93 results about "Amphiphilic chitosan" patented technology

The present invention relates to one kind of amphiphilic chitosan quaternary ammonium salt with long alkane radical and its preparation process. The amphiphilic chitosan quaternary ammonium salt with long alkane radical is prepared with water soluble chitosan derivative as modified target and through epoxy long chain alkyl quaternary ammonium salination, and has high solubility. Compared with available technology, the present invention has the features of simple preparation process suitable for industrial production, capacity of using the product as gene medicine carrier, emulsifier and antiseptic, and wide application of the product in medicine, daily chemical, etc.

The invention relates to a hyaluronic acid-modified amphipathic chitosan derivative carrier with tumor microenvironment specificity drug release effect. The hyaluronic acid-modified amphipathic chitosan derivative carrier is characterized in that firstly, a hydrophilic group is introduced into a chitosan skeleton; then, a hydrophobic group is introduced into a specifically degradable link arm containing disulfide bonds, so as to realize the amphipathic function; the amphipathic derivative is assembled into nanomicelle by self in a waterborne medium, and is further modified by a charge adsorbing principle to target the molecular hyaluronic acid; the nanomicelle can effectively load an anti-tumor drug, and the hyaluronic acid is targeted to the tumor microstructure and then is degraded by hyaluronic acid enzyme in focus cells, so that the drug can be quickly released from the nanomicelle to act on the focal part, thereby obviously improving the concentration, therapy effect and biological utilization degree of free drug on the focal part. The hyaluronic acid-modified amphipathic chitosan derivative carrier has the advantages that the carrier which carries pharmaceutical activity or pharmacological activity molecules can be applied to internal injection of blood vessels or muscles or oral administration, so as to obviously improve the anti-tumor activity of drug; the preparation method is simple, the technology is matured, and the preparation method is suitable for large-scale production.

The invention relates to a sulfhydrylated amphipathic chitosan derivative carrier with biological adhesiveness. The derivatives are structured by respectively introducing hydrophilic groups, hydrophobic groups and groups containing sulfydryl. The derivative in an aqueous medium can be self-assembled to nano-micelle so as to load pharmaceutically active or pharmacologically active molecules. After the carrier reaches the mucosa of a living body, the sulfydryl groups can be bonded with surface protein of the mucosa through covalent bonds: disulfide bonds, so that the detaining and acting time of micelle on the surface of the mucosa is prolonged. In addition, the chitosan derivative further has the function of mutual effect in compact connection with cells and opening compact connection with cells of the mucosa. The auxiliary material can be used as the carrier of the pharmaceutically active or pharmacologically active molecules to be used for administration via oral administration, ocular administration, nasal mucosa administration and the like, so that medicine absorption is remarkably improved, and the bioavailability is improved. The carrier provided by the invention is simple in preparation method and manure in process, so that the carrier is suitable for large-scale continuous production.

Production of amphiphilic chitose derivative and its usage are disclosed. The process is carried out by taking chitose as raw material, alkalizing, reacting with 4-methyl bromoethyl acid in 2-propanol medium to obtain 6-0-carboxy-propyl-chitose, purifying, and reacting with long-chain fatty acyl chloride to obtain N-acyl-6-0-carboxy-propyl-chitose. In chemical formula, R=-(CH) n, n=8, 10, 12, 14, 16 and 18. It has excellent biological compatibility and degradation, good tissue adhesion and mechanical strength. It can improve wound heal and have styptic and adhesion-preventing functions.

This invention discloses a method for preparing amphiphilic chitosan derivative and its pharmaceutical application. The method comprises: connecting acylchlorinated long-chain fatty acid and chitosan by esterification, connecting end-activated poly (benzyl malate) and O-long-chain alkyl chitosan via amido bond, and performing catalytic hydrogenation to remove protective groups and obtain amphiphilic chitosan derivative. The amphiphilic chitosan derivative can form nanoparticles of 100-300 nm in aqueous solution, and has such advantages as high biodegradability, high biocompatibility and easy modification.

The invention provides a method for preparing immobilized lipase by utilizing an amphipathy chitosan microsphere carrier, and relates to a method for preparing immobilized lipase. The method comprises the following steps: taking micron-order chitosan microsphere resin prepared by an inverse suspension crosslinking method as an immobilization carrier matrix, performing C2-bit benzene formolatiom on the chitosan microsphere matrix, leading in hydrophobic interaction groups, then using epoxy chloropropane to activate C6-bit hydroxyl, and coupling tetraethylenepentamine to prepare chitosan microspheres with hydrophobic phenyl and hydrophilic polyamine molecules, and taking the chitosan microspheres as the covalent immobilization carrier of lipase after coupling glutaraldehyde. According to the invention, the carrier is adopted to immobilize the antarctic candida lipase B, and the hydrophobic groups and hydrophilic arm molecules are led in, so that the immobilization efficiency of chitosan microspheres to the lipase is improved. When the quality of added lipase of the dry carrier per gram is 40 mg, and the antarctic candida lipase is immobilized for 3 h at room temperature under the condition that the pH is 7.5, the obtained immobilized lipase has the activity recovery rate of 197%, and has the activity of 481.6 U/g.

The invention discloses the synthesis of a new-type chitosan-based hybrid macromolecule and a method for producing or using the macromolecule. This macromolecule comprises an amphiphatic chitosan and a silicon-based coupling agent that is anchored by a chemical bonding. The method for producing the hybrid macromolecule can be easily operated under ambient environment. The produced macromolecule can be self-assembled in an aqueous environment to form a nanocarrier, and has the ability to efficiently encapsulate drugs for a subsequent sustained release purpose. This self-assembled hybrid nanocarrier demonstrated features of excellent biocompatibility, drug loading ability and cellular uptake efficiency.

The invention relates to a polyethyleneimine (PEI) derivative taking an amphipathic chitosan as a cross linker. The molar ratio of the amphipathic chitosan to PEI in the derivative is 1:(1-20), the molecular weight range of the PEI in the raw materials for the preparation of the derivative is 600-70,000, and the molecular weight range of the chitosan in the raw materials for the preparation of the derivative is 1,000-50,000. The invention further provides a preparation method and application of the derivative. The PEI derivative has the advantages that: the PEI derivative is connected with low-molecular-weight PEI through a chemical cross-linking method by using the advantages of the chitosan, and the cytotoxicity arising from high-molecular-weight PEI is greatly lowered under the premise that a certain transfection efficiency is ensured; and particles can be prevented from aggregating in a blood circulation fluid environment due to the introduction of a hydrophilic surface by the chitosan, the stability is improved, the size of a complex formed by deoxyribonucleic acid (DNA) and the PEI derivative connected with the low-molecular-weight PEI can reach nanoscale, and thus, the PEI derivative is suitable for the in-vivo transmission of gene drug.

The invention discloses PH-sensitive chitosan drug-carrying micelle with targeting and fluorescent characteristics and a preparation method thereof; the multifunctional chitosan drug-carrying micelle with targeting property, PH sensitivity, invisibility and fluorescent tracing combined in a whole is constructed by using PH-sensitive amphiphilic chitosan as drug-carrying micelle and polyethylene glycol as a link arm, and grafting folic acid and fluorescent dye thiazole orange to two ends of the micelle; the chitosan drug-carrying micelle of the invention has good fluorescent properties, and has good drug-carrying property for anticancer drug 5-fluorouracil, with drug-carrying efficiency up to 42.76%; under physiological environmental PH (PH=7.4), accumulative drug release within 8 h is only 2%, accumulative drug release within 26 h is less than 8%, and toxic and side effects of the chitosan drug-carrying micelle for normal tissue cells during transport of the anticancer drug 5-fluorouracil can be decreased; in addition, under tumor cell lysosome PH value (PH=4.5), good PH-sensitive drug release property is exhibited, and 5-fluorouracil release within 4 h is up to 95%.

The present invention discloses one kind of glycopeptides conjugate microsphere or microcapsule and its preparation process. The glycopeptides conjugate microsphere or microcapsule has polysaccharide to form the glycosyl part of the glycopeptides conjugate and polypeptide to form the peptide chain part of the glycopeptides conjugate, and the polysaccharide and the polypeptide are connected in covalent bond form. The preparation process includes the first preparation of water soluble chitosan, and the subsequent initiating the ring-opening polymerization of several kinds of amino acid and carboxylic acid inner anhybride monomers by means of the nucleophilicity of the amino group in chitosan to form polysaccharide with chitosan as main chain and peptide chain segment grafted to the side chain and the glycopeptides conjugate with polysaccharide and polypeptide connected via covalent bond. Microsphere or microcapsule may be formed with the amphiphilic chitosan for medicinal use.

The invention relates to a three-function peptide-modified gene carrier as well as a preparation method and application thereof, particularly provides a polypeptide with the functions of tumour targeting, membrane penetrating boosting and core positioning, a gene carrier formed by coupling the polypeptide and amphiphilic chitosan-modified polyethyleneimine, a preparation method of the gene carrier, a compound prepared from the gene carrier and DNA, and the application of the polypeptide with the three functions and the gene carrier in the preparation of a medicine for gene treatment. The three-function peptide-modified gene carrier is high in internal transfection efficiency, low in cytotoxicity, strong in targeting performance, and has wide clinical application prospect.

The invention discloses a preparation method for a chitosan nanometer preservation coating film material. The preparation method comprises the following steps that 1, an amphiphilic chitosan derivative is dissolved in water, stirring is performed, a hydrophilic chitosan derivative is added, stirring is performed, and a nano-particle blending solution is obtained; 2, the hydrophilic chitosan derivative is added in the nano-particle blending solution again to enable the total mass percentage of the hydrophilic chitosan derivative in the solution to be 1-3%, the solution is stirred evenly, and then the chitosan nanometer preservation coating film material is obtained. The preparation method is simple and easy to operate, and the prepared material is compact and uniform in formed film structure, higher in watertightness and antibacterial activity and good in mechanical strength, has the effects of inhibiting air exchanging of fruits and vegetables and reducing the breathing intensity, water evaporation and direct infection of pathogenic bacteria on the fruits and vegetables and the like in fruit and vegetable preservation and can reduce nutrient ingredient loss and improve the preservation effect.

The invention discloses a preparation technology of nano-micelles for conveying anti-tumor medicines through oral administration, namely a preparation method of nano-micelles with mucous layer permeation and P-gp inhibition dual effects. Chitosan, quercetin and 6-phosphogluconic acid are used as raw materials to prepare an amphiphilic chitosan-quercetin succinate-6-phosphogluconic acid copolymer through a condensation and esterification method and a target product is synthesized through a self-assembling technology; the nano-micelles have a good mucous layer permeation capability and also has the P-gp inhibition effect; the oral administration conveying efficiency of the anti-tumor medicines can be effectively improved. The nano-micelles can be used for medical biological materials and medicine carriers and have good research and development application prospects.

The invention relates to the field of pharmaceutic preparations, and discloses a composition of ciclosporin A and amphipathic chitosan derivatives (N,O-carboxymethyl N-cholic acid chitosan) and a preparation method thereof. The composition has the characteristics of high medicament loading rate, high stability and high possibility of being absorbed, and can be used for overcoming the defects such as serious toxic or side effect of the existing ciclosporin A. The preparation method of the composition is simple, and the process is mature, thus the preparation method id applicable to large-scale industrial production.

The invention relates to a method for preparing amphoteric chitosan water reducing agents. The amphoteric chitosan water reducing agents are prepared from chitosan, methoxy polyethylene glycol, acetic anhydride and chlorosulfonic acid through reaction. The method has the innovation point that the natural chitosan is used as raw materials, methoxy polyethylene glycol (MPEG) and hydrophilic sulfo groups are introduced, and the novel amphoteric chitosan water reducing agents are prepared. The prepared amphoteric chitosan water reducing agents have the advantages that the product performance is stable, the cement adaptability is high, the compatibility is good, the cement initial net pulp flowability can reach a value higher than 250mm (W/C=0.29), the concrete water reducing rate can reach about 25 percent, the one-hour collapsbillity can reach 140mm, and in addition, no pollution is caused on the environment. The preparation method has the advantages that the preparation process is noveland unique, the industrial production is convenient, and the like.

This invention relates to a method for synthesizing amphiphilic chitosan. The method comprises: dissolving chitosan, reacting, precipitating, cooling, washing, vacuum-filtering, vacuum-drying, alkalizing, carboxymethylating, desalting, dehydrating and drying to obtain amphiphilic chitosan. The method introduces electrically negative carboxymethyl group and electrically positive quaternary ammonium group onto the molecular chain of chitosan, thus the molecular chain of chitosan contains substituents with two different charge types. After modification, the quaternization degree and the carboxymethylation degree of chitosan are 80% and 70%, respectively. Amphiphilic chitosan has higher apparent viscosity, higher solubility, lower pH value, better pH stability, and wider applications than chitosan.

The invention discloses a drug-loaded mixed micelle comprising taxane medicaments, amphiphilic chitosan derivatives and polyethylene glycol polyester block copolymer. The invention further discloses a preparation method of the drug-loaded mixed micelle. The product does not contain polyoxyethylene castor oil and ethanol, reduces adverse drug reactions, increases security of drug clinic application; by adding the amphiphilic chitosan derivatives and the polyethylene glycol polyester block copolymer, the stability of the preparation is enhanced and drug loading and drug efficacy are increased; and the preparation process is simple and controllable, and the production can be expanded easily.

The invention discloses a preparation method and application of an amphiphilic chitosan derivative protein adsorption-resistant coating. The preparation method comprises carrying out hydrophobic modification on chitosan through cholesteryl chloroformate to obtain an amphiphilic cholesterol-modified chitosan (CHCS), uniformly spin-coating a glass slide with the CHCS solution, carrying out drying at 20-80 DEG C to obtain a CHCS protein adsorption-resistant coating, characterizing physical and chemical properties of a CHCS film and a CHCS monomolecular film, and researching protein adsorption-resistant performances of a series of CHCS coatings. The research result shows that a substrate coated with the CSCH film has good protein adsorption resistance. The preparation method of the protein adsorption-resistant coating has simple processes and utilizes easily controlled conditions. Chitosan has good biocompatibility, blood compatibility, safety, microbial biodegradability, film-forming performances and a wide resource range, can reduce a production cost and is expected to become a novel environmentally friendly anti-fouling material.

The invention discloses an amphiphilic chitosan and its preparation. The amphiphilic chitosan is stearic acid, N-acetyl-L-cysteine grafted chitosan, and has a molecular weight of 10 to 300 kDa. The amphiphilic chitosan of the invention is used as a nano microcapsule embedding wall material, a hydrophobic substance can be embedded to form a water-soluble nano microcapsule solid, or can be used as the embedding wall material of a hydrophilic substance to form water-insoluble nano-capsules. The invention also discloses amphiphilic chitosan-macadamia oil nano microcapsules and a preparation methodand an application thereof. The nano microcapsule is formed by embedding a core material by the wall material, the core material is macadamia oil, and the wall material is the amphiphilic chitosan provided by the invention. The nano-microcapsules provided by the invention have the advantages of high embedding rate, good dispersibility and uniformity, and the macadamia oil has reduced volatility through embedding of the amphiphilic chitosan, and the stability and bioavailability are significantly improved.

The invention discloses amphipathic chitosan with a chemical crosslinking characteristic and a preparation method thereof. The method comprises the following steps of: reacting chitosan with long-chain aliphatic aldehyde to obtain N-long-chain alkyl chitosan; reacting the N-long-chain alkyl chitosan with phthalic anhydride; reacting an obtained product with iodo-polyethylene glycol monomethyl ether; and performing a deprotection reaction on an amino group by using hydrazine hydrate to obtain N-long-chain alkyl-O-polyglycol chitosan. In a preparation process, the method effectively protects the amino group in a chitosan molecule, avoids introducing a polyglycol group on the amino group, and remains part amino group in the amphipathic chitosan by removing the amino group protection; the product can serve as a precursor for preparing amphipathic chitosan hollow microcapsules; and polyethylene glycol with high biocompatibility, low toxicity and easy degradation is introduced on a hydroxyl group of the chitosan to serve as a hydrophilic group, so that the research and application values of the derivative on a medicament carrier are improved.

The invention relates to a brain tumor targeted drug delivery system and a preparation method thereof. The brain tumor targeted drug delivery system comprises a mediated molecule, a basic carrier and a drug, wherein the mediated molecule refers to glucose; the basic carrier refers to an amphipathic chitosan derivative; the mediated molecule and the basic carrier are covalently bound to form a drug delivery carrier; and the drug delivery carrier forms nano-micelles so as to encapsulate the drug. According to the drug delivery system, the accumulated amount and brain entry efficiency of the encapsulated hydrophobic antitumor drugs in the brain can be obviously improved, and the damage of the drug on other normal tissues is reduced.

The invention relates to an uncharged amphiphilic chitosan nano drug carrier and a preparation method and application thereof. The preparation method is characterized in that lipophilic micromolecular deoxidized bile acid and hydrophilic micromolecular glycide are respectively grafted on chitosan molecules, thus obtaining a degradable amphiphilic chitosan material with good biocompatibility; in a wide pH solution, the amphiphilic chitosan material can quickly form a nano micelle which has a grain size of 150-300nm and is uniformly distributed through the principle of molecular self assembly under ultrasound conditions; and the inner lipophilic structure of the nano micelle is beneficial to improvement of the solubility of fat-soluble drugs in the aqueous solution, thus being expected to improve the in-vivo bioavailability of the drugs. The method has the advantages of simple requirements for instruments and equipment, simple and controllable preparation process and easy realization of large scale, so that the method is suitable for preparing nano carrier release systems of antitumor drugs with high price and poor water solubility and bioavailability such as paclitaxel, doxorubicin, camptothecin, vincaleucoblastine and the like. As a new dosage form of the antitumor drugs, the drug carrier has wide market prospects and potential clinical tumor treatment values.