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Drug for treating solid malignant tumors and preparation method

A technology for malignant tumors and chemotherapy drugs, which is applied in the field of drugs and preparations for the treatment of solid malignant tumors, and can solve problems such as limited treatment options, lack of specific targets, high probability of metastasis, and unproven clinical efficacy of solid malignant tumors. , to increase intake and storage, reduce interstitial hydraulic pressure, and improve microenvironment

Pending Publication Date: 2021-11-30
四川超影药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] (1) Currently available treatment options are very limited due to lack of specific targets and high probability of metastasis
[0007] (2) For the method of hyperthermia combined with nanoparticles and chemotherapeutic drugs to treat cancer, the efficacy in the treatment of solid malignant tumors has not been clinically proven
[0008] (3) Most of the existing Phase II and Phase III clinical trials have failed to prove that combined nano-drug therapy is superior to chemotherapy or hyperthermia alone, so the preclinical research and clinical transformation of chemotherapeutic drugs encapsulated by thermosensitive nanocarriers still face huge challenges. needs and challenges
[0009] The difficulties in solving the above problems and defects are as follows: (1) It is difficult for the chemotherapeutic drugs wrapped in the carrier to reach the local tumor tissue (<1%), and the nanometer cannot produce the EPR effect (Enhanced Permeation and Retention effect) in solid tumors; (2) Solid malignant Tumor tumor microenvironment (high interstitial fluid pressure, decreased blood perfusion, immunosuppression); (3) natural immune system clearance response to nanomedicine (opsonization, complement response, immune cell phagocytosis, etc.)

Method used

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  • Drug for treating solid malignant tumors and preparation method

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preparation example Construction

[0034] Such as figure 1 As shown, the preparation method of the medicine for the treatment of solid malignant tumors provided by the embodiments of the present invention adopts the double emulsion method to prepare DPPC-PLGA targeting nanoparticles loaded with paclitaxel Ptx and heat sensitizer BML, specifically comprising the following steps:

[0035] S101: first completely dissolve DPPC, amino NH2-PLGA-NH2 and paclitaxel in dichloromethane (DCM), and then add the thermal sensitizer BML dissolved in deionized water to the mixed solution;

[0036] S102: Sonic emulsify the mixed solution on an ice bath with an ultrasonic oscillator (cell pulverizer). When emulsifying, add polymer polyvinyl alcohol PVA aqueous solution (2%w / w,) and further emulsify until the nanoemulsion reaches the required diameter;

[0037] S103: Evaporate all the DCM under stirring in the fume hood, wash and collect (at least twice) by ultra-high speed centrifugation, and covalently couple hyaluronic acid t...

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Abstract

The invention belongs to the technical field of a chemotherapeutic drug wrapped by a nano-carrier, and discloses a drug for treating solid malignant tumors and a preparation method. The drug for treating solid malignant tumors is the chemotherapeutic drug wrapped by the nano-carrier. The drug wrapped by the nano-carrier for wrapping the chemotherapeutic drug consists of a shell of the nano-carrier of a polylactic acid-glycollic acid copolymer and dipalmitoyl phosphatidylcholine. hyaluronic acid used for targeting a tumor cell factor CD44, a 1-butyl-3-methylimidazole-L-lactic acid as a thermal sensitizer, and Ptx paclitaxel; the molar ratio of the polylactic acid-glycollic acid copolymer to the dipalmitoyl phosphatidylcholine is (1: 3)-(1: 5); and 1 to 5 * 10 <-4> mmol / mL of the hyaluronic acid, 2 to 10 *10 <-5> mmol / mL of the 1-butyl-3-methylimidazole-L-lactic acid, and 1 to 5 mg / mL of the Ptx. The microenvironment of tumors is effectively improved, interstitial fluid pressure of tumor tissue is reduced, and the drug resistance of the tumor tissue is reduced.

Description

technical field [0001] The invention belongs to the technical field of chemotherapy drugs encapsulated by nanocarriers, and in particular relates to a drug for treating solid malignant tumors and a preparation method thereof. Background technique [0002] Currently, chemotherapy is less effective for solid tumors, such as breast cancer. Breast cancer is the most common cancer among women worldwide and one of the leading causes of cancer-related death. Despite methods for early detection and intervention, metastatic breast cancer remains largely incurable, especially triple-negative breast cancer (TNBC). TNBC is an aggressive subtype of breast cancer, accounting for 10-20% of all breast cancer cases. Due to the lack of specific targets and the high probability of metastasis, currently available treatment options are very limited. Metastatic breast cancer is characterized by a unique tumor microenvironment (TME) that is distinct from other subtypes. Components of the TME i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K47/69A61K31/337A61K41/00A61P35/00B82Y5/00B82Y40/00
CPCA61K47/61A61K47/6937A61K47/6929A61K31/337A61K41/0052A61P35/00B82Y5/00B82Y40/00A61K2300/00
Inventor 阎锋张欢
Owner 四川超影药业有限公司
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