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Long-circulating anti-tumor targeting drug carrier and preparation method thereof

A monomer and polymer technology, applied in the field of long-circulating anti-tumor targeted drug carrier and its preparation, can solve the problems of non-specific protein adsorption, wide molecular weight distribution, uncontrollable molecular weight, etc. The effect of adsorption, narrow molecular weight distribution and controllable molecular weight

Inactive Publication Date: 2013-06-12
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the PHPMA carrier also has obvious shortcomings: it has a single function and does not have the function of preventing non-specific adsorption of proteins, resulting in the adsorption and accumulation of drugs in non-focused parts during blood circulation, resulting in insufficient circulation time of drug carriers in the body, affecting The therapeutic effect of the drug; in addition, because the preparation of the current PHPMA carrier generally adopts ordinary free radical polymerization, the molecular weight is uncontrollable and the molecular weight distribution is very wide, which seriously affects the EPR effect of the carrier and the release of the drug from the carrier, thereby further affecting the treatment of the drug Effect

Method used

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  • Long-circulating anti-tumor targeting drug carrier and preparation method thereof
  • Long-circulating anti-tumor targeting drug carrier and preparation method thereof
  • Long-circulating anti-tumor targeting drug carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1, PEG 2k -b-PMAGG 8k preparation of

[0034] Dissolve 2.4 g of hydroxyl- and methyl-terminated PEG with a number average molecular weight of 2000 in 40 mL of toluene, add 0.68 g of 4-dithiobenzoate-4-cyanovaleric acid (CPAD) and 0.041 g of DMAP, and wait After complete dissolution, 0.74 g of DCC was added and reacted for 90 hours under stirring at room temperature. Suction filtration, pour the filtrate into excess diethyl ether, suction filtration, the resulting precipitate was dissolved in a small amount of toluene, and then precipitated with diethyl ether, and this was repeated three times. The precipitate was vacuum-dried at 40° C. for 24 hours, and the obtained product was a macromolecular chain transfer agent of PEG.

[0035] Take 0.13g of this chain transfer agent, 0.46g of MAGG, 5mg of 4,4'-azobis(4-cyanovaleric acid) and 5mL of pure water, put them in a vacuum reaction tube, vacuumize under refrigeration, and then return to room temperature, Infl...

Embodiment 2

[0038] Example 2, PEG 2k -b-(PHPMA 20k -co-PMAGG 15k ) preparation

[0039] The preparation method of the block copolymer is basically the same as in Example 1, except that the original MAGG is changed to a mixture of HPMA and MAGG for feeding, and the feeding amounts are 1.16 g of HPMA and 0.87 g of MAGG. When the reaction was terminated, the reaction tube was quickly put into liquid nitrogen, and then the small molecules were removed by dialysis, and finally the solvent was evaporated to obtain the desired product. The molecular weight and composition of the product can be determined by aqueous GPC and 1 HNMR to co-confirm.

[0040] Products with different compositions and molecular weights can be obtained according to different reaction times. If the reaction time is 48 hours, the number average molecular weight of the obtained copolymer is 37000, the molecular weight distribution is 1.09, the molecular weight of the PMAGG part is 15000, and the molecular weight of the...

Embodiment 3

[0041] Embodiment 3, polymer PEG containing amino acid 2k -b-PMAGG 20k preparation of

[0042] 2.2g polymer PEG 2k -b-PMAGG 20k With 0.072g tyrosine in 10ml mass concentration of 10% sodium carbonate aqueous solution, with 0.191g EDC and 0.115g (NHS) as a catalyst, react overnight at 4 ° C, then dialyze in pure water for 4 × 6h, freeze-dried Polymer PEG containing tyrosine 2k -b-PMAGG 20k . That 1 H NMR spectrum see image 3 .

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Abstract

The invention discloses an anti-tumor targeting drug carrier and a preparation method thereof. The carrier is a high polymer copolymerized by PEG, HPMA and MAGG. A polymerization method of reversible addition-fragmentation transfer (RAFT) is used to obtain copolymerizing components and copolymer with controllable molecular weight and narrow molecular weight distribution (the molecular weight distribution d being less than 1.4), a general formula of the copolymer being PEG-b-P (HPMA-co-MAGG). By adjusting a PEG chain length of the polymer, a composition ratio of the HPMA and the MAGG and the molecular weight of the polymer, the anti-tumor targeting drug carrier with substantially increased circulation time in body is obtained. The polymer can be used for targeting transportation of the antitumor drugs; not only is high in targeting and good in biocompatibility, but also can prevent nonspecific protein adsorption and prolong the circulation time in body; and is the excellent anti-tumor targeting drug carrier.

Description

technical field [0001] The invention relates to a long circulation anti-tumor targeting drug carrier and a preparation method thereof. Background technique [0002] Tumor has always been a major disease that threatens human health. At present, there are three main treatment methods for tumor treatment: surgery, chemotherapy and radiotherapy. However, there are situations such as high mortality rate, low cure rate and poor prognosis in various treatment methods. Although chemotherapy and radiotherapy have significant curative effects in the treatment of tumors, there are still many problems. For chemotherapy, due to the lack of targeting of chemotherapy drugs themselves, it is difficult to effectively reach the lesion site, and while killing tumor cells, it will also non-selectively kill normal cells, so there are low treatment efficiency and toxic side effects. Major problems seriously affect the treatment effect of cancer. For radiotherapy, due to the limited penetration...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F222/38C08F220/58C08F2/38C08G65/48C08F8/32C08F8/20A61K47/34A61K51/06A61P35/00A61K101/02
Inventor 魏振柯喻青松石旭东甘志华
Owner INST OF CHEM CHINESE ACAD OF SCI
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