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Method for preparing temperature-sensitive stereocomplex polylactic acid copolymer drug-loaded micell

A compound polylactic acid, temperature-responsive technology, applied in the fields of polymer materials and biomedical engineering, can solve problems such as side effects, and achieve the effect of improving sustained release effect and drug loading rate.

Inactive Publication Date: 2015-11-11
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the process of tumor treatment, conventional chemotherapy has serious side effects on normal tissues and organs of the human body. Therefore, research on new drug carriers to reduce the side effects of chemotherapy and make the drug release controllable has always been a research hotspot.
So far, there is no report on the preparation of nano drug-loaded micelles with a temperature-responsive polymer as the hydrophilic end and stereocomplexed polylactic acid as the hydrophobic end.

Method used

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  • Method for preparing temperature-sensitive stereocomplex polylactic acid copolymer drug-loaded micell
  • Method for preparing temperature-sensitive stereocomplex polylactic acid copolymer drug-loaded micell

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023]Take 0.12g of isopropanol and 5.76g of L-lactide, put them in a flask, add 0.016g of stannous octoate, protect with argon, react at 130°C for 24 hours, dissolve the product with dichloromethane, and precipitate in ether 2~3 times, filter, and vacuum dry the filter cake to obtain PLLA; take 0.12g of isopropanol and 5.76g of D-lactide, put them in a flask, add 0.016g of stannous octoate, protect with argon, at 130°C React for 24 hours, dissolve the product with dichloromethane, precipitate in ether 2 to 3 times, filter, and dry the filter cake in vacuum to obtain PDLA; take 4.8g PLLA or PDLA and dissolve it in 30mL dry chloroform, under the protection of argon, to 0.0971 g of triethylamine was added to the above solution. The system was cooled to 0°C with an ice bath under constant stirring, and 0.166 g of 2-bromoisobutyryl bromide dissolved in 20 mL of dry chloroform was added dropwise to the above system within 30 min. The whole reaction system was stirred at room tempe...

Embodiment 2

[0025] Take 0.12g of isopropanol and 11.52g of L-lactide, put them in a flask, add 0.032g of stannous octoate, protect with argon, react at 130°C for 24 hours, dissolve the product with dichloromethane, and precipitate in ether 2~3 times, filter, and vacuum-dry the filter cake to obtain PLLA; take 0.12g of isopropanol and 11.52g of D-lactide, put them in a flask, add 0.032g of stannous octoate, protect with argon, at 130°C React for 24 hours, dissolve the product with dichloromethane, precipitate in ether 2 to 3 times, filter, and dry the filter cake in vacuum to obtain PDLA; take 4.8g PLLA or PDLA and dissolve it in 30mL dry chloroform, under the protection of argon, to 0.0971 g of triethylamine was added to the above solution. The system was cooled to 0°C with an ice bath under constant stirring, and 0.083 g of 2-bromoisobutyryl bromide dissolved in 20 mL of dry chloroform was added dropwise to the above system within 30 min. The whole reaction system was stirred at room te...

Embodiment 3

[0027] Take 0.17g of isopropanol and 8.06g of L-lactide, put them in a flask, add 0.022g of stannous octoate, protect with argon, react at 130°C for 24 hours, dissolve the product with dichloromethane, and precipitate in ether 2~3 times, filter, and vacuum dry the filter cake to obtain PLLA; take 0.17g of isopropanol and 8.06g of D-lactide, put them in a flask, add 0.022g of stannous octoate, protect with argon, at 130°C React for 24 hours, dissolve the product with dichloromethane, precipitate in ether for 2 to 3 times, filter, and dry the filter cake in vacuum to obtain PDLA; dissolve 6.72g PLLA or PDLA in 30mL dry chloroform, and pour to Add 0.1360g triethylamine in the above solution. The system was cooled to 0°C with an ice bath under constant stirring, and 0.232 g of 2-bromoisobutyryl bromide dissolved in 25 mL of dry chloroform was added dropwise to the above system within 30 min. The whole reaction system was stirred at room temperature under the protection of argon f...

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Abstract

The invention belongs to the fields of high polymer materials and biomedical engineering, and particularly relates to a method for preparing a temperature-sensitive stereocomplex polylactic acid copolymer drug-loaded micelle. The method includes the specific steps that poly L polylactic acid and poly D polylactic acid are bromized, and a temperature-sensitive polylactic acid segmented copolymer is obtained through atom transfer radical polymerization; then stereocomplex is performed, drugs are loaded, and thus a drug-loaded micelle which uses hydrophobic stereocomplex polylactic acid as the core and a hydrophilic chain temperature-sensitive polymer as the shell layer is formed. The nano drug-loaded micelle has the advantages of being compact in core structure, low in drug release speed, responsive to temperatures and the like; the stability of drug carriers can be improved easily, and drug release can be effectively controlled.

Description

technical field [0001] The invention belongs to the fields of polymer materials and biomedical engineering, and in particular relates to a preparation method of temperature-responsive stereocomplex polylactic acid copolymer drug-loaded micelles. Background technique [0002] The polymer drug carrier is to use the polymer as the drug carrier. After combining with the drug molecule, it is placed in the environment where it will be released, and the drug can be released slowly through diffusion and other methods, so as to achieve the purpose of safe and effective treatment of diseases. Biodegradable polymers have more advantages because they can be degraded in vivo and can be excreted from the body or consumed by normal metabolism in the body. Among them, polylactic acid (PLA) has good biocompatibility and biodegradability. Its degradation products can participate in the normal metabolism of the human body, and its performance can also be adjusted by copolymerization with other...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K45/00C08F293/00C08G63/91C08G63/08
Inventor 任杰周科瑜李建波
Owner TONGJI UNIV
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