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Star-like macromolecule nanometer microsphere and preparation method and application thereof

A nano-microsphere and macromolecule technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, organic active ingredients, etc. It can solve problems such as nanocarriers and other problems, and achieve the effect of good drug release function, stable chemical properties and good biocompatibility.

Active Publication Date: 2013-06-12
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At this time, the drug encapsulated in the nanospheres will be released in advance before reaching the tumor site, which will weaken the function of the nano-drug carrier and affect the therapeutic effect. carrier's big problem

Method used

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  • Star-like macromolecule nanometer microsphere and preparation method and application thereof
  • Star-like macromolecule nanometer microsphere and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: 5, 10, 15, 20-tetrakis (4-aminophenyl) porphyrin (TAPP) as an initiator to initiate polymerization ε - caprolactone

[0021] Under argon protection, TAPP (16.85 mg, 0.025 mmol), stannous octoate (1.00 mg, 0.0025 mmol), ε - Caprolactone (0.7 g, 6.14 mmol) was added into a 10 mL round bottom flask, and the mixture was heated and stirred at 110°C for 72 h. After the reaction was complete, the solid was dissolved in dichloromethane and precipitated in cold methanol. filtered, washed with ether, and dried in vacuo to obtain poly ε - caprolactone compound (TAPP-PCL). 1 H NMR (CDCl 3 , 300MHz) δ : 1.39 (m, 2H), 1.63 (m, 4H), 2.30 (t, 2H), 4.05 (t, 2H), 7.94 (d, porphyrin), 8.14 (s, porphyrin), 8.85 (s, porphyrin). The molecular weight of the polymer was determined to be 23394 by size exclusion chromatography.

Embodiment 2

[0022] Embodiment 2: Dipyridamole is used as an initiator to initiate the polymerization of caprolactone

[0023] Under argon protection, dipyridamole (12.61 mg, 0.025 mmol), stannous octoate (1.00 mg, 0.0025 mmol), ε - Caprolactone (0.7 g, 6.14 mmol) was added into a 10 mL round bottom flask, and the mixture was heated and stirred at 110°C for 72 h. After the reaction was complete, the solid was dissolved in dichloromethane and precipitated in cold methanol. filtered, washed with ether, and dried in vacuo to obtain poly ε - caprolactone compound (Dipyridamole-PCL). 1d H NMR (CDCl 3 , 300MHz) δ : 1.39 (m, 2H), 1.63 (m, 4H), 2.30 (t, 2H), 4.05 (t, 2H), 1.72 (m, dipyridamole), 3.81 (m, dipyridamole), 4.27 (m, dipyridamole). The molecular weight of the polymer was determined to be 22985 by size exclusion chromatography.

Embodiment 3

[0024] Example 3: 5, 10, 15, 20-tetrakis (4-aminophenyl) porphyrin (TAPP) as an initiator to initiate polymerization ε - caprolactone

[0025] Under argon protection, TAPP (16.85 mg, 0.025 mmol), stannous octoate (1.00 mg, 0.0025 mmol), ε - Caprolactone (0.3 g, 6.14 mmol) was added into a 10 mL round bottom flask, and the mixture was heated and stirred at 110°C for 72 h. After the reaction was complete, the solid was dissolved in dichloromethane and precipitated in cold methanol. filtered, washed with ether, and dried in vacuo to obtain poly ε - caprolactone compound (TAPP-PCL). 1 H NMR (CDCl 3 , 300MHz) δ: 1.39 (m, 2H), 1.63 (m, 4H), 2.30 (t, 2H), 4.05 (t, 2H), 7.94 (d, porphyrin), 8.14 (s, porphyrin), 8.85 (s, porphyrin). The molecular weight of the polymer was determined to be 12674 by size exclusion chromatography.

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Abstract

A star-shaped polymer nanosphere with 5,10,15,20-tetrakis (4-aminophenyl) porphyrin or dipyridamole (Dipyridamole) as the core, characterized in that its surface is hydrophilic The polyethylene glycol of water, the interior is hydrophobic polyε-caprolactone, the molecular weight of the polymer nanosphere is 30000~50000, the molecular weight of the hydrophilic part is 5000×4, and the molecular weight of the hydrophobic part is 10000~30000, The average particle size of the nano-microspheres is 20-60nm. The composite nano microsphere of the invention has good biocompatibility and stable chemical properties. The star-shaped macromolecule nano microsphere of the invention can be used as a drug carrier, has a slow-release effect, and can also be used as a fluorescent label. The invention discloses its preparation method and application.

Description

technical field [0001] The invention relates to a biodegradable star-shaped macromolecular nano microsphere, which can be used as a drug carrier, specifically, as a carrier of paclitaxel. Background technique [0002] Paclitaxel is a compound extracted from the bark of Taxus brevifolia. It is a specific stabilizer of microtubules, which can promote the assembly of microtubules and maintain the stability of microtubules. In cells, paclitaxel binds to polymerized microtubules and does not react with unpolymerized tubulin dimers. Cells exposed to paclitaxel will accumulate a large number of microtubules in the cells, and the accumulation of these microtubules interferes with the normal function of cancer cells (stopping cell division in mitosis, blocking normal cell division). Paclitaxel is mainly suitable for ovarian cancer and breast cancer, and it is also effective for lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma and brain tumor. Since the solub...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/34A61K31/337A61K49/12A61P35/00
Inventor 蒋锡群张鲁中武伟张亚军
Owner NANJING UNIV
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