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PH-sensitive dentritic polymer drug carrier

A polymer and dendritic technology, which can be used in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve the problems of poor chemotherapy effect and failure, and achieve the effects of large drug loading, good stability, and reduced treatment costs

Inactive Publication Date: 2010-05-19
INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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  • Abstract
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  • Claims
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Problems solved by technology

[0006] Chemotherapy is currently the most important method in the treatment of malignant tumors other than surgery and radiotherapy. However, the effect of conventional chemotherapy on many tumors is poor or even fails.

Method used

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  • PH-sensitive dentritic polymer drug carrier
  • PH-sensitive dentritic polymer drug carrier
  • PH-sensitive dentritic polymer drug carrier

Examples

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Embodiment 1

[0017] Example 1. Preparation of pH-sensitive dendrimer drug carrier

[0018] PAMAM and acrylic acid were reacted in a mol ratio of 1:64. Solvent DCM, catalyst DCC, DMAP were reacted at room temperature for 48 hours to obtain product 1. Filtered, dialyzed and lyophilized. Folic acid and PEG, mol ratio 1:1 solvent DCM, catalyst DCC, DMAP, react at room temperature for 24 hours to obtain FA-PEG. FA-PEG and acrylic acid, molar ratio 1:1, solvent DCM, catalyst DCC, DMAP, react at room temperature for 48h. Product 2 was obtained. Filtered, dialyzed and then freeze-dried. Product 1, product 2, monomer DEA, catalyst CuBr, Bpy, carry out polymerization reaction. The solvent is a mixed solvent of methanol and water. In a closed state, pass N2, remove O2, and react at 50°C for 8 hours under the protection of N2 to obtain the final product PAMAM-MA-PDEA-MAPEG-FA. The final product of the reaction was finally treated with dialysis and freeze-dried to obtain the final product.

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Abstract

The invention discloses a pH-sensitive dentritic polymer drug carrier. The structure of the drug carrier is one of the following: (1) A-B-C, (2), (3) A-B-C-D and (4), wherein A is dentritic polymer core comprising repeated groups, B is pH-sensitive polymer, C is hydrophilic polymer and D is targeting molecule. The pH-sensitive dentritic polymer has a nano-grade grain diameter, and can be used for coating antitumor drug. Besides, the pH-sensitive dentritic polymer has strong tumor targeting effect in vivo, thereby releasing drug quickly after reaching the tumor position.

Description

technical field [0001] The invention relates to the fields of pharmaceutical polymer materials and biomedicine, in particular to a pH-sensitive dendritic polymer and its application as a drug carrier. The polymer can be used as a nano-carrier for antitumor drugs, antiviral drugs, and gene therapy drugs . Background technique [0002] Dendrimers are a kind of artificially synthesized macromolecules. Its invention is only more than 20 years ago, but its research has penetrated into various industries, its application range is continuously expanding, and its potential application value is eye-catching. Dendritic polymers are composed of repeating units. Polyamidoamine (PAMAM) is the most common. Its characteristics include highly symmetrical structure, perfect single-molecule nanospheres, extremely high functional group density on the surface, controllable size and shape, and unique physical and chemical properties. It has minimal toxicity and is not immunogenic. These proper...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61K47/34A61P35/00A61K47/10
Inventor 金义光任霞杜丽娜杨江勇李淼
Owner INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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