Preparation and anti-tumor study of parthenolide targeting liposomes in vitro

YUAN Hui; YI Qikun; LI Shizhuang; LIANG Jiawen; ZHANG Yuting; CHEN Haoliang; YAN Xueying

doi:10.13506/j.cnki.jpr.2024.11.002

Abstract：Objective To prepare cyclic polypeptide cNGQ-loaded parthenolide liposomes(cNGQ-Lips@PTL),opti-mize the formulation and perform anti-tumor study in vitro.Methods Using encapsulation rate as index,Box-Behnken de-sign-effect surface method was used to optimize the prescription.The morphology,particle size,in vitro drug release behav-ior,serum stability and blood compatibility of cNGQ-Lips@PTL were detected by transmission electron microscopy,laser particle size analyzer,dynamic dialysis and visible spectrophotometry.Fluorescence microscopy,CCK-8 assay,apoptosis de-tection kit and flow cytometry were used to detect cell compatibility,cNGQ-Lips@PTL targeting efficiency and cytotoxicity of NSCLC cells.ResuIts cNGQ-Lips@PTL was successfully prepared with uniform particle size and spheroid shape,the average particle size was 128.3 nm,the Zeta potential was-26.7 mV,the encapsulation rate was 74.89%,and the drug load-ing was 12.08%.cNGQ-Lips@PTL In PBS with pH=5.5,the cumulative release in 24 h was 62.35%.In the cell uptake ex-periment,the fluorescence intensity and uptake rate of cNGQ-Lips@PTL group were significantly higher than those of TL-Lips group and free group.In the cytotoxicity test,the PTL concentration in cNGQ-Lips@PTL was 80 μmol·L-1,and the survival rate of A549 cells was 5.21%after incubation for 48 h.In the apoptosis experiment,98.74%of cells in cNGQ-Lips@PTL group were in the late stage of apoptosis.ConcIusion The cNGQ-Lips@PTL prepared in this study has obvious targeting effect and strong inhibitory effect on non-small cell lung cancer,which provides a valuable reference for the subse-quent development of nano preparations with targeting effect.