Drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy and preparation method thereof
A technology of drug-loaded microspheres, radiotherapy and chemotherapy, applied in the field of nanomaterials, can solve the problems of limited anti-tumor effect of drugs, poor histocompatibility, large drug dosage, etc., to improve drug utilization rate and good histocompatibility. , the effect of improving the release
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[0074] refer to figure 1 , which shows a flow chart of an embodiment of a method for preparing drug-loaded microspheres with a synergistic sensitization effect of tumor radiotherapy and chemotherapy of the present invention, which may specifically include:
[0075] Step S41, polyacrylic acid PAA and polyethylene glycol PEG aminated at both ends are subjected to amide reaction under the action of the first activator to obtain a block polymer of PAA-PEG;
[0076] Step S42, the block polymer of PAA-PEG and 1-hydroxyethyl-2-methyl-5-nitroimidazole MN are subjected to an esterification reaction under the action of a second activator to obtain MN-PAA - PEG polymer microspheres;
[0077] In step S43, the MN-PAA-PEG polymer microspheres and doxorubicin DOX are self-assembled to obtain doxorubicin-loaded DOX / MN-PAA-PEG microspheres.
[0078] The drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy provided by the embodiment of the pres...
Embodiment 1
[0093] The drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy of the present invention are composed of polyacrylic acid PAA, polyethylene glycol PEG aminated at both ends, 1-hydroxyethyl-2-methyl-5-nitroimidazole MN And doxorubicin DOX is used as a raw material, and is prepared through amide reaction, esterification reaction and self-assembly.
[0094] This example discloses the preparation method of the drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy of the present invention, specifically:
[0095] Step 1, polyacrylic acid PAA and polyethylene glycol PEG aminated at both ends, under the effect of the first activator, carry out amide reaction, obtain the block polymer of PAA-PEG:
[0096] Dissolve 300mg of polyacrylic acid PAA (number average molecular weight 2000) in 30mL of 2-(N-morpholino)-ethanesulfonic acid buffer (MES, 10Mm, pH 6.0) to form a homogeneous polyacrylic a...
Embodiment 2
[0111] Step 1. Dissolve 300mg of polyacrylic acid (PAA, number average molecular weight 2000) in 30mL of 2-(N-morpholino)-ethanesulfonic acid buffer (MES, 10Mm, pH 6.0) to form a polyacrylic acid solution , 57.5 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and 34.5 mg of N-hydroxysuccinimide (NHS) were added to the PAA solution to obtain The mixture A was activated by stirring at room temperature for 10 min. Then use triethylamine (TEA) to adjust the pH value of the mixed solution to 7.2 to form the activated polyacrylic acid mixed solution B; Polyethylene glycol (PEG, number average molecular weight 7000), stirred at room temperature for 16 hours to obtain a mixed solution containing PAA-PEG, dialyzed to remove impurities, and dried to obtain a PAA-PEG block polymer;
[0112] Step 2. Dissolve 300 mg of PAA-PEG in 15 mL of dimethyl sulfoxide, then add 123 mg of EDC and 76 mg of 4-dimethylaminopyridine (DMAP) in sequence, and stir for 2 hours in the ...
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