Preparation and in vitro evaluation of hydroxycamptothecin loaded transferrin modified stealth niosomes
The aim was to prepare hydroxycamptothecin (HCPT) loaded transferrin modified stealth niosomes (Tf-PEG-NS) and to evaluate the physicochemical characteristics, cytotoxicity and cell uptake of Tf-PEG-NS. The amphiphilic copolymer of Poly (methoxy-polyethyleneglycol cyanoacrylate-con-hexadecyl cyanoacrylate) (PEG-PHDCA) acted as surface modified materials was synthesized and characterized. By coupling oxidized transferrin to PEG, Tf-PEG-NS were prepared by thin-film hydration-sonication dispersion method with particle size of (121.2±9.8)nm and encapsulation efficiency of (93.00±0.61)％. In vitro drug release of Tf-PEG-NS was up to 90％ within 4B. In vitro cytotoxicity of Tf-PEG-NS was about 3 and 1.5 times that of HCPT injection and PEG-NS on KB cells, respectively. The relative uptake into nucleis of Tf-PEG-NS was significantly higher than other formulations, which was 79, 5.9 and 1.7 times that of HCPT injection, NS and PEG-NS respectively after 12h incubation. The in vitro results suggest that Tf conjugated PEG-coated niosomes could be a potentially effective HCPT delivery carrier for tumor therapy.
hydroxycamptothecin niosomes transferrin cytotoxicity cell uptake
HONG Ming-huang PEI Yuan-ying
School of Pharmacy, Fudan University, Shanghai 200032, China
国际会议
上海
英文
75-83
2007-10-19（万方平台首次上网日期，不代表论文的发表时间）