33results about How to "Improve brain targeting" patented technology

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.