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Novel efficient anti-tumor targeting drug carrier and preparation method thereof

A polymer chain and monomer polymerization technology, which is applied in the direction of antineoplastic drugs, drug combinations, and pharmaceutical formulations, can solve problems such as wide molecular weight distribution, single function, and uncontrollable molecular weight, and achieve high targeting, excellent performance, and The effect of good biocompatibility

Inactive Publication Date: 2014-07-23
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Novel efficient anti-tumor targeting drug carrier and preparation method thereof
  • Novel efficient anti-tumor targeting drug carrier and preparation method thereof
  • Novel efficient anti-tumor targeting drug carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1, preparation PEG 5k -b-P(HPMA 30k -co-MAGG 5k -co-BHMAGG 8k )

[0050] Dissolve 2.4g of single-terminal hydroxyl or amino PEG with a number average molecular weight of 5000 in 40mL of dry toluene, add 0.68g of CPAD and 0.041g of DMAP, add 0.74g of DCC after complete dissolution, and stir at room temperature for 96 hours. Suction filtration, pour the filtrate into excess diethyl ether, and then 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.

[0051] Take 52mg of macromolecular chain transfer agent, 312.5mg of HPMA, 52mg of MAGG, 83mg of BHMAGG, 1mg of 4,4'-azobis(4-cyanovaleric acid), and 5mL of DMSO in a Shrek tube, vacuumize under refrigeration, and then recover Return to room temperature, fill with argo...

Embodiment 2

[0053] Embodiment 2, preparation PEG 5k -b-P(HPMA 30k -co-MAGG 5k (Folate)-co-BHMAGG 8k )

[0054] Folate-NH 2 Preparation: 4.41g of folic acid and 10-fold excess of ethylene glycol bis-2-aminoethyl ether were reacted at 35°C for 48 hours in anhydrous DMSO as a solvent under the catalyst of EDC and NHS equivalent to folic acid. After the reaction was completed, the reaction solution was poured into water for precipitation. The filtrate was collected and freeze-dried, and the product was purified by semi-preparative liquid chromatography (Shimadzu LC-6AD, Japan).

[0055] PEG 5k -b-P(HPMA 30k -co-MAGG 5k (Folate)-co-BHMAGG8k ) preparation: the PEG prepared in Example 1 5k -b-P(HPMA 30k -co-MAGG 5k -co-BHMAGG 8k ) and Folate-NH 2 With anhydrous DMSO as solvent, it is prepared under the catalysis of EDC and NHS.

[0056] The specific steps are: take 0.5g PEG 5k -b-P(HPMA 30k -co-MAGG 5k -co-BHMAGG 8k ) was dissolved in 20ml of anhydrous DMSO, 0.3g of EDC and 0.1...

Embodiment 3

[0057] Example 3, PEG 5k -b-P(HPMA 30k -co-MAGG 5k (Folate)-co-HMAGG 8k (Dox)) preparation

[0058] The PEG prepared in 100mg embodiment 2 5k -b-P(HPMA 30k -co-MAGG 5k (Folate)-co-BHMAGG 8k ) first remove the Boc protection in 15ml of pure trifluoroacetic acid, the reaction time is 30 minutes, after the reaction is completed, the trifluoroacetic acid is removed by rotary evaporation to obtain PEG 5k -b-P(HPMA 30k -co-MAGG 5k (Folate)-co-HMAGG 5.4k ). The product was dissolved in 20ml of anhydrous DMSO, 100mg of Dox and 0.2ml of glacial acetic acid were added, and reacted at 37°C for 48 hours. After the reaction was completed, the resulting reaction solution was purified with a gel chromatographic column, and the characterization results were as follows: figure 2 with image 3 shown.

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Abstract

The invention discloses a novel efficient anti-tumor targeting drug carrier and a preparation method thereof. The carrier is a diblock copolymer consisting of a chain segment A and a chain segment B, wherein the chain segment A is PEG, and the chain segment B is a random copolymer formed by the following three monomers: HPMA, MAGG and BHMAGG. By adoption of a reversible addition fragmentation chain transfer polymerization method, the copolymer with controllable copolymerization components and molecular weight, and narrow molecular weight distribution (with the molecular weight distribution PDI being less than 1.4) is obtained. By modification of side chain functional groups of the MAGG and the BHMAGG in the polymer, a water-soluble polymer drug carrying system with significant targeting and controlled drug release functions is obtained. The polymer drug carrying system can be used for efficient transportation of anti-tumor drugs, has advantages of high targeting property, good biocompatibility, adjustable drug carrying amount, and drug release with pH responsiveness, and is an anti-tumor targeting drug carrier with excellent performances.

Description

technical field [0001] The invention relates to a novel high-efficiency 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 methods for the treatment of tumors: surgery, chemotherapy and radiotherapy. However, various treatment methods still have problems such as low cure rate, high recurrence and high mortality. At present, some chemotherapeutic drugs are commonly used clinically to treat tumors, such as doxorubicin, epirubicin, daunorubicin, carboplatin, nitrogen mustard (Chlormethine) and paclitaxel ( Paclitaxel) and other drugs have shown remarkable curative effect in the treatment of tumors, but there are still many problems, mainly because the drugs themselves lack targeting, and it is difficult to effectively reach the lesion site. At the same time, while these drugs kill tumor cells, they also non-selectively kill normal t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08F220/58C08F222/38C08F2/38C08G65/48C08F8/32C08F8/28A61K47/48A61K45/00A61K31/704A61P35/00
Inventor 喻青松甘志华
Owner INST OF CHEM CHINESE ACAD OF SCI
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