Characterization and antitumor activity of resveratrol liposome modified with polyethylene glycol
LI Yuxin, CHEN Lin, LI Juan*, ZHANG Zhiying, SUN Runguang*
(Research Institute of Biophysics and Biomedicine, School of Physics and Information Technology, Shaanxi Normal University, Xi′an 710119, Shaanxi, China)
Abstract:
The effectiveness of polyethylene glycol (PEG) modified resveratrol(RES) liposomes was evaluated in terms of stability, drug encapsulation and antitumor activity. The best mol ratios of phospholipid/cholesterol(8∶1) and phospholipid/resveratrol(3∶1) with the highest drug entrapment efficiency were determined by designed orthogonal experiments using the sonic hydration method. After modified with PEG-2000, the prepared samples can keep their size about 300 nm and maintain high entrapment efficiency even after 6 days of storage. Exemplified by human leukemia K562, the antitumor activity of PEG modified resveratrol liposomes (PEG-RES-LIP) was studied. Results showed that the optimal drug concentration and action time of PEG-RES-LIP on K562 was 120 μg/mL and 48 h. The highest inhibition ratio were 67.3%±2.3% and 85.9%±1.9% for RES-LIP and PEG-RES-LIP, respectively.The results demonstrated modifying RES liposomes with PEG is an effective way to improve the stability and drug entrapment efficiency of RES liposomes as well as enhance their antitumor activity, thus providing a new preparation method for RES liposome with better stability and higher antitumor activity.
KeyWords:
resveratrol; modifying; liposome; stability; antitumor activity
