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33results about How to "Improve brain targeting" patented technology
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Menthol derivative containing fatty acid and preparation containing said derivative
InactiveCN1651397AImprove reaction speedIncrease responsivenessPreparation from carboxylic acid halidesSolventOrganic solvent
A menthol derivative containing fatting acid is prepared through catalytic esterifying reaction between menthol and straight-chain or branch-chain C5-C30 fatty acid. A medicine containing said derivative is also disclosed, which has high cerebral target performance.
Owner:SHENYANG PHARMA UNIVERSITY
Piperazine (piperidine) cyclohexyl derivative and applications of piperazine (piperidine) cyclohexyl derivative in treatment of neuropsychiatric diseases
ActiveCN105367565AGood receptor selectivityImproving the effect of cognitive impairmentOrganic active ingredientsNervous disorderLow affinityAcute toxicity testing
The present invention discloses a piperazine (piperidine) cyclohexyl derivative and applications of the piperazine (piperidine) cyclohexyl derivative in treatment of neuropsychiatric diseases. According to the present invention, the pharmacological experiment results show that the piperazine (piperidine) cyclohexyl derivative provides high affinity with a dopamine D2 receptor, a dopamine D3 receptor, a serotonin 5-HT1A receptor and a serotonin 5-HT2A receptor, provides good D3 / D2 receptor selectivity and good 5-HT1A / 5-HT2A receptor selectivity, and provides low affinity with alpha receptor; the in vivo test results show that the preferred compound has characteristics of good anti-schizophrenia effect, good pharmacokinetic property, low side effect, low acute toxicity and high safety, and has the development value of being adopted as the novel efficient and low-toxic anti-neuropsychiatric disease; and the piperazine (piperidine) cyclohexyl derivative is a compound represented by the structural general formula (I), or a geometric isomer, an optical isomer, a salt, a hydrate or a solvate thereof. The formula (I) is defined in the specification.
Owner:SHANGHAI INST OF PHARMA IND +1
Anti-glioma drugs based on Venenum Bufonis extract and preparation method thereof
InactiveCN105477020AIncrease apoptosis rateGrowth inhibitionAmphibian material medical ingredientsPowder deliveryGlycerolMedium-chain triglyceride
The invention relates to antitumor drugs and discloses anti-glioma drugs based on Venenum Bufonis extract and a preparation method thereof, the drugs being a bufotalin submicron emulsion and a bufotalin nanoparticle preparation, wherein the bufotalin submicron emulsion comprises Venenum Bufonis extract, medium chain triglyceride, a lecithin, poloxamer 188, glycerol, sodium oleate and injection water; the bufotalin nanoparticle preparation comprises Venenum Bufonis extract, glycerol monostearate, medium-chain fatty acid glyceride, oleic acid, a lecithin, poloxamer 188, sodium deoxycholate and injection water. Both the two preparations can combine with endothelial cells in cerebral blood capillaries, enabling the drugs to be transmitted into the brain through membranes or by means of adsorption, medication, endocytosis and transferring, cerebral targeting of the drugs is improved, and further increase of bufotalin in the brain is facilitated, and glioma resistance is achieved by inducing apoptosis and excessive autophagy of cells.
Owner:赵婷
Dual brain-targeted prodrug with organic-amine-modified vitamin C being carrier
ActiveCN105641711AImprove distributionImprove brain targetingOrganic active ingredientsOrganic chemistryPharmacyVitamin C
The invention discloses a dual brain-targeted prodrug with an organic-amine-modified vitamin C being a carrier. The dual brain-targeted prodrug is a structure or pharmacy acceptable salt or water compound shown in the general formula (I), wherein X represents -(CH2)n-, -C(O)-(CH2)n-C(O)-or-(CH2)m-O-, -(CH2)m-NH-, -(CH2)m-C(O)-, -c(o)-(ch2)M-, -C(O)-(CH2)m0NH-, n represents 0-6, m represents 1-4, and Drug represents medicine acting on the central nervous system. The series of prodrug can improve brain-targeted performance of the medicine and increase the concentration of the central nervous system, in this way, the treatment effect of the medicine is improved, meanwhile, medicine distributed on peripheral organs is reduced, and toxic and side effects of the medicine are reduced.
Owner:SICHUAN UNIV
Borneol fatly acid ester derivative and preparation containing said derivative
InactiveCN1651395AImprove brain targetingPromote absorptionAntibacterial agentsOrganic active ingredientsBranched chain fatty acidsDisease
A derivative of the borneol ester of fatty acid, which is a target auxiliary of the medicine for treating cerebral diseases, is prepared through esterifying reaction between borneol or isoborneol and the straight-chain or branch-chani C5-C30 fatty acid.
Owner:SHENYANG PHARMA UNIVERSITY
Invisible brain-targeted triptolide nano-liposome and preparation method
ActiveCN107899022ASimple detection operationHigh precisionOrganic active ingredientsNervous disorderCouplingPolyethylene glycol
The invention belongs to the technical field of medicines and discloses invisible brain-targeted triptolide nano-liposome and a preparation method. The preparation method comprises the following steps: using nano triptolide lipidosome as a medicine carrier, and performing invisibility modification on the medicine carrier by using polyethylene glycol PEG (Polyethylene Glycol), so as to obtain invisible triptolide nano-liposome; connecting brain-targeted ligand Lf with the surface of the PET-TP nano-liposome by adopting a covalent coupling method, thereby obtaining the invisible brain-targeted triptolide nano-liposome. Through optimization of preparation processes, the invisible brain-targeted triptolide nano-liposome which is uniform in particle size distribution, relatively high in packaging rate and good in stability is successfully prepared, and related results are not available in document reports; the average particle size of the prepared Lf-PEG-TP nano-liposome is 105.98+ / -2.65nm,the packaging rate of the nano-liposome is 55.96+ / -2.13%, and the Lf coupling percentage of the nano-liposome is 79.26+ / -3.57%.
Owner:深圳市锦泰医药科技合伙企业有限合伙 +1
Brain-targeted water soluble drug carrier as well as preparation method and application thereof
InactiveCN104208709AImprove brain targetingSmall toxicityNervous disorderPharmaceutical non-active ingredientsSide effectNano brain
The invention provides a brain-targeted water soluble drug carrier as well as a preparation method and application thereof. An LDL (low density lipoprotein) receptor of an endothelial cell of blood-brain barrier is selected as a transmission water soluble drug to treat a target spot of central nervous system diseases, and chitosan with very good biocompatibility is taken as a drug carrier material to research a low-toxicity efficient water soluble drug nano brain-targeted preparation. The brain-targeted water soluble drug carrier can be used for strengthening brain targeting of water soluble drugs, strengthening the curative effect, lowering the toxic and side effect, and improving the bioavailability.
Owner:吴正治 +1
Dual-brain-targeting prodrug commonly modified by glucose and vitamin C
InactiveCN107899016AEasily damagedImprove brain targetingEsterified saccharide compoundsNervous disorderVitamin CSide effect
The invention discloses a dual-brain-targeting prodrug commonly modified by glucose and vitamin C; the dual-brain-targeting prodrug is the structure shown in a general formula (I) or pharmaceuticallyacceptable salts and aquo-complex; the formula is as shown in the specification. In which, X represents -(CH2)a , C(O) (CH2)a C(O) or (CH2)b O , (CH2)b NH , C(O) (CH2)b O , C(O) (CH2)b NH ; a represents 0-6, b represents 1-4; Y represents (CH2)n , C(O) (CH2)n C(O) or C(O) (CH2)m , (CH2)m C(O) ; n represents 0-6, m represents 1-4; Drug represents a drug applied to a central nerve system.A series of prodrug can improve the brain targeting property and pivot concentration, so as to enhance the drug effect; meanwhile, the drug distribution at a peripheral organ is reduced, and the toxic and side effects of the drug are reduced.
Owner:SICHUAN UNIV
Nasal administration type nano-sized brain-targeting drug for galanthamine and preparation method of nasal administration type nano-sized brain-targeting drug for galanthamine
ActiveCN105617396AWith protectionGood regeneration performanceNervous disorderPharmaceutical non-active ingredientsBrain sectionSolvent
The invention provides a nasal administration type nano-sized brain-targeting drug for galanthamine and a preparation method of the nasal administration type nano-sized brain-targeting drug for the galanthamine. The preparation method includes subjecting chitosan to oxidation by periodate so as to obtain different molecular weights of CS-CHO with chitosan chains containing o-dialdehyde functional groups, further, taking a DMSO (dimethyl sulfoxide) as a solvent and chlorous acid as an oxidizing agent to oxidize the o-dialdehyde functional groups into CS-COOH, and subjecting the CS-COOH and the galanthamine to esterification reaction so as to obtain the nano-sized brain-targeting drug. The nasal administration type nano-sized brain-targeting drug for the galanthamine has the advantages that the drug can envelop connecting tissues surrounding olfactory tracts or axons of olfactory receptor neurons through olfactory region mucous membranes to reach cerebral spinal fluid or the brain and can bypass blood-brain barriers to enter a central nervous system to be absorbed into the brain directly, and accordingly the drug is quick in action, needs no parenteral administration, avoids hepatic first-pass effect and is convenient to use by applying a dosing device.
Owner:深圳市锦泰医药科技合伙企业有限合伙 +1
Protein-mediated brain-targeting gene delivery system and application thereof
InactiveCN102614525AHigh transfection efficiencyImprove expression levelNervous disorderGenetic material ingredientsGene deliveryHydrophilic polymers
The invention, belonging to the technical field of biology, relates to a protein-mediated brain-targeting gene delivery system and an application thereof, particularly an application in medicines for treating Parkinson disease. The gene delivery system is formed by modifying lactoferrin on a cationic high-molecular material through hydrophilic polymers to compound plasmid DNA by electrostatic action. According to the invention, the transfection efficiency and expression efficiency of genes on brain capillary vessel endothelial cells can be effectively improved, especially the brain targeting and the expression of the genes in the brain are significantly raised after administration through noninvasive intravenous injection; compared with a targeting head-constructed gene delivery system used in the prior art, the brain targeting effect is significantly improved. The results of the experiment of animal model prove that the gene delivery system can significantly improve the behavior disorder of animal pattern with Parkinson, obviously increase the number of dopaminergic neurons in corpus striatum and substantia nigra, and simultaneously raise the level of corpus striatum monoamine neurotransmitters.
Owner:FUDAN UNIV
Preparation method of novel nasal administration brain-targeted nano drug loading system
ActiveCN105617395AGood membrane permeabilityRegulate Response RatioNervous disorderPharmaceutical non-active ingredientsBrain sectionSensory neuron
The invention provides a preparation method of a novel nasal administration brain-targeted nano drug loading system. The preparation method includes: utilizing periodate to oxidize chitosan to obtain hydroformylated chitosan different in molecular weight and containing o-dialdehyde functional group on a chitosan chain; using DMSO (dimethylsulfoxide) as a solvent and chlorous acid as oxidant to oxidize the o-dialdehyde functional group into o-dicarboxylated chitosan, and enabling the carboxylated chitosan and hydrophilic small-molecule drug R-(OH)n to be in esterification to obtain targeting drug. The targeting drug can reach cerebrospinal fluid or brain through olfactory region mucosa along connecting tissue winding around an olfactory tract or axon of olfactory sensory neurons, thereby being capable of bypassing a blood brain barrier to enter a central nervous system to be directly absorbed by the brain. The preparation method has the advantages that the targeting drug is quick in action and needless of injection administration, liver first pass effect is avoided, and a quantifying device is used, so that convenience in use is realized.
Owner:深圳市锦泰医药科技合伙企业有限合伙 +1
Huperzine A solid lipid nano particle and preparation method thereof
ActiveCN101658494BImprove stabilityImprove bioavailabilityPowder deliveryOrganic active ingredientsLipid formationOrganic solvent
The invention relates to the field of pharmaceutical preparations, which discloses a huperzine A solid lipid nano particle and a preparation method thereof. The huperzine A solid lipid nano particle is prepared from the following components in weight percent: 0.05-1% of huperzine A, 3-10% of lipid material, 2-10% of emulsifying agent and the balance water. The preparation method adopts a high-pressure even emulsification method to coat the huperzine A into a solid lipid nano particle so as to prepare the huperzine A solid lipid nano particle. The particle diameter of the huperzine A solid lipid nano particle prepared by the invention is 10-100nm, the medicine envelopment rate and the medicine-carrying quantity are high, and the stability is good; simultaneously, the use of an addition agent and an organic solvent which are harmful to a human body is avoided; and the bioavailability is enhanced, the brain targeting property is increased, and the dose and the toxic or side effect are small.
Owner:GUANGDONG PHARMA UNIV
Chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and preparation method thereof
ActiveCN109730966ANo degradabilityCumulative toxicity NonePowder deliveryNervous disorderNasal cavityFreeze-drying
The invention discloses a chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and a preparation method thereof. The system includes hydrophobic micro-molecule drugs, polyethylene glycol derivatives and chitosan oligosaccharide which have a neuroprotective effect. The invention also provides a preparation method of the nasalcavity nano preparation brain-targeted delivery system. The preparation method includes the steps of 1, preparing nano-particle freeze-dried powder; 2, stirring the freeze-dried powder and chitosan oligosaccharide in isotonic normal saline before use to form a nasal cavity preparation with good membrane permeability. The system is simple in preparation method and can improve the hydrophobicity ofthe micro-molecule drugs, reduce the toxicity and enhance the ne neuroprotective effect. The system is free of carriers, biodegradation problems and accumulation of toxin. The drug carrying rate reaches 25 percent or above, a permeable membrane has good absorption performance after being modified by chitosan oligosaccharide, and the drugs are delivered into the brain with high targeting property.The application modes of the dosage form include nasal dripping, spray and the like, the operation is simple, convenience is provided for patients who have taken the drugs for a long time, and the system has a good application prospect in the aspect of treating nervous system diseases.
Owner:NASAL PHYTO SZ PHARMA TECH CO LTD
Method for preparing nano-liposome marked by colloidal gold and loaded with PD (pharmacodynamics) medicine
ActiveCN103932986AHigh encapsulation efficiencySmall particle sizeNervous disorderInorganic non-active ingredientsWater bathsSide effect
The invention discloses a method for preparing nano-liposome marked by colloidal gold and loaded with a PD (pharmacodynamics) medicine. The method comprises the following steps: dispersing lecithin and a cholesterol and ethanol solution in a PBS (Phosphate Buffer Solution) containing colloidal gold and levodopa or amantadine PD therapeutic medicine under specific conditions, then adding the PBS solution into a water bath to stir, completely volatilizing the ethanol and then performing appropriate ultrasonic treatment to prepare the nano-liposome. The prepared nano-liposome marked by colloidal gold and loaded with the PD medicine is small in particle diameter and excellent in stability; meanwhile, the nano-liposome is located and marked by the gold, thereby improving the stability of the PD medicine, improving the bioavailability, reducing the usage amount of the medicine and reducing the toxicity. The preparation method is simple to operate; the reaction is easy to control; the product, namely the nano-liposome can be used for researching the medicine administration effect of the nano-levodopa or amantadine liposome, improving the toxic and side effects of the levodopa or the amantadine and enhancing the brain targetability. The product also can be used as a probe which is used for researching a cerebral metabolism pathway of the nano-liposome.
Owner:HEBEI NORMAL UNIV
A stealthy brain-targeted triptolide nanoliposome and its preparation method
ActiveCN107899022BReduce drug distributionImprove brain targetingOrganic active ingredientsNervous disorderDrug carrierPharmaceutical drug
The invention belongs to the technical field of medicine, and discloses a stealthy brain-targeted triptolide nano-liposome and a preparation method thereof. The nano-triptolide liposome is used as a drug carrier; polyethylene glycol PEG is used for stealth Stealthized triptolide nano-liposomes were prepared by chemical modification; the brain-targeting ligand Lf was connected to the surface of PEG-TP nano-liposomes by covalent coupling method to prepare stealthy brain-targeted triptolide nano-liposomes. Liposomes. Through the optimization of the preparation process, the present invention successfully prepared stealth brain-targeted triptolide nanoliposomes with uniform particle size distribution, high encapsulation efficiency and good stability, and the relevant results have not been reported in the literature; the prepared The average particle diameter of Lf‑PEG‑TP nano liposomes is 105.98±2.65nm, the encapsulation efficiency is 55.96±2.13%, and the Lf even percentage is 79.26±3.57%.
Owner:深圳市锦泰医药科技合伙企业有限合伙 +1
Berberine long-circulating nano-liposome with brain targeting function and preparation method of berberine long-circulating nano-liposome
InactiveCN113694026AImprove brain targetingImproved brain targetingOrganic active ingredientsNervous disorderAmmonium sulfateBiophysics
The invention belongs to the technical field of medicine and pharmacology, and discloses a preparation method of berberine long-circulating nano-liposome BR-Lf with a brain targeting function. The preparation method comprises the following steps: preparing a PL-COOH liposome by using ammonium sulfate as a hydration medium and adopting an improved ethanol injection method; taking 2 parts by mass of PL-COOH, adding 1 part by mass of an EDC solution and 1 part by mass of an NHS solution in an ice-water bath, performing magnetic stirring and activating for 0.5 h, restoring to room temperature, adding 6 parts by mass of Lf, performing full dissolving, adding 1.4 parts by mass of TEA, performing reacting for 4 h, and terminating the reaction in the ice-water bath to obtain lactoferrin modified PEGylated blank liposome PL-Lf; and taking PL-Lf suspension, removing an external water phase through an anion-cation fiber column, adding a berberine hydrochloride BR solution according to a drug-lipid ratio of 1: 15, performing incubating at a constant temperature of 40 DEG C for at least 15 minutes, and terminating drug loading in the ice-water bath to obtain BR-Lf. By optimizing the preparation process, the BR-Lf which is uniform in particle size distribution, relatively high in encapsulation efficiency and good in stability is successfully prepared.
Owner:SHENZHEN ELDERLY MEDICAL RES INST +1
Menthol derivative containing fatty acid and preparation containing said derivative
InactiveCN1651397BImprove reaction speedIncrease responsivenessPreparation from carboxylic acid halidesMentholBranched chain fatty acids
A menthol derivative containing fatting acid is prepared through catalytic esterifying reaction between menthol and straight-chain or branch-chain C5-C30 fatty acid. A medicine containing said derivative is also disclosed, which has high cerebral target performance.
Owner:SHENYANG PHARMA UNIVERSITY
A brain-targeted gene delivery system based on polymethacrylate
ActiveCN103623424BImprove brain targetingLow toxicityNervous disorderGenetic material ingredientsGene deliveryCytotoxicity
The invention belongs to the field of biotechnology, and relates to a polymethacrylate-based brain-targeted gene delivery system and a preparation method thereof. The carrier of the gene delivery system is composed of three parts covalently linked with the cationic segment polymethacrylate, the electrically neutral segment and the brain-targeting functional group TGN. The carrier then self-assembles with the anionic plasmid DNA through electrostatic interaction to form a nanogel bundle. The invention can deliver the gene drug to pass through the blood-brain barrier and enter the brain to play a role. The invention significantly improves the brain targeting ability of the gene delivery system and the expression of genes in the brain after the administration test by non-invasive intravenous injection; its particle size, surface charge and modification degree of targeting functional groups are all controllable , which facilitates the optimization of gene delivery systems. The gene delivery system constructed by the present invention has the advantages of low cytotoxicity and high brain targeting efficiency.
Owner:FUDAN UNIV
Citicoline sodium brain-targeting thermosensitive gel and preparation method thereof
ActiveCN102579320BFast absorptionFacilitated releaseOrganic active ingredientsNervous disorderNasal cavityCiticoline sodium
The invention discloses citicoline sodium brain-targeting thermosensitive gel. The citicoline sodium brain-targeting thermosensitive gel is a preparation which can be absorbed fast and has high bioavailability. The citicoline sodium brain-targeting thermosensitive gel utilizes water as a solvent and comprises solute components of 10 to 400mg / ml of citicoline sodium, 0.1 to 3.0mg / ml of Tween-80, 0.5 to 5.0mg / ml of phosphatide E80, 0.5 to 3.0mg / ml of poloxamer P188, and 5.0 to 10.0mg / ml of poloxamer P407. The invention also discloses a preparation method of the citicoline sodium brain-targetingthermosensitive gel. The citicoline sodium brain-targeting thermosensitive gel has a high drug loading amount, is uniform and stable, has good fluidity, is in a state of gel at a temperature of 33 DEG C, has good biological adhesion strength, is suitable for being applied through a nasal cavity, has a good appearance, and does not produce floating oil and layering.
Owner:四川梓橦宫药业股份有限公司
Citicoline sodium brain-targeting thermosensitive gel and preparation method thereof
ActiveCN102579320AStrong brain targetingSimple central drug deliveryOrganic active ingredientsNervous disorderNasal cavityCiticoline sodium
The invention discloses citicoline sodium brain-targeting thermosensitive gel. The citicoline sodium brain-targeting thermosensitive gel is a preparation which can be absorbed fast and has high bioavailability. The citicoline sodium brain-targeting thermosensitive gel utilizes water as a solvent and comprises solute components of 10 to 400mg / ml of citicoline sodium, 0.1 to 3.0mg / ml of Tween-80, 0.5 to 5.0mg / ml of phosphatide E80, 0.5 to 3.0mg / ml of poloxamer P188, and 5.0 to 10.0mg / ml of poloxamer P407. The invention also discloses a preparation method of the citicoline sodium brain-targetingthermosensitive gel. The citicoline sodium brain-targeting thermosensitive gel has a high drug loading amount, is uniform and stable, has good fluidity, is in a state of gel at a temperature of 33 DEG C, has good biological adhesion strength, is suitable for being applied through a nasal cavity, has a good appearance, and does not produce floating oil and layering.
Owner:四川梓橦宫药业股份有限公司
A kind of chitosan lipoprotein nasal administration nanocomposite and its preparation method and application
ActiveCN113116854BSmooth and round appearanceGood dispersionPowder deliveryMaterial nanotechnologyA lipoproteinPharmaceutical formulation
The invention belongs to the field of pharmaceutical preparations, and discloses a chitosan lipoprotein intranasal administration nanocomposite, comprising lipoprotein nanoparticles, chitosan or / and chitosan derivatives having the effect of promoting absorption of nasal mucosa. The invention also discloses a preparation method of chitosan lipoprotein intranasal administration nanocomposite, comprising: self-assembling chitosan or / and chitosan derivatives and lipoprotein nanoparticles through dynamic force to form a good membrane permeability nasal preparations. The preparation condition of the chitosan lipoprotein intranasal administration nanocomposite is mild, the process is simple, and the industrialized production is easy. The system is safe, non-toxic, and has good biodegradability, which can improve the absorption of lipoprotein drugs in the nasal mucosa and ensure high-efficiency brain targeting. The dosage form is administered by nasal drops, sprays, etc., and is easy to operate, convenient for patients who take the medicine for a long time, and has a good clinical application prospect in the treatment of central nervous system diseases.
Owner:CHINA PHARM UNIV
A preparation method of brain-targeted nano-drug loading system for nasal administration
ActiveCN105617395BGood membrane permeabilityRegulate Response RatioNervous disorderPharmaceutical non-active ingredientsCarboxyl radicalSensory neuron
The invention provides a preparation method of a novel nasal administration brain-targeted nano drug loading system. The preparation method includes: utilizing periodate to oxidize chitosan to obtain hydroformylated chitosan different in molecular weight and containing o-dialdehyde functional group on a chitosan chain; using DMSO (dimethylsulfoxide) as a solvent and chlorous acid as oxidant to oxidize the o-dialdehyde functional group into o-dicarboxylated chitosan, and enabling the carboxylated chitosan and hydrophilic small-molecule drug R-(OH)n to be in esterification to obtain targeting drug. The targeting drug can reach cerebrospinal fluid or brain through olfactory region mucosa along connecting tissue winding around an olfactory tract or axon of olfactory sensory neurons, thereby being capable of bypassing a blood brain barrier to enter a central nervous system to be directly absorbed by the brain. The preparation method has the advantages that the targeting drug is quick in action and needless of injection administration, liver first pass effect is avoided, and a quantifying device is used, so that convenience in use is realized.
Owner:深圳市锦泰医药科技合伙企业有限合伙 +1
Preparation method of triptolide and berberine co-loaded nano-liposome with brain targeting function
PendingCN114272252AProlong circulation time in the bodyExtend cycle timeOrganic active ingredientsNervous disorderBerberineEthanol Injection
The embodiment of the invention discloses a preparation method of a triptolide and berberine co-loaded invisible nano-liposome. The preparation method comprises the following steps: preparing a PEGylated blank liposome PL and a carboxyl-end blank liposome PL-COOH by taking citric acid as a hydration medium and adopting an improved ethanol injection method; adjusting the pH value of the carboxyl-terminal blank liposome PL-COOH to 7 by using hydrochloric acid, taking the gradient PEGylated blank liposome PL, and adding the gradient PEGylated blank liposome PL into a berberine hydrochloride BR solution according to a drug-lipid ratio of 1: (15-25) to obtain BR-PL and BR-PL-COOH liposome; the preparation method comprises the following steps: adding a triptolide TP solution into BR-PL and BR-PL-COOH lipidosome, incubating for at least 60 minutes at a constant temperature of 40-60 DEG C, and terminating drug loading in an ice-water bath, so as to prepare the triptolide and berberine co-loaded invisible nano-lipidosome TP-BR-PL and TP-BR-PL-COOH.
Owner:THE SECOND PEOPLES HOSPITAL OF SHENZHEN +1
A method for preparing colloidal gold-labeled nanoliposomes loaded with PD drugs
ActiveCN103932986BImprove stabilityReduce dosageNervous disorderInorganic non-active ingredientsWater bathsSide effect
Owner:HEBEI NORMAL UNIV
A nano-brain-targeted drug for intranasal administration of ricolamin and its preparation method
ActiveCN105582545BGood membrane permeabilityRegulate Response RatioNervous disorderPharmaceutical non-active ingredientsCarboxyl radicalAldehyde formation
The invention provides a lycoramine intranasal medicated nano-brain-targeting medicine and a preparation method thereof. The preparation method comprises the following steps: firstly, oxidizing chitosan by utilizing periodate to obtain hydroformylated chitosan which has a different molecular weight and has a o-dialdehyde functional group on the chitosan chain; and further oxidizing the o-dialdehyde functional group by using DMSO as a solvent and chlorous acid as an oxidant to prepare o-dicarboxyl chitosan; performing an esterification reaction between carboxylated chitosan and lycoramine to prepare the targeting medicine. The medicine can reach cerebrospinal fluid or brain through olfactory mucosa along the conjunctive tissue enveloping the periphery of the olfactory tract or the axon of olfactory receptor neurons, can bypass the blood-brain barrier to enter the central nervous system, and is directly absorbed by the brain. The medicine has the characteristics of quick response, no injection administration and liver first-pass effect prevention, and is convenient to use due to application of a quantitative device.
Owner:深圳市锦泰医药科技合伙企业有限合伙 +1
A self-carrying carrier-free nasal cavity nano-preparation brain-targeted delivery system modified with chitosan oligosaccharides and its preparation method
ActiveCN109730966BReduce lossImprove compliancePowder deliveryNervous disorderPolythylene glycolOligosaccharide
The invention discloses a self-carrying carrier-free nasal cavity nano-preparation brain-targeted delivery system modified by chitosan oligosaccharides and a preparation method thereof. Including hydrophobic small molecule drugs with neuroprotective effects, polyethylene glycol derivatives, and chitosan oligosaccharides. The present invention also provides a preparation method for the brain-targeted delivery system of the nasal cavity nano-preparation. The first step is to prepare the freeze-dried powder of nanoparticles, and the second step is to stir the freeze-dried powder and chitosan oligosaccharide in isotonic saline before use to form a nasal cavity preparation with good membrane permeability. The preparation method of the system of the present invention is simple, can improve the hydrophobicity of small molecule drugs, reduce toxicity, and enhance neuroprotective effect; there is no carrier, no biodegradation problem and accumulation toxicity, the drug loading rate is as high as 25%, and the membrane is permeable after being modified by chitosan oligosaccharides Absorption is good, and the drug is delivered into the brain with high targeting. The administration method of the dosage form is nasal drop, spray, etc., and the operation is simple, which is convenient for patients who take medicine for a long time, and has a good application prospect in the treatment of nervous system diseases.
Owner:NASAL PHYTO SZ PHARMA TECH CO LTD
A kind of brain targeting eslicarbazepine ester prodrug and application thereof
ActiveCN106588773BImprove the ability to cross the blood-brain barrier (BBB)Improve Brain UptakeNervous disorderOrganic chemistryDiseaseAdjuvant
The invention relates to an eslicarbazepine ester prodrug and an application thereof, wherein the prodrug is a compound represented by the formula (I) or optical isomers or physiologically acceptable salts of the compound represented by the formula (I), wherein R represents a lipophilic substituent. The compound represented by the formula (I) is the eslicarbazepine ester prodrug containing the lipophilic substituent, is converted into eslicarbazepine through metabolism in vivo to play pharmacological effects, and can be applied in preparation of drugs for treatment, prevention or adjuvant treatment of central nervous system diseases, such as epilepsy and the like.
Owner:北京现代药物代谢研究院
Brain targeting gene delivery system based on polymethacrylate
ActiveCN103623424AProlong blood circulation timeReduce toxicity in the bodyNervous disorderGenetic material ingredientsGene deliveryCytotoxicity
Belonging to the field of biological technology, the invention and relates to a brain targeting gene delivery system based on polymethacrylate and a preparation method thereof. A vector of the gene delivery system comprises a cationic chain segment polymethacrylate, an electrically neutral segment and a brain targeting functional base TGN in covalent connection, and the vector further conducts self-assembling with an anionic plasmid DNA into nano-micelles through electrostatic interaction. The system provided by the invention can transfer gene drugs across the blood-brain barrier into the brain to play a role. Through noninvasive intravenous injection administration test, the system significantly improves the brain targeting performance of the gene delivery system and expression of the gene in the brain; the particle size, surface charge and modification degree of targeting functional groups are controllable, so as to facilitate optimization of the gene delivery system. The gene delivery system constructed by the invention has the advantages of low cytotoxicity and high brain targeting efficiency.
Owner:FUDAN UNIV
Borneol fatly acid ester derivative and preparation containing said derivative
InactiveCN1651395BImprove reaction speedIncrease responsivenessAntibacterial agentsPowder deliveryBranched chain fatty acidsDisease
A derivative of the borneol ester of fatty acid, which is a target auxiliary of the medicine for treating cerebral diseases, is prepared through esterifying reaction between borneol or isoborneol and the straight-chain or branch-chani C5-C30 fatty acid.
Owner:SHENYANG PHARMA UNIVERSITY
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