Folate-mediated targeted polymeric micelle
A technology of polymer glue and folic acid, which is applied in the direction of drug combination, drug delivery, and medical preparations of non-active ingredients, etc. It can solve the problems of phagocytosis of drug-loaded micelles, reduce the effect of targeting tumor cells, and reduce drug efficacy.
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Embodiment 1
[0026] Embodiment 1 prepares carrier material FA-PEG-DSPE
[0027] Preparation of Folate-PEG-NH 2
[0028] Take 30.9mg (0.15mmol) DCC dissolved in 5ml dimethylsulfoxide (DMSO), add 300mgNH 2 -PEG-NH 2 , 66.2mg Folate, 10μl pyridine, stirred at 25°C for 24h, added 10ml of distilled water to terminate the reaction, centrifuged, took the supernatant, dialyzed with distilled water, and lyophilized. Use DEAE Sepharose FF ion-exchange column and Sephadex G-15 column in combination with AKTA explorer rapid purification system for separation and purification, and lyophilize to obtain yellow Folate-PEG-NH 2 Solid 154mg.
[0029] Preparation of Folate-PEG-SUC
[0030] Folate-PEG-NH 2 80.9mg was dissolved in 1ml DMF, SUC 23.8mg was dissolved in 1ml DMF, mixed, reacted at 50°C, and detected by spotting. After reacting for 4 hours, add 2ml of distilled water to stop the reaction, use SephadexG-15 column combined with AKTA explorer rapid purification system for separation and purific...
Embodiment 2
[0035] Embodiment 2 prepares carrier material MPEG-DSPE
[0036] Preparation of MeO-PEG-SUC
[0037] MeO-PEG-NH 2200mg was dissolved in 2ml DMF, SUC 80mg was dissolved in 1ml DMF, mixed, reacted at 50°C, and detected by spotting. After 4 hours of reaction, 2ml of distilled water was added to terminate the reaction, separated and purified by Sephadex G-15 column combined with AKTA explorer rapid purification system, and lyophilized to obtain 159.9 mg of white MeO-PEG-SUC solid.
[0038] Preparation of MeO-PEG-DSPE
[0039] Dissolve 90 mg of MeO-PEG-SUC in 1 ml of chloroform, 8 mg of DCC in 1 ml of chloroform, mix, and dissolve 254.4 mg of DSPE in 4 ml of chloroform, add to the above solution, react at 50 ° C, and detect the reaction by spotting. After 5 hours, the reaction was complete, and the chloroform was removed by rotary evaporation, and dried in vacuum overnight. Then add 50ml of ethanol, stir for 10min, centrifuge at 7500r / min for 20min, take the supernatant, repeat...
Embodiment 3
[0042] Example 3 Carrier Material Cytotoxicity Detection
[0043] Cervical cancer cells HeLa in the logarithmic growth phase were treated with 7.5×10 3 cells / well, inoculated in 96-well plate, 24h later, given 0.2-20uM micellar solution prepared by micelle carrier material FA-PEG-DSPE and MPEG-DSPE respectively, and incubated in 37°C incubator for 48h, Add 20 μl of 5 mg / ml MTT solution, incubate at 37°C for 4 hours, replace the culture solution with 200 μl DMSO, shake for 10 minutes, and measure the absorbance at 490 nm with a microplate reader.
[0044] The results showed that within the concentration range of 0.2-20uM, the cell survival rate of FA-PEG-DSPE was 93.47±3.402%-73.20±2.043%, and the cell survival rate of MPEG-DSPE was 96.21±7.261%-84.18±1.697%. The carrier material itself is less toxic to cells and has less influence on the next drug sensitivity test ( figure 2 ).
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