A kind of drug compound and its preparation method and application
A drug compound and drug technology, applied in the medical field, can solve the problem of difficult release of functional EGCG, etc., and achieve the effect of improving the efficacy of small molecule drugs, good stability, and high drug loading
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Embodiment 1
[0076] Embodiment 1: the preparation method of drug-carrying system
[0077] see figure 1 , the preparation steps of the drug-loaded system are as follows:
[0078] 1. Use DMF (dimethylformamide) as the solvent of doxorubicin hydrochloride DOX-HCl, the concentration is 3mg / mL, add trifluoroethylamine dropwise, the molar ratio of doxorubicin hydrochloride and trifluoroethylamine is 1:10 , react overnight, remove hydrochloric acid, and prepare hydrophobic doxorubicin DMF solution (excess trifluoroethylamine will volatilize).
[0079] 2. Utilize the amino group of dopamine and the carboxyl group at both ends of PEG-COOH (molecular weight 0.5-200,000) to carry out amide reaction under the catalysis of EDC / NHS or DCC / NHS to generate PEG-dopamine, and further add the carboxyl group at the other end of PEG to PEG-dopamine / The amino group and the amino / carboxyl group of the fluorescent dye undergo amide reaction under the catalysis of EDC / NHS or DCC / NHS to prepare a fluorescent dy...
Embodiment 2
[0087] Example 2: Optimization and characterization of drug-loading system preparation
[0088] Using the method of Example 1, three different molar concentrations of ferric chloride 0.554mmol / L, 0.925mmol / L and 1.479mmol / L were used to prepare three kinds of drug-carrying systems, and named as DFEP-A, DFEP -B and DFEP-C, the results are as figure 2 As shown, the upper part is the photomicrograph, and the lower part is the diameter distribution.
[0089] From figure 2 It can be seen that the particle size increases with increasing concentration. The particle sizes of the three nano-drug loading systems are: DFEP-A: 77.4±13nm, DFEP-B: 126±24nm, DFEP-C: 296±19.7nm.
Embodiment 3
[0090] Example 3: Uptake of drug delivery system in tumor cells
[0091] Materials: Human glioma cells U87MG tumor cells were purchased from the Cell Bank of the Chinese Academy of Sciences.
[0092] DFEP-ANPs and DFEP-B NPs are from Example 2 of the present invention.
[0093] Test steps: put 2*10 5 U87MG cells were plated in a confocal 4-well plate at 37°C, 5% CO 2 , 90% humidity constant temperature incubator for overnight cultivation. Add 100 μL of 0.554mmol / L DFEP-A and 0.925mmol / L DFEP-B into 4-well plate U87MG cells respectively, incubate for 1, 4 and 8 hours, discard the culture medium, add 1mL PBS to wash, repeat 2-3 Once, fixed with 4% formaldehyde fixative solution for 20min, dripped DAPI dye solution to stain cell nuclei for 5min, covered with a cover glass, and observed under a laser confocal scanning microscope with a magnification of 200 times. It can be clearly seen that the DFEP-A and The green fluorescence and red fluorescence brightness of tumor cells U8...
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