaction. The drug delivery system disclosed by the invention is good in physical and chemical stability, simple and feasible in preparation condition, rich in raw material source, low in cost and low in side effect; and the drug delivery system can be used for effectively inhibiting tumor cell proliferation in coordination with thermal therapy by loading the gene drug and targeting to tumor parts, being an innovation of vector in tumor gene therapy and photo-thermal therapy.

The invention discloses ferritin nanoparticles of C-terminal modified tumor penetrating peptide RGERPPR and a preparation method and application of the ferritin nanoparticles. The C terminal of the ferritin nanoparticle is modified with a tumor penetrating peptide RGERPPR, the tumor penetrating peptide RGERPPR is connected with the C terminal of ferritin through a connecting sequence, and the tumor penetrating peptide RGERPPR is exposed to the outside of ferritin. The C-terminal modified tumor penetrating peptide RGERPPR ferritin nanoparticles have strong targeting ability and cell penetratingpower, and can be strongly combined with tumor cells, and the prepared anti-tumor drug has strong cytotoxicity, provides a very good carrier model for subsequent drug targeting tumor cell treatment,and has a very good application prospect.

The invention discloses a method for determining the concentrations of two anti-tumor drugs, metabolites and endogenous substances related to the activity of a metabolic enzyme in human plasma, whichcomprises the following steps: preprocessing, respectively taking voriconazole and bromouracil as internal standards, separating drug components in supernate by using high performance liquid chromatography in a preprocessed sample, performing drug targeting detection by using a high-resolution mass spectrum multi-reaction monitoring mode, and quantifying to realize the analysis and determination of the concentrations of the two anti-tumor drugs, the metabolites and the endogenous substances related to the activity of the metabolic enzyme in the plasma. The method has the advantages of rapidness, extremely high targeting property, high flux, high sensitivity, strong specificity, good precision and accuracy, good stability, high extraction recovery rate, no obvious matrix effect and dilutioneffect and the like. The method for determining the concentrations of two anti-tumor drugs, metabolites and endogenous substances related to the activity of the metabolic enzyme in the human plasma can be used for monitoring the blood concentration of irinotecan and metabolites thereof and the blood concentration of fluorouracil and endogenous substances related to the activity of the metabolic enzyme thereof clinically.

The invention relates to a synthesis method of an organic mineralized structure based on framework nucleic acid coding. The method includes following steps: synthesizing a framework nucleic acid whichstably exists in a solution containing Mg<2+> or Ca<2+>; providing a cationic cluster with a mineral element that is Si or Ca; and bonding the cationic cluster and the phosphate skeleton of the framework nucleic acid by electrostatic attraction to form a nucleic acid-inorganic composite, thus solving a synthesis problem of the organic mineralized structure. The invention further relates to the nucleic acid-inorganic composite synthesized by the method, and applications of the nucleic acid-inorganic composite in preparation of composites of the nucleic acid-inorganic composite and metal or metal oxide, preparation of silica nanopores used for sequencing, preparation of organic inorganic multi-element composite materials with stable configuration or porous materials used for membrane separation techniques and preparation of mesoporous silica for drug targeted transport.

A composition and method of fabrication are presented with which nanoparticles may be used as a tool to deliver drugs to a specific target within or on a mammalian body. Specifically, by using stabilizers other than Dextran 70.000 during the polymerization process, according to the present invention, surfactants, which were deemed necessary coating material in the prior art, are no longer required. This is a significant simplification of the fabrication procedure. Many substances are useful as stabilizers, but the preferred stabilizers comprise Dextran 12.000 or polysorbate 85. In the present invention a drug is either incorporated into or adsorbed onto the stabilized nanoparticles. This drug / nanoparticle complex is then administered to the organism on any route such as by oral application, injection or inhalation, whereupon the drug exerts its effect at the desired site of pharmacological action. In a novel medical treatment process, the drug / nanoparticle complex may be administered preferably either by intravenous injection or by oral application. The resulting drug action, which does not occur or which occurs only to an insufficient extent when the drug is administered alone, shows that when linked to said nanoparticles drugs can reach a specific target within or on the mammalian body. The usefulness of the present invention as a universal approach to deliver any drug or diagnostic agent to a specific target within or on the mammalian body was demonstrated by experiments showing an unexpected transfer of the drug across the blood brain barrier.

The invention discloses a preparation method for drug targeting controlled release nano-particle eye drops, which pertains to the preparation methods of eye preparations. The invention firstly dissolves certain portions by weight of drug and biodegradable polymer in organic solvent so as to obtain solution A; additionally, certain portions by weight of cholesterol modified chitosan is dissolved in water, and solution B is obtained by stirring and rotating; the two are mixed and stirred till the organic solvent is fully volatilized; the drug-carrying polymer nanoparticles are obtained by centrifugal separation, water washing and drying; and then the eye drops are prepared by the general preparation method of the industry of eye drops. The eye drops which are prepared by the method of the invention can ensure the effective drug treatment concentration without the need of frequent and high-concentration drug delivery, can significantly prolong the eye surface acting time of the drug and release the drug continuously and constantly, the eye surface retention time of the drug-carrying particles of the eye drops can be up to six hours, the efficacy is improved and the side effects of the drug are reduced simultaneously.