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Tree-like polymer targeting nanometer drug delivery carrier and its preparation method

A nano-drug delivery carrier and dendritic polymer technology, which is applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of difficult targeted drug delivery and small drug loading, and achieve the effect of high drug loading

Inactive Publication Date: 2013-06-05
万礼 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned polymers have their own characteristics and have achieved certain effects, their drug loading capacity is relatively small. Therefore, it is still necessary to continue to study new targeted drug delivery nanocarriers based on dendrimers (PAMAM), and it is expected that the above-mentioned carriers have unique characteristics. Drug release properties to meet specific targeted drug delivery sites and specific tumor uses
Most of the carrier drugs for tumor treatment at the present stage are aimed at solid tumors, while liquid tumors represented by myeloma are difficult to carry out targeted drug delivery because tumor cells are scattered throughout the body and cannot be administered in a centralized manner.

Method used

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  • Tree-like polymer targeting nanometer drug delivery carrier and its preparation method
  • Tree-like polymer targeting nanometer drug delivery carrier and its preparation method
  • Tree-like polymer targeting nanometer drug delivery carrier and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1P

[0043] Example 1 PEG 5k -b-PAMAM G3 -Cys 8 preparation method

[0044] method:

[0045] a) taking 3 generations of polyamide-amine type dendritic polymer homocystamine to react in an equimolar ratio to obtain intermediate 1 with a yield of 90%;

[0046] b) Intermediate 1 reacts with maleimide-based polyethylene glycol monomethyl ether in an equimolar ratio in tris(2-chloroethyl) phosphate under the condition of pH 7.0 to obtain Intermediate 2, Polyethylene glycol molecular weight 5000, yield 85%;

[0047] c) at the end of PAMAM or -NH 2 , connect the sulfhydryl groups through ionic bonds to obtain the nano drug delivery carrier PEG 5k -b-PAMAM G3 -Cys 8 , yield 61%:

[0048] The synthetic route of above-mentioned reaction is:

[0049]

Embodiment 2P

[0050] Example 2PEG9k -b-PAMAM G4 -Cys 16 method of making

[0051] It is basically the same as Example 1, except that PEG is polyethylene glycol with a molecular weight of 9000, PAMAM is a 4th generation polyamide-amine dendritic polymer, hydrozone is hydrazone, and doxorubicin.

Embodiment 3

[0052] Example 3PEG 2k -b-PAMAM G2 -Cys 2 method of making

[0053] It is basically the same as Example 1, except that PEG is polyethylene glycol with a molecular weight of 2000, PAMAM is a 2nd generation polyamide-amine dendritic polymer, hydrozone is hydrazone, and doxorubicin.

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Abstract

The invention relates to a tree-like polymer targeting nanometer drug delivery carrier. The structural general formula of the nanometer drug delivery carrier is PEG-b-PAMAM-(Cys)n. According to the invention, the carrier is sensitive to pH, and a hydrogen bond between the carrier and a drug will break when the pH of the environment is low, so the drug is released, and targeting drug delivery is realized. The carrier has an effective treatment effect on myeloma. A large amount of lactic acid generated in the myeloma cell propagation process because of glycolysis causes a case that the pH of focus positions is lower than the normal pH of a body fluid, and the osteoclast formation and activation and the enzyme catalysis bone break further reduce the pH, so complication syndromes, such as osteolytic damages and the like, are caused. The carrier has the characteristics of specificity, slow release and high drug load, and can substantially improve the treatment effects on liquid tumors, such as myeloma and the like.

Description

technical field [0001] The invention belongs to a nanometer drug delivery carrier, in particular to a dendrimer targeted nanometer drug delivery carrier and a preparation method thereof. Background technique [0002] Nano-drug delivery carriers with targeting effect prepared based on dendrimers (PAMAM) are research hotspots in recent years. Chinese patent CN101259284A discloses a dendrimer-based nano-prodrug system for liver targeting, the general formula of which is T-PEG-PAMAM-(DOX)n. Chinese patent CN101294955A discloses a method for preparing a probe molecule that specifically recognizes tumor cells, including a synthesis step of dendritic molecule-polyethylene glycol-folate. Chinese patent CN101327328A discloses a dendrimer targeting nanoparticle and its preparation and application. The general formula is PAMAM-PEG-X, wherein X is a targeting gene such as folic acid, galactose, polypeptide, liposome, antibody, etc. CN101569751A discloses a tumor-targeting non-ionic de...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61P35/00C08G81/02
Inventor 杨烨顾春艳孙晓泉陆美玲万礼王旭立
Owner 万礼
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