Drug nano preparation and preparation method thereof
A nano-preparation and drug technology, which is applied in the field of preparation of nano-drug-loaded preparations, can solve the problems of high expression level of transcription factor HIF1alpha in tumor cells, impermeability to tumor tissue, etc., to achieve increased penetration, increased toxicity, and simple preparation process Effect
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Embodiment 1
[0052] 1. Preparation of 20% PEG2K-AZO-PAMAM (20% PEG grafting rate, PEG molecular weight 2000) nanocarrier
[0053] 1) Take 5mg of AZO, ultrasonically dissolve it in 3ml of pyridine, add 4.37mg of EDC·HCl, 2.56mg of NHS and 0.23mg of 4-DMAP, adjust the pH of the solution to 5 with 1mol / L HCl, and stir at room temperature for 2 hours to activate the carboxyl group of AZO .
[0054] 2) Dissolve 37mg of mPEG-NH2 (MW=2000) in 1ml of pyridine; slowly add the mPEG pyridine solution into the AZO solution under magnetic stirring, and add 5 μl of triethylamine dropwise; stir overnight at room temperature.
[0055] 3) Remove the pyridine solution by vacuum rotary evaporation at 50°C to obtain an orange-yellow film product. Add 10ml of pure water to redissolve, centrifuge at 3000rpm for 5min to remove free AZO precipitate, and obtain mPEG-AZO aqueous solution. Add 4.37mg EDC·HCl, 2.56mg NHS, adjust the pH of the solution to 5 with 1mol / L HCl, stir at room temperature for 2 hours, and ...
Embodiment 2
[0065] This embodiment removes mPEG-NH 2 The molecular weight of PEG5K-AZO-PAMAM is 5000, and the dosage is 92.5 mg, and other steps are the same as in Example 1 to prepare 20% PEG5K-AZO-PAMAM (20% PEG grafting ratio, PEG molecular weight 5000).
Embodiment 3
[0067] In this example, except that the dosage of 20.5% PAMAM (G5.0) was 200 μl, other steps were the same as in Example 1 to prepare 10% PEG2K-AZO-PAMAM (10% PEG grafting ratio, PEG molecular weight 2000).
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