Preparation and characterization of multi-functional targeting nano-carrier based on pH-redox tumor microenvironment / 中国药科大学学报

In order to construct a novel multifunctional targeting nano-carrier based on pH-redox characteristics of tumor microenvironment,ketone bonds and disulfide bonds were bonded to the oligomeric hyaluronic acid (oHA) being sensitive to pH and the reduction environment.The chemical structure of oligomeric hyaluronic acid-8-mercaptomenthone 1,2-glycerolketal (oHMST) was characterized by 1H NMR,IR and ESI-MS.Curcuminloaded micelles were prepared by dialysis.The single factor investigation was carried out on the dosage form.Some properties,including particle size zeta potential,the morphology of micelles,and pH-sensitivity were studied.The materials were synthesized successfully.The micelles were spheric with a diameter of about 100 nm.The Zeta potential of the micelles was-(21.97 ± 1.08) mV.The in vitro test showed that oHMST carriers have good pH-sensitivity and redox-sensitivity.

Biocompatibility and brain-targeting ability of nano-micelles on glioma cells / 吉林大学学报(医学版)

Objective To investigate the biocompatibility and safety of nanoscale brain-targeting-carrier micelles [poly (ethylene)-b-poly (lactic acid)/OX26 conjugate micells (copolymer/OX26)],and to explore its possibility as brain-targeted-drug carrier for brain glioma.Methods The C6 glioma cells were cultured in vitro and divided into experimental groups with different concentrations (10, 20, 40, 80 mg · L-1 )of nano micelle, and the medium without micelle was used as control group.The inhibitory effect of nano-micelles on the rat brain glioma C6 cells was examined by Trypan blue cell counting assay.Flow cytometry (FCM)was used to detect the changes of apoptosis and cell cycle of C6 cells,and confocal laser scanning microscope (CLSM)was performed to analyze the distribution of copolymer/OX26 into C6 cells. Results The results of Trypan blue cell counting assay showed copolymer/OX26 didn’t affect the growth of C6 cells,and there were no significant differences in the number of C6 cells between control group and expreimental groups (P >0.05).The results of FCM showed that the cell cycle and and the apoptotic rates of C6 cells had no changes compared with control group (P > 0.05).The results of CLSM showed that the fluorescence intensities in experimental groups were higher than those in blank micelles group and blank control group (P < 0.05 ), and they were increased in dose- and time-dependent manner (P <0.05).Conclusion Copolymer/OX26 has no effect on the growth and apoptosis of glioma cells.By bonding OX26,copolymer/OX26 can significantly increase the intake of C6 cells on the nano micelles.

Tumor-targeting carrier equipped with cell-penetrating peptides / 中国肿瘤生物治疗杂志

Equipping tumor-targeting carrier with cell-penetrating peptide with high transduction efficacy has become a trend. According to the fusion modes and tumor-targeting mechanisms, cell-penetrating peptides can be divided into five categories: first, self-targeting cell-penetrating peptides; second, fusion carriers made of targeting ligands and cell-penetrating peptides; third, cell-penetrating peptide-modified nano-carrier; fourth, tumor-microenvironment-targeting cell-penetrating peptides; fifth, other special cell-penetrating peptides. Fusion carriers, which can not be effectively released into the cytoplasm after transducted into target cells, can be further modified to increase their efficacy. In all, cell-penetrating peptide introduced into tumor-targeting carrier should provide a new era for anti-tumor pharmacy research and cancer therapy.