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62 results about "Bio distribution" patented technology

Reversibly crosslinked biodegradable polymersome with asymmetric membrane structure as well as preparation method and application thereof to nucleic acid medicines

The invention discloses a reversibly crosslinked biodegradable polymersome with an asymmetric membrane structure as well as a preparation method and application thereof to nucleic acid medicines. The polymersome and the preparation method have the advantages that a triblock polymer PEG-P(TMC-DTC)-PEI or PEG-P(DLLA-DTC)-PEI is synthesized and is self-assembled and self-crosslinked to obtain the polymersome with the asymmetric membrane structure or the triblock polymer is linked with a targeting molecule and is self-assembled to obtain targeting RCCPs; the inner shell of the polymersome is PEI and is used for compounding and loading nucleic acid through electrostatic interaction; a membrane is reversibly crosslinked biodegradable polyester / polycarbonate with good biocompatibility; dithiolane of a side chain is similar to a human body natural antioxidant lipoic acid; the outer shell of the polymersome takes PEG as the background and can target cancer cells; by studying that the carrier is compounded with functional siRNA and studying the gene silencing effects in vitro and vivo, in vivo blood circulation and bio-distribution, the condition of treating lung cancer in situ bearing mice and toxic and side effects of the polymersome, the polymersome is expected to become a nanosystem platform integrating the advantages of simplicity, stability, multifunction, and the like and is used for carrying out efficient and active targeting delivery on siRNA to tumors in situ.
Owner:SUZHOU UNIV

Protein-polymer combination and preparation method thereof

The invention discloses protein-polymer combination and a preparation method thereof. The polymer is combined to the protein through an initiator connected to the protein, and the initiator can be connected to the N- end or the C- end of the protein and any position which is far away from the protein activity site and / or where the protein activity is not influenced. The interferon-polymer combination which is prepared with the method and has the specific site not only reserves bioactivity in vitro better, but also greatly improves the half-life period, bio-distribution and anti-tumor effect of interferon in vivo, so that firm technological base of is established for clinical transformation of potent interferon; and besides, the in-situ fixed-point polymerization method can further be widely applied to other protein or small peptide drugs to improve the pharmacological characteristics.
Owner:TSINGHUA UNIV

Primer for specifically detecting human genome DNA and application thereof

The invention discloses a method for detecting human DNA by specifically detecting the human SRGAP2 gene, a primer and probe for specifically detecting the human SRGAP2 gene, and a TaqMan qPCR methodcapable of being used for detecting the human DNA in animal organs, tissue, cells, body fluid and blood. The method is suitable for detecting the human DNA in any animal sample and includes but not limited to biochores, metabolism and residues of cell and gene treatment products in the body of an animal receiving treatment.
Owner:SHANGHAI AISAER BIOTECH CO LTD

RNAi CONJUGATES, PARTICLES AND FORMULATIONS THEREOF

Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, comprising conjugates of an RNAi agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the RNAi agent and / or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
Owner:TVA (ABC) LLC

Novel 18F labeled aromatic amino acids, preparation method and application thereof in tumor imaging

The invention discloses novel radioactive 18F labeled aromatic amino acids, which is characterized in that one end of the acids is provided with F substituted alkoxy benzoyl structure, and the other end of the derivatives is provided with alpha-amino acid structure; substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; R2 is methoxyl group; and n is a number between 1 and 5. The substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; the R2 is methoxyl group; and the n is a number between 1 and 5. Compounds improve fat solubility. Different amino acid structures are introduced into the structure, and F in the structure is 19F and 18F. The substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; the R2 is methoxyl group; and the n is a number between 1 and 5. The substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; the R2 is methoxyl group; and the n is a number between 1 and 5. Compared with the prior art, the 18F labeled amino acid derivatives provided by the invention have better discrimination degree of biological distribution, the potential of being used as a tumor imaging agent (particularly a brain tumor imaging agent), as well as the characteristics of simple preparation and high labeling rate.
Owner:BEIJING SHENLANHAI BIO PHARM TECH

Targeted conjugates and particles and formulations thereof

Nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker have been designed. Such nanoparticles and microparticles can provide improved temporospatial delivery of the active agent and / or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
Owner:TVA (ABC) LLC

Antibody mimic conjugates and particles

Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, comprising conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and / or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
Owner:TVA (ABC) LLC

2-aryl benzothiazole compound with high affinity with a(BETA) plaque and preparation method and application thereof

The invention provides a 2-aryl benzothiazole compound with high affinity with A(beta) plaque and a preparation method and application thereof. The structure of the compound is shown by formula (I). In-vitro competitive binding experiments indicate that the kind of molecules have medium affinity with the A(beta) 1-42 aggregate; in-vitro autoradiography experiments indicate that the molecules marked by Tc-99m can be combined with the A(beta) plaque in blood vessels of the brain with specificity and high affinity; in-vivo bio-distribution experiments on a normal mice indicate that a developer partially marked by Tc-99m has the advantages of low initial brain extraction, fast blood removal and the like, and is expected to become a new single-photon A(beta) plaque developer for early-stage clinical diagnosis of CAA (cerebral amyloid angiopathy) or AD (Alzheimer's disease).
Owner:BEIJING NORMAL UNIVERSITY

Obstruction type multi-module water quality biological detection equipment and method

The invention discloses obstruction type multi-module water quality biological detection equipment and an obstruction type multi-module water quality biological detection method. The equipment comprises an obstruction index selection module and a water quality testing device, wherein the obstruction index selection device is used for selecting a qualified or effective gradient obstruction degree combination, and the water quality testing module is used for detecting the water quality of the water body to be detected according to the behaviors of indicator organisms passing through each obstruction in the effective obstruction degree combination after being injected into the water body to be detected. According to the method, on the basis of behavior difference of the indicator organisms ina clean water body and a polluted water body, the distribution area of the indicator organisms is counted by establishing the relationship between the water body pollution degree and the distributionarea of the indicator organisms so as to determine the pollution degree of the water body. The method can accurately and quickly detect the pollution degree of the water body, does not need chemicalanalysis, physical detection and other technologies, and has the advantages of low cost, quick operation, accurate result and the like.
Owner:HOHAI UNIV +1

Targeted ligands

The invention contemplates a composition containing a multispecific ligand containing at least a first ligand binding moiety and a second ligand binding moiety. The first ligand binding moiety specifically binds with a pre-selected first affinity to at least a first ligand. The first ligand has a first biodistribution. The second ligand binding moiety specifically binds with a pre-selected affinity to at least a second ligand. The second ligand has a second biodistribution. The affinity of first and second ligand binding moieties are selected to bias the biodistribution of the multispecific ligand in favor of a selected location of one or both of the ligands.
Owner:HERMAN WILLIAM

2-Alkoxy-6-[18F]fluoronicotinoyl substituted Lys-C(O)-Glu derivatives as efficient probes for imaging of PSMA expressing tissues

6-[18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [18F]PSMA-1007 and [Al18F]HBED-CC-PSMA. Unexpectedly, the 6-[18F]fluoro-2-alkoxy and 6-[18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the 18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.
Owner:UNIV OF COLOGNE

Protein-based pharmacological active substance composition, and preparation method and applications thereof

A protein-based pharmaceutical active substance composition, the preparation method therefor, and the use thereof. The pharmaceutical active substance delivery system comprises solid or liquid pharmaceutical active substance and particulates composed of protein coating, wherein the protein coating includes free protein associated therewith, the part of pharmaceutical active substance is wrapped in the protein coating and the other part of pharmaceutical active substance is associated with the free protein, the particles have an average particle diameter of 10-200nm. Maximum kinetic hydrated particle size is over 10nm when the particles are dispersed in an aqueous solution. The pharmaceutical active substance delivery system will not quickly dissociate to the size of 10nm or less when it is dissolved and diluted by the injection, thus the effect of enrichment in the tumor site and the bio-distribution are improved.
Owner:THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA

Targeted constructs and formulations thereof

Targeted constructs and pharmaceutical formulations thereof, comprising at least one conjugate of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via an optional internal linker moiety have been designed which can provide improved temporospatial delivery of the active agent and / or improved biodistribution. Methods of making the targeted constructs and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
Owner:TVA (ABC) LLC

Micromolecule lung cancer targeted radioactive therapeutic agent and preparation method thereof

The invention discloses a micromolecule lung cancer targeted radioactive therapeutic agent. Isotope 131I is marked with eight-peptide molecules with XGXG structures, wherein G shows L glycine, and X shows optional one of 20 amino acids. The invention further discloses a preparation method of the micromolecule lung cancer targeted radioactive therapeutic agent. The micromolecule lung cancer targeted radioactive therapeutic agent has good stability and biological distribution characteristics, can obviously suppress growth of tumour in a human lung cancer nude mouse animal model body, does not have obvious toxic and side effects to vitals such as livers, kidneys, lungs, hearts and the like, is applicable to targeted therapy for patients suffering from non-small cell lung cancer (squamous carcinoma and glandular cancer), and has an important clinical application value in the aspect of molecule targeted treatment for lung cancer.
Owner:ZHUJIANG HOSPITAL SOUTHERN MEDICAL UNIV

Pharmaceutical composition, a method of preparing it and a method of treatment by use thereof

InactiveUS20080131498A1Overcomes insolubility problemEliminate side effectsBiocideTetrapeptide ingredientsSide effectOral medication
Pharmaceutically acceptable liposome-encapsulated busulphan formulations for parenteral administration are provided, as well as such formulations furthermore comprising glutathione and / or at least one glutathione precursor and a process for manufacture of the preparations. The formulations are stable, have improved biodistribution and significantly reduced side effects over those produced by oral administration or parenteral administration of free drug. The formulations are useful as part of stem cell and / or bone marrow transplant conditioning regimens. A method of treatment of a mammal by use of such formulations.
Owner:BUSULIPO

Hsp90-targeting conjugates and formulations thereof

Conjugates of an active agent attached to a targeting moiety, such as an HSP90 binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and / or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.
Owner:TVA (ABC) LLC

Precise block polymer nanoassembly and preparation method thereof

The invention provides a precise block polymer nanoassembly and a preparation method thereof. According to the invention, a precise amphiphilic block polymer with a structure as shown in a formula I is adopted as a matrix; and a controllable nanoassembly, namely a spherical micelle and / or rod-like micelle structure can be formed by adjusting the length and sequence structure of a hydrophobic chain segment and utilizing of cooperation with other operations and condition control; and the obtained nanoassembly is low in dispersity, good in stability, good in uniformity and repeatability and single in molecular weight, so the biological distribution of the nanoparticles corresponding to the polymer in a living body can be conveniently quantified by using a mass spectrum. The preparation method provided by the invention is simple and easy to implement, and product repeatability is good.
Owner:UNIV OF SCI & TECH OF CHINA

Docetaxel micelle nano-drug as well as preparation method and application thereof

The invention discloses a docetaxel (DTX) micelle nano-drug as well as a preparation method and application thereof. The preparation method comprises the following steps: dissolving a polymer in oligomeric ethylene glycol to obtain a polymer mother solution; dissolving dTX in the oligomeric ethylene glycol to obtain a DTX mother solution; mixing the polymer mother solution with the DTX mother solution to obtain a mixed solution of the DTX, the polymer and the oligomeric ethylene glycol; and mixing the mixed solution of the DTX, the polymer and the oligomeric ethylene glycol with a buffer solution to obtain the DTX micelle nano-drug. Compared with a free drug, the nano-drug prepared by loading the chemotherapeutic drug can increase the solubility of the free hydrophobic drug, increase the circulation time of the drug, change the biological distribution of the drug, reduce the enrichment of normal tissues and the like, can quickly release the DTX in cells, has long blood circulation time, high tumor enrichment amount and deep tumor penetrability, and achieves targeted therapy and efficient inhibition on prostatic cancer.
Owner:SUZHOU UNIV

Methods for large tissue labeling, clearing and imaging

The present invention relates to methods for preparing an animal tissue for fluorescence microscopy, to an animal tissue obtainable by said methods, to methods for analyzing said animal tissues, and to methods for the detection of metastases, for analyzing the biodistribution of a biopharmaceutical drug, and for analyzing the biodistribution of nanoparticles. The methods for preparing an animal tissue according to the present invention encompass whole-body labeling, clearing and imaging methods. The methods of the invention are advantageous in that they, for instance, allow the visualization of single cells within mammalian tissues including pig and human brains, tumor metastases at the single cell level and of the distribution of biopharmaceutical drugs (e.g. the distribution of cancer-targeting therapeutic antibodies in whole animals such as intact mice) at single cell level in whole mouse.
Owner:DEEP PICTION GMBH

Bionic drug-loading nano-system combining cell membrane antagonism with nano-enzyme, preparation method and application

PendingCN113599368AMaintain biological activityIncreased ability to evade immune clearancePowder deliveryNanomedicineAntagonismPolymer
The invention discloses a bionic drug-loading nano-system combining cell membrane antagonism with nano-enzyme, a preparation method and application. The system comprises a shell of a cell membrane for loading chemotherapeutic drugs and an inner core of a nano-enzyme modified high-molecular polymer nano-microsphere for loading oxygen-carrying bodies. The bionic nano-carrier maintains the biological activity of cell membrane protein, improves the immune clearance avoiding capacity and biocompatibility of nano-particles, prolongs the blood circulation time of the nano-particles and improves the in-vivo biological distribution of the nano-particles. The drug-loading nano-microsphere is uniform in morphology, has long blood circulation time, can generate a cascade catalytic reaction to generate a large amount of active oxygen, kills leukemia cells, and can effectively inhibit recurrence and metastasis of leukemia; and a new strategy for cooperative treatment of leukemia is provided. The system combines nano-enzyme chemical power treatment with bionic treatment and drug chemotherapy of cell membranes, bone marrow targeted treatment of leukemia can be realized, and the problems of metastasis, recurrence, drug resistance and the like of leukemia are expected to be solved.
Owner:SOUTHEAST UNIV +1

HSP90 targeted conjugates and particles and formulations thereof

Conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to an HSP90 targeting moiety via a linker have been designed. Nanoparticles and microparticles comprising such conjugates can provide improved temporospatial delivery of the active agent and / or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or other diseases.
Owner:TVA (ABC) LLC

Liposome co-loaded with CD73 antibody and adriamycin, and preparation method and application of liposome

The invention provides a liposome co-loaded with CD73 antibody and adriamycin, and a preparation method and application of the liposome. A lipid core coated with the adriamycin is arranged in the liposome co-loaded with the CD73 antibody and the adriamycin, the outside of the lipid core is modified with the CD73 antibody, and the CD73 antibody is coupled to a phospholipid PEG active ester micelle and then is modified on the surface of the lipid core. The lipidosome co-loaded with the CD73 antibody and the adriamycin reduces the drug resistance and the toxic and side effects of the adriamycin in treatment of the triple negative breast cancer, improves in-vivo biological distribution of the adriamycin, improves bioavailability, and turns an immune microenvironment in a triple negative breast cancer tumor, so that the triple negative breast cancer tumor is converted into a thermal tumor, and a relatively good treatment effect for the triple negative breast cancer is realized.
Owner:SHANDONG UNIV

Natural protected area protection vacancy analysis method and system

The invention provides a natural reserve protection vacancy analysis method and system, and relates to the field of ecological protection, and the method comprises the steps: carrying out the unit-area incremental evaluation of a physical environment, a biological environment and an interference factor of a target region according to a natural reserve vector diagram in the target region under a large resolution, obtaining an analysis result of whether a protection vacancy area exists in the target area; before or during the process, acquiring spatial geographical environment data of a target area to construct a basic database; collecting data representing ecological system and natural resource distribution characteristics, data representing biological distribution characteristics and datarepresenting ecological system service characteristics, and constructing an index database; and processing the basic database and the index database to enable the basic database and the index databaseto perform calculation under high resolution so as to obtain a macroscopic evaluation result of the target area. The method can realize identification of the protected vacant area of the natural reserve, is beneficial to guidance of ecological restoration and is beneficial to ecological environment protection.
Owner:国家林业和草原局华东调查规划院

Composite nano-drug carrier as well as preparation method and application thereof

The invention discloses a composite nano-drug carrier as well as a preparation method and application thereof, and particularly relates to a polysialic acid (PSA) modified zein nano-drug carrier and a drug loading system thereof, in particular to a tumor targeted drug delivery system, and preparation methods and application of the polysialic acid (PSA) modified zein nano-drug carrier and the drug loading system of the polysialic acid (PSA) modified zein nano-drug carrier and the tumor targeted drug delivery system. The drug carrier can realize enhanced drug delivery efficiency, active targeting ability and specific biological distribution at tumor sites, thereby inhibiting growth, migration and invasion of tumors. By taking HNK as an example, experiments prove that the PSA-zein-HNK has enhanced tumor accumulation in a mouse model carrying 4T1 breast cancer, so that an ideal anti-tumor effect and favorable biological safety are generated, and moreover, the PSA-zein-HNK remarkably inhibits the breast cancer from being transferred to the lung and the liver. Therefore, the nanoparticles are expected to become an effective tumor targeting drug carrier for drug development and disease treatment.
Owner:QIQIHAR MEDICAL UNIVERSITY

Macrolides compound and siRNA-containing composition and preparation method thereof

ActiveCN104940952AImprove pharmacokinetic profileAltered biodistributionGenetic material ingredientsDigestive systemCholesterolPolyethylene glycol
The invention belongs to the biological medicine field, and more specifically relates to a macrolides compound and siRNA-containing composition and a preparation method thereof. The composition comprises a siRNA sequence and the macrolides compound, and also comprises one or combination of more than two of cation lipid, phosphatide and cholesterol-polyethylene glycol. The macrolides compound and siRNA-containing composition can increase the pharmacokinetics characteristic for siRNA treatment, is capable of changing bio-distribution, intracellular intake, targeting property and transfection efficiency, and reducing adverse reaction.
Owner:厦门成朴希晟股权投资合伙企业(有限合伙)

3-18F-fluorolactic acid analogue as well as preparation method and application thereof

The invention discloses a 3-18F-fluorolactic acid analogue as well as a preparation method and application thereof. The structural formula of the fluoro-18 marked lactic acid analogue is shown by formula A, where R1 is hydrogen or C1-C4 alkyl. The lactic acid analogue can be prepared by the following method: in the presence of amino polyether serving as a phase transfer catalyst and a basic catalyst, the compound shown by formula B and the 18F ions are subjected to nucleophilic addition to obtain an intermediate shown by formula C; in an alkaline condition, hydrolyzing the intermediate shown by the formula C to obtain the 3-18F-fluorolactic acid analogue. Compared with the prior art, the fluoro-18 marked lactic acid analogue provided by the invention has an exact characteristic of uptake by tumor, and also has relatively good bio-distribution feature, the potential of serving as a tumor developer, and the characteristics of easiness in preparation and stable labeling rate. Therefore, the fluoro-18 marked lactic acid analogue can be employed as a tumor lactic acid metabolism PET development molecular probe, and has high sensitivity and good selectivity.
Owner:上海释雅医药科技有限公司

Composition containing quaternary ammonium salt compound and siRNA and preparing method thereof

InactiveCN104997801AImprove pharmacokinetic profileAltered biodistributionAntiviralsAmine active ingredientsCholesterolBio distribution
The invention belongs to the field of biological medicine and particularly relates to a composition containing a quaternary ammonium salt compound and siRNA and a preparing method thereof. The composition contains a siRNA sequence and the quaternary ammonium salt compound or lipid with the function of the quaternary ammonium salt compound and can also contain phopholipid, cholesterol and lipid-polyethylene glycol. The composition containing the quaternary ammonium salt compound and siRNA can improve the pharmacokinetics characteristic of siRNA treatment, change bio-distribution, intracellular intake, targeting and transfection efficiency, and reduce adverse reaction.
Owner:XIAMEN CHENGKUN BIOTECH

Investigation and evaluation system for biological diversity

ActiveCN114399415APrepare reference dataBiodiversity assessments are accurateCharacter and pattern recognitionNatural language data processingEvaluation resultBio distribution
The invention relates to the technical field of ecology and biology, and discloses a biological diversity investigation and evaluation system. The investigation and evaluation system for the biodiversity comprises a region positioning system, an ecological analysis system, a simulation distribution system, a sampling investigation system, an investigation shooting system, a result confirmation system, an investigation and evaluation system and a data output system. According to the method, the biological distribution in the region is simulated, and the sampling region division is performed on the region according to the simulation result, so that the division of the sampling region is more scientific, objective, comprehensive and representative, more accurate reference data is provided for the subsequent evaluation result, and the biological diversity evaluation in the region is more accurate; the evaluation efficiency is greatly improved, and a more efficient, more accurate and less labor investigation mode is provided for evaluation of biodiversity.
Owner:GUANGDONG BYTEST TECH CO LTD
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