76 results about "Dspe peg" patented technology

The invention discloses a mitochondrion-targeting nano-drug delivery system, comprising polyethylene glycol connected with TPP and thioketal linker connected with a chemotherapeutic drug, the polyethylene glycol and the thioketal linker are connected with each other through amino and carboxyl condensation. This system also comprises DSPE-PEG and a photosensitizer; the chemotherapeutic drug forms a hydrophobic core inside, a hydrophilic shell layer is formed in the center of the polyethylene glycol, a mitochondrion-targeting crown is formed outside the TPP, and the photosensitizer is of hydrophobic structure distributed inside the core and/or around the core. TPP is selectively positioned to mitochondrion. This system is ROS responsive, the photosensitizer is laser excited to release ROS, and ROS cuts the thioketal linker to release the chemotherapeutic drug and can carry out photodynamic therapy at the same time, thus enabling synergic therapy of mitochondrion-targeting photodynamic therapy and chemotherapy. The invention also discloses a preparation method and application of the mitochondrion-targeting nano-drug delivery system.

The invention relates to a nanoparticle and a preparation method thereof. Poly(lactide-glycolide acid) (PLGA) is in the center to serve as a core, phospholipid surrounds the surface of the PLGA core in monolayer and distearoyl phosphatidylethanolamine-polyethyleneglycol-carboxyl (DSPE-PEG-COOH) penetrates the monolayer phospholipid to serve as the shell. The phospholipid, the DSPE-PEG-COOH and the PLGA have good biocompatibility, can entrap hydrophobic drugs and control the drugs to release slowly in the human bodies. The phospholipid surrounds the surface of the PLGA, thus ensuring that the particle can avoid immune system recognition so that the circulating half life of the particle is lengthened. The PEG shell ensures the particle to have spatial stability, static stability, long circulation and other characteristics and to be not easily agglomerated. Meanwhile, carboxyl is easily crosslinked with such ligands as antibodies, peptide, probes and the like, thus ensuring the particle to have targeting characteristic. The preparation method of the nanoparticle is simple, convenient practical and is easy to operate and popularize.

The invention provides an Au-ICG (gold-indocyanine green) lipidosome multifunctional nano probe and application thereof. The nano probe consists of a kernel and a shell, wherein the kernel is a nanogold particle of which the surface is wrapped with a poly-dopamine layer and adsorbs indocyanine green; the shell is a DSPE-PEG (distearoyl phosphatidyl ethanolamine-polyethylene glycol) lipidosome film which is coupled with lactobionic acid and is chelated with Gd<3+> ions. The Au-ICG lipidosome multifunctional nano probe disclosed by the invention can be used for various image modes such as MRI (nuclear magnetism imaging), CT (computed tomography) imaging and near infrared fluorescence imaging of the liver cancer; a patient only needs to stand medicine supplying of a contrast agent, and various diagnosis effects can be achieved; furthermore, by virtue of the improvement of the sensitivity, the using amount of the contrast agent can be reduced, so that the toxic and side effect is further relieved; under near infrared illumination at 808 nm, adsorbed ICG molecules can effectively convert light energy into heat energy to produce superhigh heat of 60-70 DEG C, so that liver cancer cells can be killed thermally; therefore, the multifunctional nano probe can be used as a multimodal contrast agent for liver cancer diagnosis and can be used as a photothermal therapy agent for the liver cancer.

The invention relates to a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. A molar ratio of the DSPE-PEG2000-FA to egg yolk lecithin is 0.05% to 0.15%, and a particle size of the liposome is less than 150 nm. A preparation method of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome comprises the following steps: first, preparing a DSPE-PEG2000-FA into a DSPE-PEG2000-FA micelle; second, performing incubation on the phosphatidyl ethanolamine-polyethylene glycol2000-folic acid micelle and a paclitaxel liposome together to obtain a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. Materials, which are forbidden to be used in clinical practice, are not used as crude materials in the present invention. According to the invention, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has a small particle size, and the content of the DSPE-PEG2000-FA is low; besides, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has good drug entrapment efficiency and good colloid stability. Moreover, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome can be absorbed effectively by an ovarian cancer cell having properties of sensitiveness to folic acid (+) and drug resistance, and the cytotoxicity of folic acid dependence is displayed; therefore, the efficacy of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome is stronger than that of a paclitaxel injection.

The preparation method of radiation-sensitive copolymer carrier for coating radiated nanoparticles and/or chemotherapy drugs includes forming a nanosphere by diselenide block copolymers and DSPE-PEG-biomarkers to coat chemotherapy drugs and/or radiated nanoparticles that can be released from the opened nanosphere by protons penetrating tissue during proton therapy. The treatment effect of proton therapy is enhanced by two ways of using the radiated nanoparticles released from an opened nanosphere to produce nuclear fission with the protons for releasing electrons to destroy cancer cells of tumor and the chemotherapy drugs released from the opened nanosphere for distributing among tissue to kill the cancer cells of the tumor.

The invention discloses a tumor-targeted delivery carrier based on cell-derived micro-vacuoles, a preparation method and an application. The preparation method comprises the following steps of: (A) preparing a conditioned medium: supplementing fetal bovine serum, antibiotics, DSPE-PEG-Biotin and DSPE-PEG-Folate into a basal medium; (B) using the obtained conditioned medium in cell culture, and collecting cell culture supernatant for subsequent separation; (C) carrying out low-speed centrifugation on the obtained culture supernatant to remove cell debris and apoptotic bodies, then adding SA-IONPs, mixing uniformly, incubating, then separating by a magnet, using PBS for re-suspension, eluting for multiple times to obtain the cell-derived micro-vacuoles with membrane surfaces modified by folic acid and iron oxide nano-particles, and freezing for storage; and (D) loading chemotherapeutic drugs or therapeutic genes into the functionalized micro-vacuoles doubly-modified by an electroporation mode, and carrying out re-suspension after separation with the magnet. The tumor-targeted delivery carrier based on cell-derived micro-vacuoles, the preparation method and the application disclosed by the invention are applicable to specific targeting delivery of multiple chemotherapeutic drugs and therapeutic genes, and have the advantages of enhancing the anti-tumor effect, reducing the systemic toxicity and improving the clinical effect of the current therapeutic selection, so that a new hope is brought for clinical therapy of tumors.

The invention relates to an anti-tumor medicine coupler decorated with saturated fatty acid and a self-assembling nanometer system and preparation method of the coupler. Firstly, the coupler obtained by decorating the structure of the anti-tumor medicine with different types of saturated fatty acid can be self-assembled into spherical nanoparticles uniform in granularity and high in stability in water; secondly, after any amphiphilic polymer material such as DSPE-PEG is added in the preparation process, the granularity of the self-assembled nanoparticles can be decreased, and the stability of the nanoparticles can be improved. By means of the method, the anti-tumor medicine where nanoparticles can hardly be self-assembled can be endowed with the self-assembling capacity, only one step of reaction is needed during synthesis, and the method is easy and convenient to implement; meanwhile, compared with a traditional carrier dependence type nanometer system and an amphiphilic prodrug micelle system, the self-assembling system has higher medicine loading capacity and higher stability; the preparation method is easier to implement and beneficial to industrial production and provides a new concept for design and establishment of nanometer medicines.

The invention discloses acetylation sugar ester-polyethylene glycol-phosphatidyl ethanolamine conjugate and a preparation method and application thereof. The acetylation sugar ester-polyethylene glycol-phosphatidyl ethanolamine conjugate is named as distearoyl-phosphatidylethanolamine-polyethylene glycol-p-p-carboxy phenyl-gamma-acid-alpha-D-acetylmannosamine (DSPE-PEG-Ac4MAN), and the acetylationsugar ester-polyethylene glycol-phosphatidyl ethanolamine conjugate has the structure shown in the formula I. In addition, the invention further provides brain-targeted liposome comprising the acetylation sugar ester-polyethylene glycol-phosphatidyl ethanolamine conjugate. A pharmacodynamic test proves that the liposome can have the 'prodrug' effect in a body, through the effect of hydrolytic enzymes in the body, cell uptake and body interior activity of drugs are improved, and the good killing activity on C6/U87 cells is achieved. A brain-targeted drug is prepared through drug-containing arsenic trioxide (arsenic trioxide), the purpose that the arsenic trioxide crosses the blood-brain barrier to treat glioma is achieved, and the survival time of mice is obviously prolonged. A new technical means is provided for treatment of brain glioma.

The invention discloses sugar-polyethylene glycol-DSPE (1,2-distearoyl-sn-glycero-3-phosphoethanolamine) conjugated compound and a preparation method and application thereof, wherein the sugar-polyethylene glycol-DSPE conjugated compound is prepared by conjugating sugar to DSPE-PEG (polyethylene glycol). The sugar is one of a monosaccharide, a disaccharide, a polysaccharide and the sugar acetylated, wherein the monosaccharide includes mannose, galactose, arabinose and glucose; the disaccharide includes maltose; the polysaccharide is maltotriose. DPSE is artificial phospholipid, having lipotropism; PEG is a hydrophilic substance; a sugar ligand is a target of a targeting material. The compound herein is applicable to the design of targeting carriers, especially liposomes and micelles, and is also applicable as a surfactant. In addition, the invention also provides the preparation method of the compound herein; materials for the preparation method are easy to attain, reaction conditionsare mild and easy to control, the preparation method is simple to perform, the product is easy to purify, and the yield is high. The product is applicable to biological researches and is important tothe preparation of drug carriers and the disease treatment.

The invention discloses a taxol liposome preparation with an active tumor targeting function. The preparation is prepared from taxol, egg yolk lecithin, cholesterol, phosphatidylethanolamine pegol, tbFGF-PEG-DSPE (truncated basic fibroblast growth factor-polyethylene glycol-distearoyl phosphatidylethanolamine) and injection water. According to the preparation, tbFGF capable of being specifically combined with tumor cells and tumor angiogenic blood vessels and maleinimide-polyethylene glycol-phospholipid (DSPE-PEG-MAL) are chemically coupled, thus preparing the tbFGF-PEG-DSPE, and a liposome is prepared from a coupling product and wraps the taxol, thus building a liposome dosage form with long circulation and active tumor targeting functions; therefore, the active tumor targeting and tumor resisting effects are enhanced.

The invention provides a targeted fluorescent liposome based on low-frequency ultrasonic response, a preparation method of the liposome and an application, and particularly provides an active targeting medicine carrying fluorescent acoustic liposome which comprises a bimolecular lamellar lipid membrane, medicines and fluorescent agents, wherein the bimolecular lamellar lipid membrane comprises dipalmitoyl phosphatidyl choline (DPPC), cholesterol (CHO), polyethylene glycol modified distearoyl phosphoethanolamine (DSPE-PEG) and (DSPE-PEG-iRGD), and the acoustic liposome wraps the medicines and the fluorescent agents. The medicines are selected from methotrexate (MTX), the fluorescent agents are selected from indocyanine green (ICG), and polyethylene glycol (PEG) in the polyethylene glycol modified distearoyl phosphoethanolamine (DSPE-PEG) is selected from PEG1000-PEG3000.

The invention discloses preparation and application of a tumor-targeting drug based on unsaturated fatty acid nanoparticles. Carboxyl groups of docosahexaenoic acid and amino groups of amino polyethylene glycol are subjected to a condensation reaction to prepare a micelle mPEG-DHA; carboxyl groups of DSPE-PEG-COOH and amino groups of Anti-HER2 are subjected to a condensation reaction to prepare amicelle DSPE-PEG-Anti-HER2; the micelle mPEG-DHA, the micelle DSPE-PEG-Anti-HER2, pyropheophorbide-a methyl ester and adriamycin are subjected to self-assembly to obtain the targeting nanoparticles DPSPAH/MPPa/DOX used for lipid peroxidation and photodynamic-chemotherapy combined tumor therapy. The nanoparticles DPSPAH/MPPa/DOX have a particle size of about 190 nanometers and good stability, can effectively control the release of chemotherapeutic drugs, have good biocompatibility, high efficiency, low toxicity and higher application prospects in the fields of nano drug carriers and nano drug tumor treatment.

The invention discloses a hydrophobic drug entrapped lipid-polymer with dual functions of targeting and radiosensitivity. The lipid-polymer comprises lipid molecules with a targeting function, a poly-nitroimidazole organic polymer with radiosensitivity and a hydrophobic anti-cancer drug, wherein the lipid molecules (DSPE-PEG-target) with the targeting function, soybean lecithin and DSPE-PEG are prepared from polypeptide and targeting molecules with the targeting function in the lipid molecules through chemical reactions, the hydrophobic poly-nitroimidazole organic polymer is prepared from functional groups, namely nitroimidazole, with the radiosensitivity under the action of polymerization, and the polymer is prepared from the targeting lipid molecules, the soybean lecithin, the poly-nitroimidazole organic polymer and the hydrophobic anti-cancer drug through hydrophilic/hydrophobic compounding. The radiosensitivity is improved, the synergetic treatment effects of radiotherapy and chemotherapy upon tumor are improved, and a toxic and side effect reduction function is achieved; and a synchronous treatment function of radiotherapy sensitizers and anti-cancer medicine molecules is achieved, and clinical practicability and practical treatment significances can be achieved.

The invention belongs to the technical field of nano-medicines, and provides a nano-particle with an excellent blood stabilizing performance, and a preparation method thereof. Poly(glycolide-co-lactide) (PLGA), a medicine/probe molecule, distearoyl phosphoethanolamine-polyethylene glycol-maleimide (DSPE-PEG) and pluronic F127 (PF127) which are used as raw materials undergo a rapid nanoprecipitation technique to prepare the nano-particle having the advantages of controlled particle size, good monodispersity, and excellent stability and performances in various solutions. A large number of hydroxyl groups and negative charges on the surface of the particle have a protection effect, so the nano-particle do not bind to proteins in serum, thereby the protein is avoided from being absorbed and metabolized by the reticuloendothelial system; and the hydrophobic medicine and the hydrophobic or amphipathic probe are encapsulated, so the particle can significantly prolong the blood circulation half-life of the medicine and the probe, and provides a good medicine delivery platform for disease detection and treatment.

The invention relates to the field of medical anti-tumor drug preparations, in particular to a tumor targeted mitomycin C and MTX (methotrexate) double-drug preparation for preventing malignant tumor growth and recurrence and a preparation method of the double-drug preparation. The tumor targeted mitomycin C and MTX double-drug preparation comprises a crude drug of mitomycin C, a carrier material and an MTX prodrug with targeting and anti-cancer functions, wherein the carrier material adopts lecithin and DSPE-PEG (distearoyl phosphoethanolamine-polyethylene glycol), and the MTX prodrug adopts DSPE-PEG-MTX. The tumor targeted mitomycin C and MTX double-drug preparation is spherical, has the grain diameter distributed between 20 nm and 80 nm, is suitable for being used as an intravenous injection preparation and has the characteristics of high targeting, long circulation, low toxicity and collaborative treatment.

This invention is to manufacture a kit for preparation of nano-targeted liposome drugs in combined chemotherapy and radionuclide therapy. It is a kit consisting of three components: (1) A 10 ml vial A which contains BMEDA, gluconate acetate, SnCl₂. (2) A 10 ml vial B which contains DSPC, cholesterol, DSPE-PEG, and Doxorubicin(DXR) (or Daunorubicin, Vinolbine). (3) A 10 ml vial C which contains ¹⁸⁸ReO₄⁻ (or ¹⁸⁶ReO₄⁻) solution. The procedure of using the kit is as follows: (1) Remove the contents of the ¹⁸⁸ReO₄⁻ (or ¹⁸⁶ReO₄⁻) solution from vial C. (2) Inject the ¹⁸⁸ReO₄⁻ (or ¹⁸⁶ReO₄⁻) solution into the vial A, and the mixtures react in appropriate temperature. (3) Remove the contents of the ¹⁸⁸Re-BMEDA (or ¹⁸⁶Re-BMEDA) solution from vial A. (4) Inject the ¹⁸⁸Re-BMEDA (or ¹⁸⁶Re-BMEDA) solution into the vial B, and the mixtures react in appropriate temperature. The reconstituted solution in the vial B is applied to combine bimodality radiochemotherapy for treatment of tumor and ascites.

The present invention is a method and compound for treating cancer and tumors. The invention treats cancer by encapsulating certain cancer fighting drugs in a liposome. Peptides attached to the compound then guide the compound towards its target. During its journey, DSPE-PEG is used to stabilize the compound, to allow more time in the blood stream before losing effectiveness.