35results about How to "Achieve passive targeting" patented technology

The invention discloses a preparation method of a polyene-containing taxol nanoparticle mixed micelle preparation and a freeze-drying agent, which prepares docetaxel PLA-PEG nanoparticles or micelle or nanoparticle mixed micelle through a modified solvent evaporation method, takes PLA-PEG copolymer as a carrier, and wraps docetaxel in a PLA hydrophobic core. When in use, the docetaxel PLA-PEG containing long cycle freeze-dried preparation only needs to be added with water and is dissolved, and uniform nanoparticle suspension, micellar solution or mixed micellar nanoparticle suspension can be prepared. The preparation method does not need tween-80 and ethanol solubilization, only takes the biodegradable PLA-PEG as the carrier, and does not contain any surfactant; and compared with the docetaxel injection on sale, the preparation can reduce the toxicity and the adverse reactions of the medicine, and improve the clinical application safety of the medicine.

The invention discloses a zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle, and a preparation method and an application thereof, and belongs to the field of biological materials. The zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle comprises a zwitter-ion hydrophilic shell and a lyophobic core containing two acid-sensitive bonds. The method includes the steps: separating methanol from hydroxyethyl acrylate and 2,2-dimethoxypropane and synthesizing 2,2-di(acryloyloxy-1-oxethyl) propane by an alcohol exchange method; connecting open-loop beta-propiolactone with 2-(dimethylamino) ethyl methacrylate to synthesize carboxybetaine methacrylate; obtaining a carboxybetaine methacrylate monomer polymer by an atom transfer free radical polymerization method; synthesizing triblock amphiphilic polymers by the atom transfer free radical polymerization method and a Michael addition one-pot method, and preparing the drug-loading nano-micelle by an ultrasonic drop method and a dialysis method. By aid of the drug-loading micelle, anti-tumor effects of chemotherapeutic drugs can be improved.

The invention relates to a vinflunine liposome preparation and the preparation method thereof. The vinflunine liposome preparation mainly comprises vinflunine or salt, phospholipid, cholesterin and polyethylene glycol-distearoyl phosphatidyl ethanolamine of the vinflunine, wherein salt, phospholipid, cholesterin and polyethylene glycol-distearoyl phosphatidyl ethanolamine are pharmaceutically acceptable, and the vinflunine liposome preparation can be prepared into an injection or a lyophilized preparation. The preparation method is simple in technology, easy to operate and suitable for industrial production, and long-circulating vinflunine liposomes prepared by using the method are high in encapsulation rate and good in stability.

The invention discloses a glycyrrhetinic acid-modified tanshinone-loaded phase-transition ultrasonic contrast agent and a preparation method thereof. The method includes the preparation of glycyrrhetinic acid active ester, the preparation of lipid coating and the preparation of nanospheres by adopting an ultrasonic cell disruptor to perform ultrasonic processing. The grain size of the lipid nanospheres prepared by the invention is small, the average grain size is about 310nm, and passive targeting can be implemented by a tumor site EPR (Enhanced Permeability and Retention) effect. Moreover, glycyrrhetinic acid modification can also realize active targeting to the liver, consequently, the toxic and side effects of the preparation can be decreased, and the curative effect of the drug can be enhanced. On the other hand, the nanospheres which wrap low-boiling point liquid fluorocarbon with lipid as coating have good biocompatibility. Under certain conditions, enhanced ultrasonography can be performed by liquid-gas phase transition, the theranostics of tumors can be implemented after the anticancer drug tanshinone is loaded, consequently, intermediate links can be reduced, efficiency can be greatly increased, and the contrast agent has a broad clinical application prospect.

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.

The invention belongs to the technical field of medicines, and in particular relates to a nanosuspension of annonaceous acetogenin drugs prepared from such amphiphilic stabilizers as mPEG PCL, mPEG PLA, mPEG PLGA, mPEG DSPE, mPEG Chol, SPC, Tween80, BSA, TPGS and the like, as well as a preparation method and an application of the nanosuspension. The annonaceous acetogenin total lactone nanosuspension is prepared by virtue of a solvent precipitation-ultrasonic injection method, and according to a prescription, the proportioning ratio of the annonaceous acetogenin drugs to the stabilizer is at 1 to (0.02-10) (in percentage by weight). The prepared annonaceous acetogenin nanosuspension can reach a load-loading capacity to 90% to the greatest extent and can reach a minimum grain size to 123.2nm, and the nanosuspension is good in polydispersity. The nanosuspension is stable in both gastrointestinal fluid and plasma, and the nanosuspension is applicable to oral administration and injection administration; the nanosuspension has a good in-vitro sustained-release effect and is free from burst release; the nanoparticle, in comparison with a crude drug solution, is more obvious in tumor cell inhibitory rate in vitro; the nanosuspension, in in-vivo tissue distribution, shows tumor passive targeting; therefore, the nanosuspension is beneficial for enhancing efficacy and reducing toxic and side effects. Meanwhile, an in-vivo efficacy experiment shows that the nanosuspension is outstanding in antineoplastic efficacy, and the nanosuspension has a broad development prospect.

The invention discloses a metal polymer, a metal polymer nano-micelle as well as a preparation method and application of the metal polymer nano-micelle. The metal polymer or pharmaceutically acceptable salt or solvate of the metal polymer is shown as a formula I or a formula II; alkynyl is introduced into metal iridium and ruthenium complexes and reacts with water-soluble monoazide polyethylene glycol through a click reaction to synthesize the metal polymer, and the metal polymer can be self-assembled into a nano-micelle with a core-shell structure in an aqueous solution. The preparation method is simple and convenient, the reproducibility is good, the quality is controllable, in addition, the nano-micelle can greatly improve the biocompatibility of metal drugs, can be applied to optical treatment, and has potential anti-tumor application prospects.

The invention belongs to the field of molecular imaging probes and particularly relates to a preparation method of a dual-modal nano imaging drug Dex-Rho-99mTc based on glucan, and an application of the drug in imaging diagnosis. The general formula of the drug is Rho-Dex-PEG-DTPA-99mTc, wherein the Dex represents for the glucan of which the molecular weight is 10-100k, the PEG represents for polyethylene glycol of which the molecular weight is 1-10k, the Rho represents for a fluorescent group rhodamine, the DTPA is a chelating agent of an imaging nuclide and the 99mTc is a radioisotope Technetium-99 used for SPECT imaging. In the invention, the surface of the high-molecular material glucan is modified by a certain number of amino groups and the PEG, the fluorescent group and the SPECT imaging groups are connected to the glucan supporter through the amino groups and finally the drug is marked by the radioisotope [99mTc]. The drug is good in biocompatibility, is simple in the preparation method, is safe and convenient to use and can be employed in dual-modal imaging. The dual-modal nano imaging drug has wide application prospects in the biomedical fields of early diagnosis of cancer, medicine delivery under guide of imaging, noninvasive iconography curative effect evaluation and the like.

The invention discloses a medicine carrier based on a nano diamond. The medicine carrier is a nano diamond medicine carrier with doped rare earth elements, namely europium and gadolinium. A preparation method of the medicine carrier comprises the following steps: performing silanization chemical modification on the surface of a nano diamond so as to obtain a surface silanizated nano diamond, namely ND-APTES (Nano Diamond-Aminopropyl Triethoxysilane); performing silanization modification on alpha-thenoyl trifluoroacetone so as to obtain silanizated alpha-thenoyl trifluoroacetone, namely TTA-Si;enabling the surface silanizated nano diamond and silanizated organic ligand to react with Eu<3+> and Gd<+3> in a solvent, thereby obtaining the medicine carrier ND-TTA:RE<+3> based on the nano diamond. The medicine carrier based on the nano diamond, which is disclosed by the invention, is capable of not only carrying doxorubicin hydrochloride, but also carrying other medicines, and is applicableto different diseases, and transmission of different medicines can be achieved.

The invention discloses a targeted ultrasonic phase-change bimodal imaging nano contrast agent and a preparation method and an application thereof. The ultrasonic phase-change bimodal imaging nano contrast agent comprises a shell membrane and a core coated in the shell membrane, the core comprises Fe3O4 nanoparticles and liquid PFH (perfluorohexane), and the shell membrane comprises PLGA and phospholipid.

The invention belongs to the technical field of materials, and relates to a preparation and application of cobalt-doped metal organic framework nanoparticles, and the cobalt-doped metal organic framework nanoparticles have good hydroxyl radical generation capability and good drug loading performance. Doped cobalt metal ions enable the nucleation number in a reaction system to be increased, the concentration of relative ligands is greatly consumed, polyvinylpyrrolidone is used as a stabilizer, the nano-particles are protected and dispersed, the nanoparticles stop growing in a small size, and therefore synthesis of small-size CoZn-MOF-5 materials is achieved. The nanoparticle material is small in size, good in dispersity and high in loading capacity, and can be sensitively controlled to be released under the high glutathione expression acidic tumor cell microenvironment, meanwhile, cobalt ions doped in the material can react with hydrogen peroxide overexpressed by tumor cells to generate hydroxyl free radicals, the coordination of a chemical kinetic therapy and a chemical therapy is realized, and the cobalt-doped metal organic framework nanoparticles are a good nano anti-cancer drug carrier.

The invention provides a nanoparticle targeting placenta-like chondroitin sulfate A. The nanoparticle comprise a hydrophobic core, a single lipid molecular layer coating the hydrophobic cores and a hydrophilic shell targeting the placenta-like chondroitin sulfate A. The hydrophobic core comprises a hydrophobic polymer, the compound of the hydrophilic shell is a polypeptide grafted amphipathic large molecular compound, the hydrophobic end of the amphipathic large molecular compound penetrates the single lipid molecular layer, the hydrophilic end of the amphipathic large molecular compound is connected to the polypeptide through an amido bond, and the polypeptide is exposed out of the single lipid molecular layer. The amino acid sequence of the polypeptide is selected from one or more of amino acid sequences: SEQ ID NO: 1 to SEQ ID NO: 3. The invention also provides a preparation method and application of the nanoparticle as well as the polypeptide for targeting placenta-like chondroitinsulfate A.