RESUMO
Objective To evaluate the targeting and inhibitory effects of the targeted artemether liposomes modified with APGA- PEG2000-DSPE conjugate in vitro. Methods APGA was used as targeted molecular, and the new functional material APGA- PEG2000-DSPE conjugate was synthesized and confirmed by using MALDI-TOF-MS. A kind of targeted artemether liposomes was developed by modifying APGA-PEG2000-DSPE using film dispersed method. Co-culture model of BBB-glioma C6 tumor spheroids was developed, and it was used to study the transporting efficiency across the BBB and the penetration ability of the liposomes into glioma C6 tumor spheroids viewed by a confocal laser scanning microscope. Flow cytometry was used to evaluate the targeting properties of the preparations to C6 glioma cells. SRB method was used to study the inhibitory effect of targeted liposomes on the growth of C6 glioma cells. Results The APGA-PEG2000-DSPE conjugate was confirmed by using MALDI-TOF-MS, and its average mass was 3 150. The co-culture model showed that the targeted liposomes can better transport across the BBB and then penetrate into the glioma C6 tumor spheroids. To C6 glioma cells, the IC50 of the targeted artemether liposomes, artemether liposomes and free artemether were 45, 82, and 95 μmol/L, separately. Conclusion The targeted artemether liposomes could effectively transport across the BBB and penetrate into the glioma C6 tumor spheroids. The targeted artemether liposomes had stronger inhibitory effect on brain glioma cells in vitro.