A kind of multifunctional targeting molecule and its use
A molecularly targeted, multifunctional technology, applied in the field of pharmacy, can solve problems such as low permeability and damage
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Embodiment 1
[0044] Preparation of RGD-pHA, RGD-pHA-FAM, RGD-pHA-drug, RGD-pHA-PEG-DSPE
[0045] 1) Synthesis and characterization of RGD cyclic peptide-pHA (c(RGDyK)-pHA)
[0046] Using the Fmoc solid-phase synthesis method, c(RGDyK) polypeptide and Cys(Trt)-Acp-4-tert-Butoxybenzoic acid were prepared respectively, and the two were condensed to obtain c(RGDyK)-pHA;
[0047] The synthesis process of c(RGDyK) polypeptide is as follows: Fmoc-Gly-CTC resin was deprotected with 20% piperidine in N,N-dimethylformamide (DMF) solution for 15 minutes twice, and the Fmoc-protected amino acid was dissolved in 0.5 In HBTU and HOBt (solvent is DMF) of M, add DIEA and add to the resin, react at room temperature for 45 minutes; after the reaction, the resin is washed with DMF, 20% piperidine removes Fmoc protection, and the same reaction is carried out in sequence according to the amino acid sequence; sequence reaction After completion, 1% trifluoroacetic acid (TFA) cuts the polypeptide from the resin ...
Embodiment 2c
[0061] In vitro cell targeting verification of embodiment 2c (RGDyK)-pHA
[0062] 1) In vitro targeting of c(RGDyK)-pHA-FAM
[0063] In vitro targeting of glioma cell U87: take the monolayer cultured brain glioma cells (U87 cells) in the logarithmic growth phase, digest the monolayer culture cells with 0.25% trypsin, and use 10% fetal bovine The DMEM culture solution of serum was prepared into a single cell suspension, and 1×10 5 Cells were inoculated in a 12-well culture plate with a volume of 1 mL per well, and the culture plate was moved into a carbon dioxide incubator at 37°C and 5% CO 2 and saturated humidity conditions, after 24 hours, prepare c(RGDyK)-pHA-FAM at a concentration of 5 μM with DMEM culture solution containing 10% fetal bovine serum, and use FAM, c(RGDyK)-FAM and pHA-FAM The solution is used as a control, added to the cell culture plate, incubated at 37°C for 4 hours, discarded the supernatant, washed three times with PBS solution, fixed the cells with fo...
Embodiment 3c
[0065] In vitro targeting verification of embodiment 3c (RGDyK)-pHA-LS
[0066] 1) Preparation of c(RGDyK)-pHA-LS / FAM
[0067] Liposome membrane material prescription is HSPC / Chol / mPEG 2000 -DSPE / c(RGDyK)-pHA-PEG 3400 -DSPE (52:43:4:1, molar ratio), weigh the above membrane material and dissolve it in chloroform, remove the organic solvent by rotary evaporation under reduced pressure, and obtain a uniform lipid film, dry it in vacuum for 24 hours; add 5-FAM aqueous solution to hydrate , shaken in a water bath at 60°C for 2 hours to obtain a liposome suspension; in a water bath at 60°C, use a high-pressure homogenizer (if the liposome volume is less than 10mL, use a micro-extruder instead) to squeeze the liposomes sequentially Press through 400, 200, 100 and 50nm nuclear pore membranes to reduce the particle size; then use normal saline as the eluent to separate and remove unencapsulated drugs through a Sephadex G-50 column to obtain FAM-loaded Liposomes;
[0068] 2) In vit...
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