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146results about How to "Avoid devouring" patented technology

Mesoporous nano silicon ball compound targeting drug delivery system as well as preparation method and application thereof

The invention relates to a mesoporous nano silicon ball compound targeting drug delivery system as well as a preparation method and application thereof. The preparation method of the mesoporous nano silicon ball compound targeting drug delivery system comprises the following steps: 1) preparing amino-functionalized drug loading mesoporous silicon dioxide microspheres; 2) preparing hyaluronic acid-hydrosulphonyl polypeptide-adriamycin (HA-RGD-DOX); 3) preparing mesoporous microsphere-hyaluronic acid-hydrosulphonyl polypeptide-adriamycin--paclitaxel (MSNs-HA-RGD-DOX_PTX); and 4) preparing fluorescent marker modified mesoporous microsphere-hyaluronic acid-hydrosulphonyl polypeptide-adriamycin--paclitaxel compound (MSNs-HA-RGD-DOX-PTX). The mesoporous nano silicon ball compound targeting drug delivery system has the beneficial effects that firstly multi-targeting synergistic drug delivery is realized, multiple tumour cells and tissues can be killed, and reversal drug resistance is good; secondly, blood stability is excellent; thirdly, invisibility, drug release degree and controlled release properties are good; fourthly, in vivo tracing function is good; and fifthly, the mesoporous nano silicon ball compound targeting drug delivery system has good general applicability.
Owner:WUHAN UNIV OF TECH

Preparation method and application of RGD-modified ultra-small magnetic iron oxide nanoparticles

The invention discloses a preparation method of RGD-modified ultra-small magnetic iron oxide nanoparticles. The preparation method comprises the following steps: preparing ultra-small magnetic iron oxide nanoparticles by taking ferric acetylacetonate as a reaction raw material and a precursor, taking oleylamine as a surfactant and a reducing agent and taking dibenzyl ether as a solvent; replacing oleylamine molecules wrapped on the surfaces of the nanoparticles by utilizing dopamine-modified HOOC-PEG-COOH to realize PEG-modification of the surfaces of the nanoparticles; and finally, chemically coupling RGD cyclic peptide by virtue of free carboxyl at the tail end of the PEG to obtain the RGD-modified ultra-small magnetic iron oxide nanoparticles. The method of synthesizing the ultra-small magnetic iron oxide nanoparticles has the characteristics of a simple process, a high raw material conversion ratio, strong repeatability and the like. The synthesized magnetic iron oxide nanoparticles have the characteristics of a regular morphology, an ultra-small dimension, good stability, good monodispersity, high biocompatibility, and tumor specific targeting, and the like, and can be used as a T1-weighted imaging high-performance magnetic resonance imaging contrast agent with a tumor active targeting function.
Owner:SOUTHEAST UNIV

Method for synthesizing multifunctional active targeted hyaluronic acid-polylactic acid carrier and preparing anti-tumor medicinal micelle of multifunctional active targeted hyaluronic acid-polylactic acid carrier

The invention belongs to the fields of polymer chemistry and medicinal preparations, and particularly relates to a method for synthesizing an active targeted hyaluronic acid-polylactic acid carrier, a method for preparing an anti-tumor medicinal micelle of the active targeted hyaluronic acid-polylactic acid carrier and an application thereof. By adopting a novel self-assembly technology, amphipathic PEG (polyethylene glycol) block polyester copolymer and tumor targeted ligand hyaluronic acid-polylactic acid copolymer are self-assembled by means of the electrostatic interaction to form a multifunctional composite micelle; the solubility of insoluble tumor medicaments and the drug loading capacity and encapsulation efficiency of water-soluble anti-tumor medicines can be remarkably improved by virtue of the anti-cancer drug-loaded micelle and composite micelle composition, the medicines can be biodegraded in a body, phagocytosis of a reticuloendothelial system (RES) and excretion of a kidney can be avoided. The active targeted hyaluronic acid-polylactic acid carrier has a long-circulating effect, the multifunctional composition has a prominent advantage of tumor active targeting effect, and parameters of pharmacodynamics in vitro and in vivo of the micelle are remarkably superior to those of common anti-tumor injections. Clinically acceptable administration means of the micelle includes injection administration or mucosal administration, and preparations of the micelle can be injection, transfusion, injection lyophilized powder injections or dry powder inhalation.
Owner:CHINA PHARM UNIV

Antitumor medicine conjugate with folic acid receptor-mediated and photoresponsive functions, and preparation method thereof

The invention belongs to the technical field of high-molecular medicine, and particularly relates to an antitumor medicine conjugate with folic acid receptor-mediated and photoresponsive functions and a preparation method thereof. The preparation method comprises the following steps: firstly, performing amidation reaction on folic acid and amino polyethyleneglycol; then performing amidation reaction on a product obtained in the former step and 7-ethyloic-4-hydroxymethyl coumarin to obtain a polyethyleneglycol flexible chain with a folic acid receptor targeting function and a photoresponse group; finally enabling the polyethyleneglycol flexible chain to be coupled with an antitumor medicine containing amino with an ester activation method to obtain the antitumor medicine conjugate with the folic acid receptor-mediated and photoresponsive functions. The conjugate prepared by the invention can target a tumor cell through a folic acid receptor-mediated function, and enters the cell via the endocytosis to accelerate the accumulation speed of the medicine in the tumor cell; when being irradiated by ultraviolet light with a specific wavelength or near-infrared light, the conjugate is photolyzed to release original medicine, and the medicine quickly reaches the effective concentration, so that controllable 'time / space' treatment is realized; in addition, the method provides a simple and effective manner for preparing target-controllable photoresponsive high-molecular medicine conjugates.
Owner:YANCHENG INST OF TECH

Paclitaxel polymer bonding drug and preparation method thereof

The invention provides a paclitaxel polymer bonding drug comprising a carboxyl end group contained polymer and paclitaxel esterified and bonded together with the carboxyl end group contained polymer. A preparation method of the carboxyl end group contained polymer comprises the steps of subjecting an aliphatic cyclic ester monomer to ring opening polymerization under the action of a catalyst by taking methoxy polyethylene glycol or polyethylene glycol as an initiator to obtain an amphiphilic polymer; subjecting the amphiphilic polymer and disulfide bond contained diacid to reaction in a first organic solvent under the action of organic alkaline and a condensing agent to obtain the carboxyl end group contained polymer. The solubility of paclitaxel in water can be increased by using the paclitaxel polymer bonding drug; the paclitaxel polymer bonding drug has reduction sensibility so as to be capable of being self-assembled to form a micelle; the paclitaxel polymer bonding drug has favorable hydrophilicity and biocompatibility, so that human reticuloendothelial system phagocytosis in blood circulation can be avoided, and the paclitaxel polymer bonding drug has sufficient time to reach a cancer position through an EPR (Enhanced Permeability and Retention) effect and further enters cells through endocytosis, thus an efficient targeting effect of the drug is achieved.
Owner:CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI

Method for synthesizing brain targeting head modification cyclodextrin (CD) derivative

The invention relates to a method for synthesizing a brain targeting head modification cyclodextrin (CD) derivative. The method comprises the following steps of: preparing an intermediate, namely, a mono-6-p-methylbenzene sulfonic acid-beta-cyclodextrin ester from beta-CD by an alkali aqueous solution method and introducing active amino into the reaction of the mono-6-p-methylbenzene sulfonic acid-beta-cyclodextrin ester to obtain amino-modified beta-cyclodextrin; and connecting the amino-modified beta-cyclodextrin with a mercapto brain targeting head through iso-functional group disubstituted polyethylene glycol derivative N-hydroxysuccinimide polyethylene glycol-maleimide maleinimide to prepare the brain targeting head modification cyclodextrin derivative. The method has the advantages that: the method for preparing the brain targeting head modification cyclodextrin derivative is simple and convenient, a reaction condition is mild and the derivative is taken as a medicament carrier and is easy for industrial production; a polyethylene glycol (PEG) long-chain structure is contained, so that long circulation effect is achieved and a carrier is prevented from being phagocytosed by a netlike endothelial system; and the structure is connected with a brain targeting head Tf or Lf, so that the brain transport rate of the structure serving as a medicament conveying carrier is increased.
Owner:EAST CHINA UNIV OF SCI & TECH

Multifunctional synergistic pharmaceutical composition based on adriamycin and construction method of multifunctional synergistic pharmaceutical composition

The invention relates to a multifunctional synergistic pharmaceutical composition based on adriamycin. According to the pharmaceutical composition, natural hydrophobic small molecules having a conjugated structure are covalently coupled with a polysaccharide skeleton to form an anti-angiogenesis drug, the anti-angiogenesis drug is physically mixed with the conjugated structure-modifying mitochondria damage peptide derivative and adriamycin, and the pharmaceutical composition of a nano size is assembled by virtue of various supramolecular driving forces. The pharmaceutical composition has the advantages of simultaneously regulating a tumor micro environment and tumor cells, reversing the anti-apoptosis characteristics of tumor cells, and maximizing the antitumor effect of the adriamycin. Inaddition, the multifunctional synergistic pharmaceutical composition has the advantages of the adriamycin such as high load, high stability and high targeting. The multifunctional synergistic pharmaceutical composition based on the adriamycin is compatible with corresponding medicinal auxiliary materials to prepare antitumoar drug preparations for injection, oral administration or external use. The multifunctional synergistic pharmaceutical composition is prepared by virtue of a multi-component supramolecular combination construction, so that the operation is simple, and the industrialized production is easy to realize.
Owner:CHINA PHARM UNIV

Paclitaxel-entrapped biodegradable nanocomposite and preparation method thereof

The invention belongs to the technical field of biological medicines and relates to a paclitaxel-entrapped biodegradable nanocomposite and a preparation method thereof. A paclitaxel polyethylene glycol-poly trimethylene carbonate (PEG-PTMC) nanocomposite is prepared by adopting an emulsification/solvent evaporation method, and by taking a PEG-PTMC copolymer as a carrier, paclitaxel is entrapped in a hydrophobic core of PTMC. The solubility of the paclitaxel can be effectively increased by the prepared paclitaxel PEG-PTMC nanocomposite, and a PEG long chain of a carrier material can take effect of invisibility, and thereby, the phagocytosis of an in-vivo reticulo-endothelial system is avoided. The nanocomposite has a long circulation effect, and the half-life period of the nanocomposite in blood can be prolonged. Moreover, through controlling the grain size of the nanocomposite, a passive targeting effect on a tumor tissue is realized, and thereby, a treatment effect is improved. As the nanocomposite does not contain Cremophor El or ethanol, compared with commercially available paclitaxel injections, the toxic and side effects of the nanocomposite can be reduced, and the safety of the nanocomposite in clinical application is enhanced.
Owner:FUDAN UNIV
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