10 results about "Docetaxel-PNP" patented technology

Treatments of cancers involve a wide range of treatment. The current invention relates to chemotherapy of tumors using taxanes, in particular docetaxel. More in particular it relates to a method for the treatment of a cancer in a patient comprising orally administering an effective dose of docetaxel, whereby side effects are controlled by preventing peak plasma levels of docetaxel that induce said side effects, whilst maintaining an effective plasma level of docetaxel to eradicate tumor cells.

The present invention provides an amphiphilic acid-sensitive docetaxel polymer prodrug based on acetal bond and its preparation. The prodrug molecule provided by the present invention can be prepared by modular reaction, with simple, efficient, general and highly extensible methods. The prodrug molecule can be used to prepare docetaxel prodrug micelle preparations by self-assembly in aqueous solution. The obtained prodrug micelle preparations have the characteristics of simple preparation, good micelle stability and rapid acid-responsive activation. They are relatively stable under normal physiological pH conditions, while the acetal bond can be rapidly and responsively cleaved under acidic pH conditions, so as to realize the responsive and traceless release of docetaxel, improve the hydrophilicity of docetaxel and reduce its toxic and side effects while enhancing the anti-tumor effect.

Provided are a docetaxel adiposome formulation, a preparation method therefor, and use thereof. The docetaxel adiposome formulation comprises a monomolecular phospholipid membrane and docetaxel and a neutral lipid that are wrapped in the monomolecular phospholipid membrane. Targeted modification is further carried out on the surface of the docetaxel adiposome. The adiposome formulation has good bioavailability and safety, and the anti-cancer effect of the formulation is significantly superior to that of a clinically used docetaxel injection.

The application discloses a kind of photodynamic balloon catheter systems, comprising: tube body, with opposite proximal end and distal end;Balloon, the balloon is fixed in the distal end portion of the tube body;Optical fiber assembly is inserted in the tube body, and with the light-emitting site extending to adjacent the balloon;The surface of the balloon is loaded with auxiliary material and photosensitizer in the form of coating;The photosensitizer can activate collagen and elastin under the wavelength of light 400-460nm to make them crosslink;The auxiliary material includes active drug and sustained-release material wrapped the active drug, the active drug is at least one of paclitaxel, rapamycin, zotarolimus, tacrolimus, everolimus, temsirolimus, zanolimus, biolimus, docetaxel, protein-bound paclitaxel and protein-bound dexamethasone;By the photodynamic balloon catheter system of the application can improve the utilization rate of active drug in intravascular administration.

Provided are a docetaxel liposome formulation, a preparation method therefor, and use thereof. The docetaxel liposome formulation comprises a monomolecular phospholipid membrane and docetaxel and a neutral lipid that are wrapped in the monomolecular phospholipid membrane. Targeted modification is further carried out on the surface of the docetaxel liposome. The liposome formulation has good bioavailability and safety, and the anti-cancer effect of the formulation is significantly superior to that of a clinically used docetaxel injection.

Synthesizing a drug-organic-acid-anhydride conjugate using docetaxel as a drug, including: mixing aconitic anhydride with a chlorinating reagent to produce a first mixture; dissolving the first mixture in an organic solvent to produce a dissolved mixture; stirring the dissolved mixture; evaporating the organic solvent from the dissolved mixture to produce a second mixture; washing the second mixture with an impurity remover to remove impurities and to produce an aconitic anhydride chloride solution; and mixing the docetaxel with the aconitic anhydride chloride solution to produce the drug-organic-acid-anhydride conjugate.

The invention discloses a double-target modified liposome as well as a preparation method and application thereof. The double-target modified liposome is formed by modifying a CL4 aptamer and a VTP polypeptide on the surface of a liposome. The invention proves that the CL4 and VTP modified liposome has an obvious active targeting drug delivery effect on colorectal cancer, the double-target modification targeting effect is superior to that of a single target, in-vivo and in-vitro experiments show that the uptake rate of the double-target liposome is improved by 10%-20% compared with that of the single target liposome, and a synergistic interaction effect is achieved. According to the invention, the dual-target modified liposome preparation simultaneously loaded with docetaxel and kaempferol is synthesized for the first time, and a research report that a nano-carrier simultaneously loads the docetaxel and the kaempferol is not found yet. In-vivo and in-vitro experiments prove that the CL4 and VTP modified liposome co-loaded with docetaxel and kaempferol has a remarkable effect of inhibiting the proliferation of colorectal cancer compared with a pure drug combination / unmodified double-loading / single-loading liposome, and has a good practical application value.

Synthesizing a docetaxel-aconitic anhydride conjugate using docetaxel, including: mixing aconitic anhydride with a chlorinating reagent to produce a first mixture; dissolving the first mixture in an organic solvent to produce a dissolved mixture; stirring the dissolved mixture; evaporating the organic solvent from the dissolved mixture to produce a second mixture; washing the second mixture with an impurity remover to remove impurities and to produce an aconitic anhydride chloride solution; and mixing the docetaxel with the produced aconitic anhydride chloride solution to produce the docetaxel-aconitic anhydride conjugate.

The application discloses a docetaxel nano prodrug targeting tumor cells and tumor stem cells and a preparation method and application thereof. A docetaxel compound is synthesized through esterification and thiol-maleimide addition reaction, and a nano drug-loaded particle is prepared based on the docetaxel compound, so that the problems of low drug loading, poor targeting and tumor stem cell drug resistance in the prior art are solved, meanwhile, the nano drug-loaded particle can realize precise enrichment of the drug at a tumor site, improve the anti-tumor effect and reduce toxicity.