Tumor diagnosis and treatment medicine and preparation method and application thereof
A tumor and drug technology, applied in the field of tumor diagnosis and treatment drugs and their preparation, can solve the problems of short circulation time in the body, poor tumor specificity, poor biocompatibility, etc., and achieve the effect of promoting the integration of diagnosis and treatment and strong fluorescence performance
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[0055] The present application also provides a method for preparing the above-mentioned tumor diagnosis and treatment drug, comprising the following steps:
[0056] Step 100: Dissolving indocyanine green (ICG) in solvent, adding N-hydroxysuccinimide (NHS) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride Salt (EDC), after the reaction, ICG-NHS is obtained;
[0057] Step 200: react ICG-NHS and iRGD cyclic peptide to obtain ICG-iRGD;
[0058] Step 300: Mix ICG-iRGD with albumin (HSA) and react to obtain a tumor diagnosis and treatment drug (HSA-ICG-iRGD).
[0059] In the embodiment of the present application, in step 100, the reaction of ICG with EDC and NHS can activate the carboxyl group of ICG, which is beneficial to the reaction of the carboxyl group of ICG with the amino group of iRGD cyclic peptide. In the embodiment of the present application, the solvent for dissolving indocyanine green includes one or more of methanol, ethanol, dimethylformamide, and dim...
Embodiment 1
[0074] A preparation method of a tumor diagnosis and treatment drug, comprising the steps of:
[0075] Preparation of ICG-NHS: 2mg of ICG, 1mg of NHS and 2mg of EDC were dissolved in 2mL of anhydrous DMSO under the protection of nitrogen, stirred and reacted at 20°C for 30h, then 20mL of cold acetone was added, the solution produced a large amount of precipitation, and the precipitate was filtered to obtain Solid, the solid was washed three times with cold acetone, and vacuum-dried to obtain ICG-NHS;
[0076] Preparation of ICG-iRGD: Dissolve 2 mg of ICG-NHS in 2 mL of anhydrous DMSO, add 2 mg of iRGD cyclic peptide, and react at 30° C. for 12 h to prepare ICG-iRGD. The solution was dialyzed in pure water for 72 hours with a 500 molecular cut-off dialysis bag, and then the solution was freeze-dried to obtain ICG-iRGD.
[0077] Preparation of HSA-ICG-iRGD: Mix 2 mg ICG-iRGD and 80 mg HSA in PBS solution to obtain HSA-ICG-iRGD.
Embodiment 2
[0079] 1) Preparation of ICG-NHS: 3 mg of ICG, 2 mg of NHS and 5 mg of EDC were dissolved in 5 mL of anhydrous DMSO under the protection of nitrogen, stirred and reacted at 20 °C for 30 h, and then excess cold acetone was added, the solution produced a large amount of precipitation, and the The precipitate was filtered to obtain a solid, and the solid was washed three times with cold acetone, and dried in vacuum to obtain ICG-NHS;
[0080] 2) Preparation of ICG-iRGD: Dissolve 3 mg of ICG-NHS in 5 mL of anhydrous DMSO, add 3 mg of iRGD cyclic peptide, and react at 30° C. for 12 h to prepare ICG-iRGD. The solution was dialyzed in pure water for 72 hours with a dialysis bag with a molecular cut-off of 1000, and then freeze-dried to obtain ICG-iRGD.
[0081] 3) Preparation of HSA-ICG-iRGD: Mix 3 mg ICG-iRGD and 120 mg HSA in PBS solution to obtain HSA-ICG-iRGD.
[0082] 4) Preparation of Gd-DTPA-HSA-ICG-iRGD: Dissolve 3mg HSA-ICG-iRGD in 2mL PBS, add 1.4mg DTPA-NHS to react for 2...
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