A kind of ph dissociable lightly cross-linked polymer nanomaterial and its preparation method and application
A nano-material and lightly cross-linked technology, which can be used in drug combinations, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of weak stimulus response and slow drug release, and achieve the effect of high pH sensitivity
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Embodiment 1
[0033] In this embodiment, the preparation of pH-dissociable slightly cross-linked polymer nanometers is carried out according to the following steps:
[0034] 1. Under nitrogen, dissolve 16g of polyethylene glycol methacrylate and 0.3g of chain transfer agent 4-cyano-4-(thiobenzoyl)valeric acid in 25mL of dioxane and add to the reactor After stirring for 10 minutes, add 0.1 g of azobisisobutyronitrile into the reactor, and stir and react at 40-80°C for 8 hours under the protection of nitrogen. Put it into a vacuum drying oven and dry to obtain a linear nanometer polymer;
[0035] 2. Under nitrogen, add 6g of the intermediate prepared in step 1 and 20mL of dioxane into the reactor, stir for 10 minutes and then add 4g of diethylaminoethyl methacrylate and 0.1g of the original crosslinking agent into the reactor Ester and a small amount of azobisisobutyronitrile, stirred and reacted at 40-80°C for 16 hours under nitrogen protection, settled with n-hexane for several times after...
Embodiment 2
[0042] In this embodiment, the preparation of pH-dissociable slightly cross-linked polymer nanometers is carried out according to the following steps:
[0043] 1. Dissolve 16g of polyethylene glycol methacrylate and 0.3g of chain transfer agent 4-cyano-4-(thiobenzoyl)valeric acid in 25mL of dioxane and add it to the reactor, and stir for 10 minutes Then add 0.1g of azobisisobutyronitrile into the reactor, stir and react at 40-80°C for 8 hours under nitrogen protection, settle with n-hexane several times after the reaction, and put the product collected by precipitation into a vacuum drying oven Dry in medium to obtain linear nanometer polymer;
[0044] 2. Add 6g of the intermediate prepared in step 1 and 20mL of dioxane into the reactor, stir for 10 minutes and then add 4g of diethylaminoethyl methacrylate, 0.1g of crosslinking agent orthoester and A small amount of azobisisobutyronitrile was stirred and reacted at 40-80°C for 16 hours under the protection of nitrogen. After ...
Embodiment 3
[0049] Dissolve 50 mg of slightly cross-linked polymer nanometer and 10 mg of emodin obtained in Example 1 in 10 mL of tetrahydrofuran, then slowly drip 5 mL of deionized water into it with a syringe pump, stir at room temperature for 0.5 h, and pure water The medium was dialyzed for 12 hours, and the water was changed 5 times during the dialyzing process, and finally the polymer nanoparticles loaded with emodin were obtained by freeze-drying.
[0050] Drug loading (DLC) and encapsulation efficiency (DLE) of emodin at 437nm using UV-visible spectroscopy:
[0051] DLC=(the mass of the drug in the micelle / the total mass of the micelle)×100%
[0052] DLE=(the quality of drug in micelles / the quality of input drug)×100%
[0053] The drug-loaded polymer nanoparticles prepared in Example 3 had a drug-loading capacity of 7% and an encapsulation efficiency of 35.2%.
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Abstract
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