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A kind of microchannel preparation method of polytricaprolactone-glycerine drug delivery nanoparticle

A technology of glyceric acid and caprolactone, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, drug combinations, etc., can solve the problems of unfavorable tumor cell penetration and short half-life, and achieve strong controllability and time-consuming Short, effect of improving solubility

Active Publication Date: 2020-02-21
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Large particle size is conducive to improving pharmacokinetics and drug overflow rate in blood vessels, but not conducive to tumor cell penetration; small particle size is easy to cell penetration, but has a short half-life and is easy to eliminate

Method used

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  • A kind of microchannel preparation method of polytricaprolactone-glycerine drug delivery nanoparticle
  • A kind of microchannel preparation method of polytricaprolactone-glycerine drug delivery nanoparticle
  • A kind of microchannel preparation method of polytricaprolactone-glycerine drug delivery nanoparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Add glyceric acid (0.1761g, 1.0mmol) and caprolactone (2.2823g, 20.0mmol) into the ampoule and melt at 120°C, then add stannous octoate catalyst (0.0201g, 0.05mmol), shake to mix evenly, Add N to the ampoule 2 , to ensure an oxygen-free environment, after quick sealing, react at a high temperature of 120°C for 12 hours, cool to room temperature after the reaction, add 20mL of dichloromethane to dissolve, then drop into 250mL of glacial ether to precipitate a precipitate, collect the precipitate by filtration, and dry it in a vacuum at 40°C for 24h. Obtain 1.1793 g of Tri-CL star-shaped polyester, and set aside.

[0043] The average molecular weight by GPC is 5369, the PI is 1.39, and the final yield is 47.97%.

Embodiment 2

[0045]Add glyceric acid (0.1761g, 1.0mmol) and caprolactone (3.4235g, 30.0mmol) into the ampoule and melt at 120°C, then add stannous octoate catalyst (0.0300g, 0.075mmol), shake to mix evenly, Add N to the ampoule 2 , to ensure an oxygen-free environment, after quick sealing, react at a high temperature of 120°C for 12 hours, cool to room temperature after the reaction, add 20mL of dichloromethane to dissolve, then drop into 250mL of glacial ether to precipitate a precipitate, collect the precipitate by filtration, and dry it in a vacuum at 40°C for 24h. Obtain 2.5953 g of Tri-CL star-shaped polyester, and set aside.

[0046] The average molecular weight by GPC is 10904, the PI is 1.27, and the final yield is 72.10%.

Embodiment 3

[0048] Add glyceric acid (0.1761g, 1.0mmol) and caprolactone (3.4235g, 30.0mmol) into the ampoule and melt at 140°C, then add stannous octoate catalyst (0.0300g, 0.075mmol), shake to mix evenly, Add N to the ampoule 2 , to ensure an oxygen-free environment, after quick sealing, react at a high temperature of 120°C for 24 hours, cool to room temperature after the reaction, add 20mL of dichloromethane to dissolve, then drop into 250mL of glacial ether to precipitate a precipitate, collect the precipitate by filtration, and dry it in a vacuum at 40°C for 24h. Obtain 2.5698g of Tri-CL star-shaped polyester, set aside.

[0049] The average molecular weight by GPC is 10612, PI is 1.18, and the final yield is 71.39%.

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Abstract

The invention provides a micro-channel preparation method of poly-epsilon-caprolactone-tricarballylic acid drug delivery nanoparticles. Tricarballylic acid serves as a chain extension initiator, epsilon-caprolactone is subjected to high-temperature ring opening grafting with stannous octoate as a catalyst, and amphipathic star-shaped polyester is prepared under the protection of nitrogen; curcumin serves as a model drug, a curcumin-nanoparticle preparation which is small in size, uniform in particle size and high in encapsulation efficiency is prepared through the micro-channel continuous granulating technology, the average particle size of the curcumin-nanoparticles is 100-300 nm, the polydispersity index is small than 0.3, and the encapsulation efficiency is larger than 70%; by means of the poly-epsilon-caprolactone-tricarballylic acid drug delivery nanoparticles, the solubility of the curcumin in water is obviously improved, the formed nanometer drug delivery system has sustained release characteristic, the carrier material is free of toxic and side effects, and the drug delivery nanoparticles are suitable for various drug delivery modes, such as oral administration and intravenous injection; moreover, the micro-channel nanoparticle method is high in full-process automation, high in controllability, short in granulating time, and beneficial to industrial scaling-up production.

Description

[0001] (1) Technical field [0002] The invention relates to the technical field of pharmaceutical polymer carrier preparation and pharmaceutical preparations, and mainly relates to a microchannel preparation method of polytricaprolactone-glyceric acid drug delivery nanoparticles. [0003] (2) Background technology [0004] Cancer is a disease that restricts social and economic development and seriously threatens human health. According to reports, 8.2 million people died of cancer in 2012, and malignant tumors have become one of the most important diseases affecting people's health. WHO predicts that by 2030, more than 13.1 million people worldwide will die of cancer. Traditional anticancer drugs are mostly lipophilic compounds with strong cytotoxicity, poor water solubility and instability. The bioavailability of drugs is low in vivo, and long-term, multiple or high-dose administration is required to achieve therapeutic purposes. It often shows serious side effects, allerg...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K31/12A61P35/00
CPCA61K9/0002A61K9/5153A61K9/5192A61K31/12
Inventor 郭钫元杨根生贠军贤洪伟勇
Owner ZHEJIANG UNIV OF TECH
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