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High molecule bonding adriamycin medicine, nano capsule and preparation thereof

A combination of doxorubicin and doxorubicin, applied in capsule delivery, microcapsules, nanocapsules, etc., can solve the problems of low drug loading and sudden release of drugs, and achieve reduced dosage and low production costs , to avoid the effect of sudden drug release

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

However, drug dosage forms such as liposome injections, microspheres, and implanted sustained-release agents in the body all have problems such as low drug loading and sudden drug release.

Method used

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  • High molecule bonding adriamycin medicine, nano capsule and preparation thereof
  • High molecule bonding adriamycin medicine, nano capsule and preparation thereof
  • High molecule bonding adriamycin medicine, nano capsule and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: the synthesis of block polymer PEG-PLA-OH

[0040] Add 4 g of polyethylene glycol (PEG-OH) with a number average molecular weight of 400 to a dry ampoule with a water separator, reflux condenser and magnetic stirrer, add 40 ml of anhydrous toluene, and azeotropically remove water for 30 minutes , then cooled to room temperature, 10 g of lactide (LA) monomer recrystallized three times with ethyl acetate was added, the reaction bottle was ventilated three times with high-purity argon, and then octanoic acid sulfide, which was 1 / 500 of the molar number of LA monomer, was added. Tin, stirred and reacted at 110°C for 24h, then dissolved the product in an appropriate amount of dichloromethane, settled with ether to obtain a white product, dried in vacuum at 40°C to obtain a PEG-PLA-OH block polymer, and its number-average molecular weight is 1400 (by 1 Calculated by H NMR).

Embodiment 2

[0041] Example 2: Synthesis of Carboxylated Block Polymer PEG-PLA-COOH

[0042] Dissolve 1.84g of PEG-PLA-OH polymer in 10ml of 1,4-dioxane, add 0.013g of succinic anhydride, then add 0.018ml of triethylamine (TEA) and 0.016g of N,N-dimethyl Base p-aminopyridine (DMAP), react at room temperature for 12h. The salt produced by the reaction was filtered off, and the filtrate was settled with ether to obtain a white product, which was dried under vacuum at 40°C to obtain the carboxylated block polymer PEG-PLA-COOH. Its NMR spectrum is shown in Figure 2.

Embodiment 3

[0043] Example 3: Bonding of PEG-PLA-COOH and Adriamycin

[0044] Add 0.38g carboxyl-terminated block polymer PEG-PLA-COOH to a 50ml ampoule, then add 20ml anhydrous dimethyl sulfoxide, after the polymer dissolves, add 27.2mg doxorubicin, 0.007ml TEA and 6mg DMAP was reacted at 0°C for 12 hours, and the precipitate formed during the reaction was filtered off, and the filtrate was settled with anhydrous ether to obtain a white precipitate, which was dried in vacuo. The mass content of doxorubicin in the bonded drug is 12%. Its NMR spectrum is shown in Figure 3(B). For comparison, the NMR spectrum of doxorubicin is given in Fig. 3(A).

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Abstract

The invention provides a macromolecule bonding adriamycin medicine, a nanometer capsule and a preparation method thereof. The bonding medicine is bonded by a block copolymer of poly ethylene glycol-polylactic acid and adriamycin. Firstly, the block copolymer of poly ethylene glycol-polylactic acid is acquired by ring-opening polymerization of aliphatic cyclic esters with poly ethylene glycol, solvent and catalyst being in existence; then a carboxyl end group is transformed by a hydroxyl-terminated; and then with a condensing agent being in existence, the carboxyl end group carries out amidation reaction with the adriamycin; thus acquiring the macromolecule adriamycin bonding medicine. The bonding medicine has amphiphilic property, thus being able to self assembly to prepare the nanometer capsule with a core-shell structure in the water solution. The adriamycin is wrapped inside the capsule to play a role of isolation and protection, which overcomes the deficiencies of short circulation time in vivo, large dosage and severe allergic reaction existing in the current adriamycin preparation. In addition, the nanometer particles are expected to congregate in the blood circulation through the so-called 'enhanced infiltration and retention effect', so as to improve the targeting action of the adriamycin on the tumor location.

Description

technical field [0001] The invention relates to a biodegradable polymer bonded doxorubicin drug, its nanocapsule and a preparation method. Background technique [0002] The molecular structural formula of doxorubicin is as follows: [0003] [0004] It is an anthracycline antitumor antibiotic, which 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. Synthesis of nucleic acids. It is mainly used for the treatment of lung cancer, breast cancer, bladder cancer, testicular cancer, thyroid cancer, soft tissue tumor, osteosarcoma, neuroblastoma, acute leukemia and malignant lymphoma, etc. It can also be used for the treatment of gastric cancer, liver cancer, esophageal cancer and cervical cancer Wait. At present, clinical administration is mostly intravenous infusion, but doxorubicin cannot pass through the blood-brain barrier, and the drug is rapidly distributed throughout the body after ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/34A61K31/704A61K9/51A61P35/00A61K47/60
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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