PAMAM-Rapa-BODIPY system and production method and application thereof
A systematic and natural number technology, applied in the field of diabetic eye inflammation treatment, can solve the problems of untraceable dynamic changes of rapamycin and lack of molecular probe function, so as to increase the drug tracer function and inhibit diabetic retinopathy. , the effect of reducing toxicity
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[0044] The present application also provides the preparation method of the above-mentioned PAMAM-Rapa-BODIPY system, comprising the following steps:
[0045] The reaction of rapamycin, bodipyrrole, polyamide-amine dendrimers and OEG in an activator and a solvent yields a PAMAM-Rapa-BODIPY system.
[0046] In the process of preparing PAMAM-Rapa-BODIPY system, PAMAM, Rapa, BODIPY and OEG had nucleophilic addition reaction, thus the PAMAM-Rapa-BODIPY system was obtained. In the above preparation process, the activator is N-hydroxysuccinimide; the solvent is an organic solvent well known to those skilled in the art, and this application is not particularly limited. In this application, the The solvent is methanol. In order to make the reaction more fully, the preparation method of the PAMAM-Rapa-BODIPY system is specifically:
[0047] Dissolve rapamycin, boron dipyrrole and activator in an organic solvent, then activate in 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochlori...
Embodiment 1
[0052] Example 1 Preparation process of PAMAM-Rapa-BODIPY nano drug delivery system
[0053] Synthetic method: Dissolve rapamycin (Rapa), N-hydroxysuccinimide, and fluorobodipyrrole (BODIPY) in methanol solution, triethylene glycol molecule (OEG), add EDC·HCl in advance Activation and stirring for 1 h; then add polyamide-amine dendrimer (PAMAM) methanol / water mixed solution, PAMAM: N-hydroxysuccinimide: OEG: BODIPY: rapamycin molar ratio is 1:30 : 30: 1: 1; After three days of magnetic stirring at room temperature, place it in a dialysis bag and dialyze for two days; during the dialysis process, the deionized water needs to be replaced every two hours, and the water is removed by freeze-drying to obtain the product PAMAM-Rapa-BODIPY.
[0054] 1 H NMR nuclear magnetic analysis: Weigh 5 mg of PAMAM and PAMAM-Rapa-BODIPY samples with a precision balance, dissolve them in 0.5 mL of heavy water, and measure their characteristic groups with a nuclear magnetic resonance spectrometer...
Embodiment 2
[0055] Example 2 Safety and effectiveness evaluation of PAMAM-Rapa-BODIPY in cell model
[0056] 1) Cell source: human retinal pigment epithelial cell line (ARPE-19);
[0057] 2) Determination of the activity of human retinal pigment epithelial cells (CCK-8 method): collect ARPE-19 growing in the logarithmic phase, adjust the cell suspension to an appropriate concentration with DMEM-F12 containing 10% FBS, and inoculate 5000 cells in a 96-well plate after counting Each well, placed in an incubator to continue culturing overnight; 96 wells were added with different concentrations of PAMAM-Rapa (0, 10 -6 、10 -4 、10 -2 、10 -1 , 1, 10, 100, and 500 μM), the control group was sterile double-distilled water as a drug vehicle, and a zero-adjustment well was set at the same time. There were 3 duplicate wells in each group, and the culture continued for 24 hours; 1 hour before the end of the incubation, all the wells were aspirated. Add 110 μL of complete medium suspension containi...
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