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Star polymer nano-medicament carrier preparation used for intracellular medicament delivery and preparation method thereof

A nano-drug carrier and star-shaped polymer technology, which is applied in the fields of polymer materials and medical engineering, can solve the problems of large side effects and low drug bioavailability, achieve good micelle stability, and facilitate encapsulation and delivery. The effect of the simple and easy synthesis method

Inactive Publication Date: 2011-02-02
苏州同科生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a star-shaped polymer nano-drug carrier preparation for intracellular drug delivery, which solves the problem of polymer nano-micelles as drug carriers in the prior art, which are difficult to enter into target cells and cause drug bioavailability. Lower, more side effects and other issues

Method used

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  • Star polymer nano-medicament carrier preparation used for intracellular medicament delivery and preparation method thereof
  • Star polymer nano-medicament carrier preparation used for intracellular medicament delivery and preparation method thereof
  • Star polymer nano-medicament carrier preparation used for intracellular medicament delivery and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0049] Embodiment 1 Preparation of amphiphilic six-arm star-shaped block copolymer nano drug carrier preparation

[0050] a) Add dry dipentaerythritol and ε-caprolactone into the polymerization tube at a molar ratio of 1:120, under anhydrous and anaerobic conditions, add stannous octoate according to 0.1% of the total molar weight of the monomers, under nitrogen Under protection, solution polymerization was carried out in dry toluene, the polymerization temperature was 110°C, and the polymerization time was 20 hours. The obtained polymer was precipitated, filtered, washed, and vacuum-dried to obtain a six-armed star-shaped polyhexene containing terminal hydroxyl groups. Lactone (6sPCL), number average molecular weight 13000.

[0051] b) Polyethylene glycol monomethyl ether (MPEG), dithiodipropionic acid, N, N-dicyclohexylcarboimide (DCC) and 4-dimethylaminopyridine (DMAP) with a molecular weight of 2000 The ratio (molar ratio) of 1:5:5:1 was dissolved in dry dichloromethane, ...

Embodiment 2

[0054] Embodiment 2 Preparation of amphiphilic four-arm star-shaped block copolymer nano drug carrier preparation

[0055] a) Add dry pentaerythritol and L-lactide into the polymerization tube at a molar ratio of 1:70, under anhydrous and anaerobic conditions, add stannous octoate according to 0.1% of the total molar weight of the monomers, under nitrogen protection The bulk polymerization was carried out at 120°C, and the polymerization time was 24 hours. The obtained polymer was precipitated, filtered, washed, and vacuum-dried to obtain a four-armed star-shaped polylactic acid (4sPLLA) containing terminal hydroxyl groups. The number average molecular weight 9600.

[0056] b) Dissolving polyethylene glycol monomethyl ether (MPEG), dithiodibutyric acid, DCC and DMAP with a molecular weight of 1500 in dry dichloromethane at a ratio (molar ratio) of 1:4:4:1, The reaction was stirred at 40°C for 40 hours. After the reaction finishes, remove the precipitate by filtration, concen...

Embodiment 3

[0059] Example 3 Preparation of amphiphilic three-arm star-shaped block copolymer nano drug carrier preparation

[0060] a) Dry glycerol and D, L-lactide are added into the polymerization tube at a molar ratio of 1:50, under anhydrous and oxygen-free conditions, stannous octoate is added according to 0.15% of the total molar weight of the monomers, Bulk polymerization was carried out under the protection of nitrogen, the polymerization temperature was 125 ° C, and the polymerization time was 22 hours. The prepared polymer was precipitated, filtered, washed, and vacuum-dried to obtain a three-arm star polylactic acid (3sPLA) containing terminal hydroxyl groups. The number average molecular weight is 6800.

[0061] b) Dissolving polyethylene glycol monomethyl ether (MPEG), dithiodibutyric acid, DCC and DMAP with a molecular weight of 5000 in dry tetrahydrofuran at a ratio of 1:6:6:1 (molar ratio) at 35 The reaction was stirred at °C for 45 hours. After the reaction, remove the...

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Abstract

The invention discloses a star polymer nano-medicament carrier preparation used for intracellular medicament delivery. The nano-medicament carrier preparation is characterized by comprising the following components in part by weight: 1 to 20 parts of medicament, 10 to 200 parts of amphiphilic star segmented copolymer, and 20 to 500 parts of organic solvent, wherein the amphiphilic star segmented copolymer in the carrier is formed from hydroxyl-terminated star aliphatic polyester by connecting a hydrophilic segment through a disulfide bond. By using a self-assembling behavior of the copolymer in aqueous solution, nanoparticles of which internal hydrophobic layers coat the medicament can be prepared by a dialysis method. After entering cells, the nano-medicament carrier can prompt a hydrophilic shell thereof to drop selectively by using a reducing environment in tumor cells so as to realize localized release of the medicament in the tumor cells.

Description

technical field [0001] The invention belongs to the field of macromolecular materials and medical engineering, and in particular relates to a star-shaped polymer nano drug carrier which can be used for intracellular drug delivery and a preparation method thereof. Background technique [0002] Cancer is a kind of disease that seriously endangers human health, so research on cancer treatment has always been a focus of attention. Chemotherapy is the most commonly used method among the three major methods of cancer treatment (chemotherapy, radiotherapy and surgical resection). Chemotherapy is of great significance for the treatment of cancer and the control of metastasis of cancer cells. There are also problems, such as: exposed drugs have strong toxic and side effects when circulating in the body; the distribution of drugs in the body is lack of selectivity; the bioavailability of drugs is too low; most anti-tumor drugs have poor water solubility; The metabolism in the body is...

Claims

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Application Information

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IPC IPC(8): A61P35/00A61K47/34A61K9/14
Inventor 任天斌李建波冯玥李永勇贾梦虹
Owner 苏州同科生物科技有限公司
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