Anthracycline antibiotic coupled nonlinear multi-block copolymer, and preparation method and application thereof
A technology of multi-block copolymers and anthracyclines, which is applied in the field of cyclic antibiotic coupling nonlinear multi-block copolymers, can solve the problems of low solubility, high toxicity, and application limitations, and achieve good therapeutic effects
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Embodiment 1
[0047] 1) A mixture of 25 g of 1,6-bis(p-carboxyphenoxy)hexane in 250 ml of acetic anhydride is refluxed to form acetylated 1,6-bis(p-carboxyphenoxy)hexane;
[0048] 2) 3.8 g of methoxypolyethylene glycol amine, 80 mg of compound A, 164 mg of dicyclohexylcarbodiimide and 9 mg of pyridine were mixed, stirred overnight at room temperature; then washed with ether and dried under vacuum to obtain a polymer ;
[0049] 3) Mix the products of step 1) and step 2) into a flask, melt and polymerize under reduced pressure at 170°C for 1 hour; dissolve the polymer in chloroform after cooling to room temperature, wash with petroleum ether and dry;
[0050] 4) Put doxorubicin and 800mg polymer from step 3 into 10ml dimethyl sulfoxide solution for 48 hours; then put it in an oven for 1 hour; ultrasonic for 20 minutes; put the homogenizer at minus 10-20 degrees at high speed Stir for 2 minutes, then put into 5% cholic acid solution and stir at 500 rpm for 2 hours; collect by centrifugation a...
Embodiment 2
[0052] 1) A mixture of 20 g of 1,6-bis(p-carboxyphenoxy)hexane in 500 ml of acetic anhydride is refluxed to form acetylated 1,6-bis(p-carboxyphenoxy)hexane;
[0053] 2) Mix 3 g of methoxypolyethylene glycol amine, 45 mg of compound A, 130 mg of dicyclohexylcarbodiimide and 5 mg of pyridine, stir at room temperature overnight; then wash with ether and dry under vacuum to obtain a polymer;
[0054] 3) Mix the products of step 1) and step 2) into a flask, melt and polymerize under reduced pressure at 180°C for 1 hour; dissolve the polymer in chloroform after cooling to room temperature, wash with petroleum ether and dry;
[0055] 4) Put 900 mg of pirarubicin and the polymer into a solution mixed with 5 ml of ethanol and 15 ml of dichloromethane; then put it in an oven for 24 hours; ultrasonically for 2 minutes; at minus 10-20 degrees, use a homogenizer Stir at high speed for 2 minutes, put the product into 3% cholic acid solution and stir at 400 rpm for 3 hours; collect by centri...
Embodiment 3
[0057] 1) A mixture of 28 g of 1,6-bis(p-carboxyphenoxy)hexane in 300 ml of acetic anhydride is refluxed to form acetylated 1,6-bis(p-carboxyphenoxy)hexane;
[0058] 2) 2 g of methoxypolyethylene glycol amine, 28 mg of compound A, 100 mg of dicyclohexylcarbodiimide and 3.5 mg of pyridine were mixed with 10 ml of chloroform, stirred at room temperature overnight; then washed with ether and dried under vacuum, get the polymer;
[0059] 3) Mix the products of step 1) and step 2) into a flask, melt and polymerize under reduced pressure at 175°C for 1 hour; dissolve the polymer in chloroform after cooling to room temperature, wash with petroleum ether and dry;
[0060] 4) Put arubicin and the 1000mg polymer of step 3 into a solution mixed with 13ml dichloromethane and 8ml dimethyl sulfoxide; then place in an oven to dry for 24 hours; ultrasonic for 7 minutes; Stir in a homogenizer at 30°C for 5 minutes at high speed, put the product in 2% cholic acid solution and stir at 500 rpm f...
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