Esterase response type gene drug loading system and preparation method thereof
A gene drug and drug-carrying system technology, applied in gene therapy, pharmaceutical formulations, drug combinations, etc., can solve the problems of inability to dissociate directly, release DNA inefficiently, etc., and achieve ERP effects, reduce inflammation, and easily enter cells Effect
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[0037] A preparation method of the esterase-responsive gene drug delivery system, comprising the following steps:
[0038] S1. Using diethylaminoethyl methacrylate as a raw material, polymerize under the catalysis of azobisisobutyronitrile to synthesize a polymer carrier with a molecular weight of about 27,000;
[0039] S2, dissolving the polymer carrier prepared in step S1 in tetrahydrofuran, quaternizing with methoxybenzyl chloride, and then demethylating with a catalyst solution;
[0040] S3, adding dexamethasone to the polymer prepared in step S2 by reacting with succinic anhydride and dicyclohexylcarbodiimide (DCC);
[0041] S4, the final product is connected with PEG and dicyclohexylcarbodisulfide to enhance its solubility in water.
[0042] The reaction equation is as follows:
[0043]
[0044] The step S1 is to pass diethylaminoethyl methacrylate through 100-200 mesh basic alumina chromatography to remove impurities, and react diethylaminoethyl methacrylate with a...
Embodiment 1
[0056] S1. Pass diethylaminoethyl methacrylate DEAEMA through a basic alumina (200 mesh) chromatographic column to remove impurities, take 2ml (0.01mol) in a centrifuge tube, add 0.0016g azobisisobutyronitrile AIBN (0.0001mol ), reacted in an oil bath at 60°C for 6 hours, and synthesized a polymer carrier polydiethylaminoethyl methacrylate (pDEAEMA) with a molecular weight of about 27,000;
[0057] S2. Dissolve the polymer polydiethylaminoethyl methacrylate (pDEAEMA) carrier material prepared in step S1 in 40ml tetrahydrofuran, put it into a round bottom flask and add 2.34g 4-methoxybenzyl chloride (0.015 mol), magnetically stirred at room temperature (25°C) for 24 hours, and the molar ratio of the two was 1:1.5.
[0058] Remove the solvent tetrahydrofuran by rotary evaporation, and the obtained 2-methylbutanoic acid 2-(diethyl(4-methoxybenzyl)-14-azayl)ethyl ester pDEAEMA-MP is dissolved in 25ml of anhydrous chloroform Add anhydrous aluminum chloride / anhydrous chloroform cat...
Embodiment 2
[0067] Step S1 and step S2 of this embodiment are the same as in embodiment 1, wherein the reaction time of step S1 is 6.5 hours, and the reaction time of step S2 is 23 hours.
[0068] Step S3 is that the product 2-methylbutanoic acid 2-(diethyl(4-hydroxybenzyl)-14-azepine) ethyl ester obtained in step S2 is dissolved in 25ml of chloroform, and 1.5g (0.015mol) of butyl The dianhydride and 3.708g (0.018mol) dicyclohexylcarbodiethylene (DCC) were reacted and refluxed at 60°C for 3.5 hours, and the product (pDEAEMA-MP-BA) was obtained by rotary steaming for 2 hours to remove chloroform, and the remaining The product was washed three times with ether and freeze-dried.
[0069] The molar ratio of S2 product, succinic anhydride, and dicyclohexylcarbodiethylene DCC is 1:1.5:1.8;
[0070] The product (pDEAEMA-MP-BA) was dissolved in 25ml of chloroform, 4.0g (0.01mol) of dexamethasone and 2.472g (0.012mol) of dicyclohexylcarbodiene (DCC) were added, and refluxed at 60°C for 3.5 hours....
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