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Novel tumor-targeting arboraceous polymer nano carrier of camptothecin drug

A technology of dendrimers and nanocarriers, applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve problems such as unsatisfactory positioning effect and inevitable cytotoxicity, so as to prolong blood circulation time, prevent degradation, The effect of improving targeting efficiency

Inactive Publication Date: 2012-05-02
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the positioning effect of passive targeting only using nano-effects is not very ideal.
Moreover, there are a large number of amino groups on the surface of the entire generation of PAMAM dendrimers, which are easily protonated and positively charged under physiological pH conditions, so they inevitably have certain cytotoxicity.

Method used

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  • Novel tumor-targeting arboraceous polymer nano carrier of camptothecin drug
  • Novel tumor-targeting arboraceous polymer nano carrier of camptothecin drug
  • Novel tumor-targeting arboraceous polymer nano carrier of camptothecin drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1. Synthesis of PAMAM

[0037] A) Purification of raw materials

[0038] Methanol was dried with iodine pellets for 24h (after adding, heated to 66°C to keep small droplets dripping drop by drop, and refluxed for 24h), then distilled at atmospheric pressure, and the collected fraction was 64-66°C;

[0039] Methyl acrylate was dried with anhydrous sodium sulfate for 24 hours (after adding, heated to 78 degrees to keep small droplets dripping drop by drop, and refluxed for 24 hours), then distilled at atmospheric pressure, and the collected fractions were 77-79 degrees Celsius;

[0040] Ethylenediamine was dried with potassium hydroxide for 24h and then distilled under reduced pressure (pressure at 1000±50Pa), collecting fractions at 45-47°C.

[0041] B) Synthesis of PAMAM G0.5

[0042] Weigh 2.0068g of ethylenediamine (about 0.033mol) in a 250mL three-necked flask, add 22.0103g of methanol under conditions of ice-water bath, electromagnetic stirring, and nitrogen prote...

Embodiment 2

[0056] 1. Synthesis of PAMAM

[0057] A) Purification of raw materials

[0058] Methanol was dried with iodine pellets for 24 hours (after adding, heated to 66°C to keep small droplets dripping drop by drop, and refluxed for 24 hours), then distilled at atmospheric pressure, and the collected fraction was 64-66°C;

[0059] Methyl acrylate was dried with anhydrous sodium sulfate for 24 hours (after adding, heated to 78°C to keep small droplets dripping drop by drop, and refluxed for 24 hours), then distilled at atmospheric pressure, and the collected fraction was 77-79°C;

[0060] Ethylenediamine was dried with potassium hydroxide for 24h and then distilled under reduced pressure (pressure at 1000±50Pa), collecting fractions at 45-47°C.

[0061] B) Synthesis of PAMAM G0.5

[0062] Weigh 2.0068g of ethylenediamine (about 0.033mol) in a 250mL three-necked flask, add 22.0103g of methanol under conditions of ice-water bath, electromagnetic stirring, and nitrogen protection, mix w...

Embodiment 3-4

[0076] Except replacing PAMAM G4.0 with PAMAM G3.0 and PAMAM G5.0 respectively, others are the same as in Example 1.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to preparation of a novel target nano carrier and application of the novel target nano carrier in a camptothecin drug targeting delivery system. The system can be represented as PAMAM-HA / drug, wherein PAMAM is polyamide amine-amine arboraceous macromolecules of different generations, HA is hyaluronic acid of different molecular weights, and the drug is one or more of camptothecin anticancer drugs such as camptothecin, 10- hydroxycamptothecine, topotecan and the like. The carrier is used for wrapping the camptothecin drugs, and has the actions of prolonging the drug blood circulation time, improving the drug bioavailability, reducing the non-tumor part concentration of the drug, reducing the drug cytotoxicity, and simultaneously protecting the lactonic rings of the camptothecin drugs from damage, thereby improving the tumor treatment efficiency from multiple aspects. The nano carrier provided by the invention has important significance in promoting the safe delivery of the camptothecin drugs and the effective treatment of tumor.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the preparation of a novel tumor-targeting dendritic polymer nanocarrier and its application in targeted delivery of camptothecin drugs. After inclusion of camptothecin drugs with dendrimers modified by hyaluronic acid, it is helpful for the administration of camptothecin compounds in the active form of lactone ring closure. Compared with the existing commercially available preparations, it has improved biological Utilization, enhanced targeting, reduced side effects, extended drug half-life, and stable storage, etc. Background technique [0002] Camptothecin (CPT), a pyrrole [3,4-b] quinoline alkaloid, was first isolated in 1966 by Wall et al. It has been found that camptothecin has certain curative effect on various malignant tumors such as head and neck tumors, bladder cancer and leukemia. Its derivative 10-hydroxycamptothecin (Hydroxycamptothecin, OPT) has a more ob...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K47/36A61K31/4745A61P35/00
Inventor 祁小乐何环吴正红马晓丽丑晓华顾琳赵可张淼焦芳
Owner CHINA PHARM UNIV
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