188 results about "Targeted liposomes" patented technology

This invention provides a liposomal construct for delivering a diagnostic or therapeutic agent to a mammal comprising a liposomal carrier, a diagnostic or therapeutic agent entrapped within or associated with said liposomal carrier and a sequestering agent distributed within said liposomal carrier to reduce leakage of the diagnostic or therapeutic agent from the liposomal construct prior to delivery.

A metal targeting complex which associates with a charged liposomal structure is provided. The metal targeting complex provides the targetability of the liposomal construct to the desired receptor sites of a warm-blooded host for therapy or diagnostic use.

The invention relates to an injection anticancer long circulating targeting liposome which is characterized in that anti-angiogenic drug is combined with anticancer drug, the liposome modified by polypeptide with tumor targeting function and hydrophilic polyethyleneglycol is adopted for loading and transporting the two drugs to tumor positions, and the tumor curative effect is enhanced through the different releasing rates and action mechanism of the two drugs.

The present disclosure provides lipid-containing compositions, including targeted liposomes encapsulating drug, and pharmaceutical formulations thereof, as well as methods for the making and using the lipid-containing compositions, including the use of the targeted liposomes in the treatment of cancer and other diseases.

The present disclosure provides lipid-containing compositions, including targeted liposomes encapsulating drug, and pharmaceutical formulations thereof, as well as methods for the making and using the lipid-containing compositions, including the use of the targeted liposomes in the treatment of cancer and other diseases.

The invention discloses a dual target liposome and a preparation method and application thereof. The target liposome provided by the invention consists of liposome and modifiers on the surface of the liposome, wherein the modifiers on the surface of the liposome comprise p-aminophenyl-alpha-D-manno-pyranoside and transferrin. The invention also discloses a medicament-loaded liposome, which is obtained by wrapping daunorubicin by using the target liposome. The obtained target liposome has good capability of crossing the blood brain barrier, targets brain glioma, and can be used as a medicament carrier. The medicament-loaded liposome can target the medicament to a brain glioma site after crossing the blood brain barrier so as to greatly increase the concentration of the medicament at a tumor site and improve the effect of chemotherapy. The target liposome provides a new measure for brain glioma chemotherapy, contributes to the research of non-invasive therapy of the brain glioma, and has important theoretical meaning and clinical meaning.

The present invention is in the field of drug delivery, and specifically, cationic liposome-based drug delivery. In embodiments, this invention provides methods of making ligand-targeted (e.g., antibody- or antibody fragment-targeted) liposomes useful for the delivery of liposomes to tumors, including brain tumors. In embodiments, the liposomes deliver temozolomide across the blood-brain barrier for treatment of primary or metastatic brain tumors. Additional cancers that can be treated with the liposomes include neuroendocrine tumors, melanoma, prostate, head and neck, ovarian, lung, liver, kidney, breast, urogenital, gastric, colorectal, cervical, vaginal, angiosarcoma, liposarcoma, rhabdomyosarcoma, choriocarcinoma, pancreatic, retinoblastoma and other types of cancer. In another embodiment the liposomes deliver melphalan for the treatment of multiple myeloma, other tumors of the blood or other solid tumors. In still other embodiments the liposomes can deliver other drugs such as pemetrexed or irinotecan for treatment of cancer or drugs including atropine for treatment of organophosphate poisoning.

An immunoliposome composition targeted to the alphaV-integrin subunit of integrin receptors comprised of ligand-targeted liposomes bearing at least one targeting-ligand derived from an antibody and having binding specificity for at least one integrin receptor comprising an alpha V subunit including αvβ1, αvβ3 αvβ5, αvβ6, or αvβ8 integrin cell receptors is described. The antibody-derived targeting ligand may be a Fab′ fragment, a scFv, or the like. Binding of the immunoliposome to αv-integrin expressing cells, preferably results in internalization of the immunoliposome for cytoplasmic delivery of a liposome-entrapped agent.

A metal targeting complex which associates with a charged liposomal structure is provided. The metal targeting complex provides the targetability of the liposomal construct to the desired receptor sites of a warm-blooded host for therapy or diagnostic use.

The invention provides indocyanine green nanometer targeted liposome. The indocyanine green nanometer targeted liposome comprises indocyanine green, a phospholipid layer and a folic acid-modified polyethylene glycol derived phospholipid layer, wherein the indocyanine green is surrounded by the phospholipid layer; the folic acid-modified polyethylene glycol derived phospholipid layer comprises polyethylene glycol derived phospholipid and folic acid connected with the polyethylene glycol derived phospholipid through an amido bond; phospholipid in the polyethylene glycol derived phospholipid is inserted in the phospholipid layer; the folic acid is exposed outside the phospholipid layer; the mass ratio of the indocyanine green to the phospholipid to the folic acid-modified polyethylene glycol derived phospholipid is (1-5): (1-3): (1-3). The invention further provides a preparation method of the indocyanine green nanometer targeted liposome and photo-thermal treating application thereof; when the indocyanine green nanometer targeted liposome is applied, the indocyanine green is difficultly gathered, and has excellent stability and a targeting property.

The present invention discloses one kind of folic acid acceptor targeting liposome as medicine carrier and its preparation process and application. The liposome has components including synthetic phospholipid, cholesterol, folic acid acceptor targeting anchor point and polyglycol hydrating anchor point. The present invention has relatively simple preparation process, and can prepare liposome of size smaller than 200 nm in large scale and prepare freeze dried powder of weak alkali medicine, including leurocristine, etc. carried on the liposome with greatly raised use convenience and stability. The medicine is re-constructed with bacteria-free water or brine before use, and the medicine leakage rate is lower than 10 %.

The present invention relates to integrin ligand modified long circulation liposome carrying anticarcinogen for injection, and is especially one kind of injected anticarcinogen carrying targeting liposome administration system. The efficient administration system is obtained through modifying the surface of liposome simultaneously with both polyethylene glycol and integrin containing arginine-glycine-asparagic acid sequence or RGD analogue.

The invention relates to a targeted lipidosome drug-loading system containing aptamers and a preparation method of the system. The targeted lipidosome drug-loading system containing the aptamers comprises the aptamers, an antitumor drug and nano-liposomes prepared from sphingomyelin, wherein the antitumor drug is wrapped with the nano-liposomes and the aptamers are connected onto the nano-liposomes through chemical bonds for specifically identifying tumor cells. The nano-liposomes are prepared from sphingomyelin and are connected with an appropriate quantity of the aptamers after the antitumor drug is wrapped with the nano-liposomes, sphingomyelin contains more amido bonds and can resist chemical and biological degradation better, protect stability of a lipidosome structure and increase the drug accumulation content of the tumor cells, and accordingly, the antitumor effect is improved.

Provided is a novel peptide ligand (Leu-Ala-Arg-Leu-Leu-Thr) for binding to an EGFR surface pocket based on its 3D crystal structure. When conjugated to the distal end of liposome surface PEG moieties, the peptide ligand directs liposome binding and uptake by EGFR high expressing cancer cells (H1299 and SPCA1) specifically and efficiently. The targeted delivery of liposomal anticancer drug doxorubicin results in better therapeutic efficacy towards cells in vitro. In vivo, the targeted liposomes are injected via tail vein and the time course of their distribution and accumulation in xenograft tumor tissues are studied using a live animal fluorescence imaging system. The LARLLT targeted liposomes were seen to gradually concentrate at the tumor site and be preferentially retained more than 80 hours after injection.

Provided is a novel peptide ligand (Leu-Ala-Arg-Leu-Leu-Thr) for binding to an EGFR surface pocket based on its 3D crystal structure. When conjugated to the distal end of liposome surface PEG moieties, the peptide ligand directs liposome binding and uptake by EGFR high expressing cancer cells (H1299 and SPCA1) specifically and efficiently. The targeted delivery of liposomal anticancer drug doxorubicin results in better therapeutic efficacy towards cells in vitro. In vivo, the targeted liposomes are injected via tail vein and the time course of their distribution and accumulation in xenograft tumor tissues are studied using a live animal fluorescence imaging system. The LARLLT targeted liposomes were seen to gradually concentrate at the tumor site and be preferentially retained more than 80 hours after injection.

The invention relates to an anti-tumor targted lipidosome decorated by pH sensitive polypeptide. The lipidosome is mainly prepared by phospholipid, cholesterol, lipid-polyethylene glycol and lipid-polyethylene glycol-pH sensitive polypeptide. The pH sensitive polypeptide can have enhanced transmembrane capacity in an acidified environment of tumor tissue, and the lipidosome can be mediated to efficiently enter a cell on a tumor part.

The inventors have discovered that increased levels of intracellular zinc leads to cell death by apoptosis and necrosis. Surprisingly, p53 minus cells under cell death when treated with zinc. Thus, the invention is directed to zinc compositions useful in the targeted delivery of zinc compounds to cancer cells, to kill the cancer cells. Such compositions may contain targeted liposomes as the delivery vehicle. Likewise, the invention is directed to methods of killing cancer cells as well as treating cancer in a patient. The method involved delivering zinc-containing compositions to a cancer cell.

The invention relates to an NRP-1 ligand polypeptide-polyethylene glycol-phosphatide compound, an active targeting liposome drug delivery system mediated thereby and a preparation method thereof. A carrier system comprises; a. phosphatide; b. cholesterol; c. methoxy polyethylene glycol-phosphatide compound; and d. polypeptide-polyethylene glycol-phosphatide compound containing an RPARPAR sequence. The above components are in a molar ratio of: a:b=5:1-1:5, a:c=1000:0.1-1000:100, and a:d=1000:0.1-1000:100. The system can carry out intravenous route drug administration and target the drug to a tumour position according to tumour EPR effect and RPARPAR mediation effect. The liposome drug delivery system can be applied to tumour diagnosis or targeting delivery of a treatment medicament.

A method is disclosed for encapsulating plasmids, oligonucleotides or negatively-charged drugs into liposomes having a different lipid composition between their inner and outer membrane bilayers and able to reach primary tumors and their metastases after intravenous injection to animals and humans. The formulation method includes complex formation between DNA with cationic lipid molecules and fusogenic / NLS peptide conjugates composed of a hydrophobic chain of about 10-20 amino acids and also containing four or more histidine residues or NLS at their one end. The encapsulated molecules display therapeutic efficacy in eradicating a variety of solid human tumors including but not limited to breast carcinoma and prostate carcinoma. Combination of the plasmids, oligonucleotides or negatively-charged drugs with other anti-neoplastic drugs (the positively-charged cis-platin, doxorubicin) encapsulated into liposomes are of therapeutic value. Also of therapeutic value in cancer eradication are combinations of encapsulated the plasmids, oligonucleotides or negatively-charged drugs with HSV-tk plus encapsulated ganciclovir.

The invention belongs to the medical field, and specifically, relates to a novel glycyrrhetinic acid-modified lipid, a liver targeting liposome, a micelle and a compound, and their preparation method. The novel glycyrrhetinic acid-modified lipid contains glycyrrhetinic acid as a liver targeting mediating material, and is utilized as a membrane material of a liposome or a micelle to enable the liposome or the micelle to have liver targeting activity. Specifically, the novel glycyrrhetinic acid-modified lipid is prepared from raw materials of glycyrrhetinic acid and a phosphatide or cholesterol by a reaction in a condensing agent-containing solvent. The invention also provides a liver targeting liposome carrier and a liver targeting micelle carrier mediated by glycyrrhetinic acid. The liver targeting liposome carrier is prepared from the novel glycyrrhetinic acid-modified lipid, cholesterol and a phosphatide. The liver targeting micelle carrier is prepared directly from the novel glycyrrhetinic acid-modified lipid. The invention also provides a liver targeting liposome compound or a liver targeting micelle compound comprising an encapsulation layer of the liver targeting liposome carrier and the liver targeting micelle carrier. Therefore, glycyrrhetinic acid mediation-related drugs can be targeted to hepatic cells; toxicity of the glycyrrhetinic acid mediation-related drugs on normal tissue is reduced; and drug effects of prevention and treatment of liver complaints are improved.

The invention belongs to the field of pharmacy, and relates to a brain tumor multiple targeting drug delivery system of a stability polypeptide mediated cross-barrier film, which is composed of stability polypeptide DCDX and c(RGDyK) and liposome. The drug delivery system is can resist an endogenous enzyme barrier and mediate cross-blood cerebral barrier (BBB) and blood-brain tumor barrier(BBTB). The experiment result displays that the liposome can delivers an entrapment model medicine to a target tissue, survival stage of the glioma model animal can be prolonged by the entrapment doxorubicin, and the curative effect of the medicine can be obviously increased. The brain tumor multiple targeting drug delivery system has good application prospect on diagnosis and treatment of brain tumor.

A solid phase synthesis method for preparing peptide-spacer-lipid conjugates, the peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the peptide-spacer-lipid conjugates. The present invention provides a convenient solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to automation, the purification is easier in each reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides a peptide-spacer-lipid conjugate prepared by the solid phase synthesis method of the present invention, which can be incorporated into a liposome as the targeting moiety for liposomal drug delivery to specific cells, and provides a targeting liposome containing the present peptide-spacer-lipid conjugate.

The present invention is a composition and process for avoiding non-specific uptake of targeted liposomal complexes in the lung and other highly vascular issues. The reversible masking of liposomal complexes allows increased delivery of nucleic acid molecules to target cells or tissues.

The invention relates to a method for preparing a dual-function targeting quantum dot lipidosome. The method comprises the following steps: preparing a single quantum dot lipidosome: dissolving phospholipid, cholesterol, methoxy polyethylene glycol-phospholipid complex and NRP-1 ligand polypeptide polyethylene glycol phospholipid complex into chloroform to obtain a uniform lipid membrane, and drying the chloroform by evaporation; dissolving in an ammonium sulfate solution of quantum dots, and oscillating to obtain lipidosome suspension; extruding, and diluting with normal saline to obtain an active targeting lipidosome containing the quantum dots; adding the active targeting lipidosome containing the quantum dots into an adriamycin normal saline solution, and treating in a water bath for 20 minutes at the temperature of 60 DEG C; and diluting with normal saline through a SephadexG-50 gel column, removing free medicaments, and thus obtaining the dual-function targeting quantum dot lipidosome. The lipidosome prepared by the method can be used for marking and treating glioma cells.

The invention belongs to the technical field of medicines, and particularly discloses a composition and a preparation method of cyclic dinucleotide cGAMP (cyclic Guanosine Adenosine Monophosphate) encapsulated by a targeting liposome and application of the cyclic dinucleotide cGAMP to anti-tumor. The targeting liposome consists of lecithin, cholesterol, polyethylene glycol and the like as well as a link targeting molecule of the targeting liposome; a cGAMP slow release drug encapsulated by the targeting liposome can be used for enhancing the intensifying cell osmosis action, enhancing an immune reaction, effectively targeting drug delivery and intensifying the inhibition on the growth of multiple tumor cells. Therefore, the cGAMP encapsulated by the targeting liposome can be used for preparing an anti-tumor targeting slow release drug, and has important potential application in the field of targeting immune anti-tumor.

The invention relates to an anti-tumor multi-medicine resistant targeted liposome and a preparation method thereof, in particular to an anti-tumor multi-medicine resistant long circulating targeted liposome. The invention is characterized in that: quercitin and an anti-tumor medicine are jointly coated in the liposome, and simultaneously target tumor tissues to reverse the multi-medicine resistance of tumors, cytotoxicity of anti-tumor medicines on medicine resistant tumors is enhanced, the change of pharmacokinetic properties of the anti-tumor medicines in vivo and the enhancement of toxic and side effects of the anti-tumor medicines in vivo, which are caused by the difference and interaction of the pharmacokinetic properties of different medicines in vivo, are avoided, and the treatmenteffect on medicine resistant tumors is improved.

The invention belongs to the biology medicine field, and relates to a fiber growth factor receptor (FGFR)-mediated vascular targeted liposome carrier, a preparation method thereof and an application thereof. The invention aims at solving the technical problem of proving a cationic liposome with high transfection efficiency and tumor vascular targeting. The targeted liposome is prepared by using the components with the following mixture ratios: the mixture ration of DOTAP, cholesterol and tb FGF polypeptide is: the mol ratio of the DOTAP to the cholesterol equals to 2:1-2, and the weight of the tb FGF polypeptide is 10-80 percent of the total weight of the DOTAP and the cholesterol. The liposome can be combined with the FGF receptor (FGFR) on the surface of tumor new-generated vascular cells particularly, and can realize the preparation method thereof and the application of tumor vascular targeting therapy by wrapping up various micromolecule anti-tumor drugs, therapy genes and adenoviral vectors carrying therapy genes.

There is provided targeting drug delivery system (DDS) nanoparticles that can be accumulated in target tissues such as inflammatory sites of inflammatory diseases and can thus be utilized in a therapeutic or diagnostic DDS for locally delivering drugs or genes to the affected parts. The present invention provides a pharmaceutical composition for the medical treatment or diagnosis of an inflammatory disease comprising a sugar-modified liposome having a sugar chain bound to the membrane of the liposome.

The present invention provides for liposomes loaded with a therapeutic agent, which liposomes are targeted to a cell of interest by incubation with a targeting protein protein conjugated to a linker molecule comprising a hydrophobic domain, a hydrophilic polymer chain terminally attached to the hydrophobic domain, and a chemical group reactive to one or more functional groups on a protein molecule and attached to the hydrophilic polymer chain at a terminus contralateral to the hydrophobic domain, for a time sufficient to permit the hydrophobic domain to become stably associated with the liposome.