PLK1 inhibitor-loaded polymer vesicle drug and preparation method and application thereof
A technology of polymers and inhibitors, applied in the field of medicine, can solve the problem of limited tumor accumulation
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Embodiment 1
[0030] PEG-P(TMC-DTC)-PAsp (Mn = 5.0-(15.0-2.0)-1.29 kg / mol) was synthesized according to existing reports, such as CN2019104726138 (reduction-sensitive reversible cross-linked polymer capsule with asymmetric membrane structure Bubbles and their application in the preparation of drugs for the treatment of liver cancer) Example 1 PEG-P (TMC-DTC)-KD10; N-hydroxysuccinimide functionalized block polymer NHS-PEG-P (TMC-DTC ) (Mn=7.5-(15.0-2.0) kg / mol, Mw / Mn=1.1) was synthesized according to existing reports, such as the preparation example of CN2020105763476 (carbonate polymer vesicles loaded with small molecule drugs and its preparation method and application) NHS-PEG-P (TMC-DTC).
[0031] A3-PEG-P (TMC-DTC) was obtained by the amidation reaction of A3 polypeptide (cDGWGPNc) and the above-mentioned NHS-PEG-P (TMC-DTC). Briefly, NHS-PEG-(TMC-DTC) (200 mg, 6.2 μmol) was dissolved in 2 mL DMF, and it was added dropwise to A3 polypeptide (13.6 mg, 12.4 μmol) and triethylamine under n...
Embodiment 2
[0034] The preparation of embodiment two Ps-Vol and A3-Ps-Vol
[0035] The DMSO solution of PEG-P(TMC-DTC)-PAsp and A3-PEG-P(TMC-DTC) with a concentration of 10 mg / mL was mixed with a mass ratio of 80:20, and 100 mL of DMSO solution with Vol ( 20 mg / mL, 5 mL), then add 0.9 mL of HEPES (5 mM, pH 6.8) buffer solution, stir at 200 rpm for 5 minutes, turn to a shaker (100 rpm, 35°C) and incubate for 6 h, then in Dialyzed in HEPES (5 mM, pH 7.4) (dialysis bag molecular weight cut-off is 7000 Da) to obtain Vol-loaded vesicles 20A3-Ps-Vol with a surface density of 20% of A3. Unless otherwise noted, the A3-Ps-Vol mentioned in subsequent experiments are Vol-loaded vesicles with a surface density of 20%. The particle size, Zeta potential, Vol drug loading (DLC) and encapsulation efficiency (DLE) of the vesicles were determined by DLS, electrophoresis and ultraviolet absorption, respectively.
[0036] By further adjusting the mass ratio of PEG-P(TMC-DTC)-PAsp and A3-PEG-P(TMC-DTC), suc...
Embodiment 3
[0046] Example 3 Anti-tumor activity and endocytosis research at the cell level
[0047] The targeting of A3-Ps-Vol to SKOV3 cells was studied by flow cytometry and confocal laser microscopy (CLSM), using FITC-labeled Vol (Vol-FITC) as a fluorescent probe. Briefly, SKOV3 cells were plated into 6-well plates, 300,000 per well, and after overnight attachment, A3-Ps-Vol, Ps-Vol and free Vol-FITC loaded with Vol-FITC at different A3 densities were added and incubated for 4 hours (Vol-FITC at a concentration of 200 nM). Afterwards, they were washed with PBS, trypsinized, centrifuged (1000 rpm, 3 min), and redispersed in PBS for flow cytometry measurements. To demonstrate the specificity of A3-Ps-Vol targeting, DU145 cells were used as a negative control.
[0048] In CLSM experiments, SKOV3 cells were plated into 12-well plates (including small discs), 50,000 per well, and after overnight attachment, Ps-Vol-FITC or A3-Ps-Vol-FITC (Vol concentration was 200 nM ) for 4 h. Then sta...
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