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High molecule adriamycin bonding medicine nano capsule with targeting function and preparation thereof

A technology of nanocapsules and doxorubicin, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and capsule delivery, etc. problem, to achieve the effect of low production cost, reduction of toxic and side effects, and reduction of drug dosage

Inactive Publication Date: 2008-08-06
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This loading method always has an insurmountable shortcoming: initial burst release
However, the permeability of capillaries itself is a very complicated issue. Different organs, tissues, different lesions, and different stages of lesions will change the structure and permeability of capillaries. Therefore, it has not been actively used so far. EPR effect to precisely design the size of polymer drugs

Method used

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  • High molecule adriamycin bonding medicine nano capsule with targeting function and preparation thereof
  • High molecule adriamycin bonding medicine nano capsule with targeting function and preparation thereof
  • High molecule adriamycin bonding medicine nano capsule with targeting function and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Synthesis of polyethylene glycol-polylactic acid-doxorubicin bonded drug (PEG-PLA-Dox)

[0040] Add 1.1 g of carboxyl-terminated block polymer PEG-PLA-COOH into a 50 ml ampoule, wherein the molecular weight of the PEG segment is 400, and the molecular weight of the PLA segment is 4000. Then add 20ml of anhydrous dimethyl sulfoxide, after the polymer is dissolved, add 200mg of doxorubicin, 0.06ml of TEA and 50mg of DMAP, react at 0°C for 24h, filter out the precipitate generated during the reaction, and use the filtrate with anhydrous ether Settling gave a white precipitate which was dried in vacuo. The mass content of doxorubicin in the bonded drug is 12%.

Embodiment 2

[0041] Embodiment 2: the block copolymer ( N Preparation of Boc-PEG-PLA)

[0042] 2g of molecular weight 400 N Add Boc-PEG-OH to a dry ampoule with a water separator, reflux condenser and magnetic stirrer, add 40ml of anhydrous toluene, azeotropically remove water for 30 minutes, then cool to room temperature, add 20g of ethyl acetate The lactide (LA) monomer was recrystallized three times, and the reaction bottle was ventilated three times with high-purity argon, then added stannous octoate whose molar number was 1 / 500 of the LA monomer, stirred and reacted at 110°C for 12h, and then the product Dissolve in an appropriate amount of dichloromethane, settle with ether to obtain a white product, and dry it in vacuum at 40°C to obtain N Boc-PEG-PLA block polymer, its number average molecular weight is 4400 (by 1 Calculated by H NMR).

Embodiment 3

[0043] Example 3: Amino-terminated block copolymer NH 2 -Synthesis of PEG-PLA

[0044] 1.1g block copolymer N Boc-PEG-PLA was dissolved in a mixed solvent of 10 ml of dichloromethane and 5 ml of trifluoroacetic acid, stirred at 0°C for 2 h, and then the dichloromethane and trifluoroacetic acid were removed by rotary evaporation. Add 10ml of triethylamine to the obtained solid, and stir at room temperature for 8h. The reaction product was precipitated with ether, filtered, washed, and dried in vacuo to obtain an amino-terminated block copolymer NH 2 - PEG-PLA having a number average molecular weight of 4300.

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Abstract

The invention provides a nanometer capsule of a macromolecule adriamycin bonding medicine with a targeting function and a preparation method thereof. The nanometer capsule is mixed assembled with two block copolymers of poly ethylene glycol-polylactic acid, wherein the polylactic acid chain end of one block copolymer is connected with adriamycin, with a molar ratio of 98-70 percent in the nanometer capsule, while the poly ethylene glycol chain end of the other block copolymer is connected with lactose, with a molar ratio of 2-30 percent in the nanometer capsule. The adriamycin connected with the polylactic acid chain end is located in the capsule inner core, which is double protected by polylactic acid and poly ethylene glycol and has sustained release function; while the lactose connected with the poly ethylene glycol chain end is located in the outer layer of the capsule, which has targeting function and leads the nanometer capsule preferentially enter the cells carrying the lactose receptors.

Description

technical field [0001] The invention relates to polymer doxorubicin-bonded drug nanocapsules with targeting function and a preparation method thereof, belonging to the field of polymer medicines. Background technique [0002] Doxorubicin is an anthracycline antitumor antibiotic. It is a non-specific drug for the cell cycle. It has the strongest effect on the S phase and also has an effect on the M, G1 and G2 phases. Its mechanism of action is mainly that doxorubicin does not intercalate into DNA through molecules and inhibit nucleic acid synthesis. It is mainly used for the treatment of acute leukemia, malignant lymphoma, liver cancer, lung cancer, gastric cancer, esophageal cancer, breast cancer, cervical cancer, bladder cancer, testicular cancer, thyroid cancer, soft tissue tumors, osteosarcoma and neuroblastoma, etc. At present, clinical administration is mostly intravenous infusion, but doxorubicin cannot pass through the blood-brain barrier, and the drug is rapidly dis...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61K47/34A61K9/51A61P35/00A61K47/26A61K47/59A61K47/60
Inventor 景遐斌胡秀丽吕常海陈学思黄宇彬郑勇辉柳时
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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