Nanomaterials as drug carriers hold promise for the treatment of carcinomas,but integrating multiple functions into a single vector is difficult.In this study,we aim to develop efficie nt materials as vectors for co-d...Nanomaterials as drug carriers hold promise for the treatment of carcinomas,but integrating multiple functions into a single vector is difficult.In this study,we aim to develop efficie nt materials as vectors for co-delivery of microRNA-122(miR-122)and sorafenib(SRF).We successfully synthesized amphiphilic galactose-modified PEGylated poly(ami no-co-ester)(Gal-PEG-PPMS)copolymers consisted of hydrophilic Gal-PEG5 k chain segments and hydrophobic poly(ω-pentadecalactone-co-N-methyldiethyleneamine-co-sebacic acid)chain segments,which self-assembled to form cationic micelles at pH 5.2.The results showed that the micelles could encapsulate SRF and bind miR122 simultaneously,increase cellular uptake efficiency.Furthermore,the micelles showed favorable transfection efficiency in enhancing miR122 expression level,the migration and invasion ability of hepatocellular carcinoma(HCC)cells we re significantly inhibited after being tra nsfected with miR122-loaded micelles.Most importantly,the co-delivery micelles decreased cell activities of HepG2 cells,which was more effective than miR122 or SRF loaded micelles alone.Collectively,Gal-PEG-PPMS nanoparticles are promising multifunctional carriers for miR122 and SRF co-delivery system to treat HCC.展开更多
基金supported by the National Natural Science Foundation of China(No.51773231)the Natural Science Foundation of Guangdong Province(Nos.2016A030313315,2014A030312018)the Project of Key Laboratory of Sensing Technology and Biomedical Instruments of Guangdong Province(No.2011A060901013)。
文摘Nanomaterials as drug carriers hold promise for the treatment of carcinomas,but integrating multiple functions into a single vector is difficult.In this study,we aim to develop efficie nt materials as vectors for co-delivery of microRNA-122(miR-122)and sorafenib(SRF).We successfully synthesized amphiphilic galactose-modified PEGylated poly(ami no-co-ester)(Gal-PEG-PPMS)copolymers consisted of hydrophilic Gal-PEG5 k chain segments and hydrophobic poly(ω-pentadecalactone-co-N-methyldiethyleneamine-co-sebacic acid)chain segments,which self-assembled to form cationic micelles at pH 5.2.The results showed that the micelles could encapsulate SRF and bind miR122 simultaneously,increase cellular uptake efficiency.Furthermore,the micelles showed favorable transfection efficiency in enhancing miR122 expression level,the migration and invasion ability of hepatocellular carcinoma(HCC)cells we re significantly inhibited after being tra nsfected with miR122-loaded micelles.Most importantly,the co-delivery micelles decreased cell activities of HepG2 cells,which was more effective than miR122 or SRF loaded micelles alone.Collectively,Gal-PEG-PPMS nanoparticles are promising multifunctional carriers for miR122 and SRF co-delivery system to treat HCC.