Ph-disintegrable light-crosslinked polymer nano-material and preparation method and application thereof
A nanomaterial, mildly cross-linked technology, applied in drug combinations, pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve the problems of weak stimuli responsiveness 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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