ZHANG Lan1,2,3, LI Yan-hui1,2,3, WANG Cai-xia1,2,3, HAO Xiao-fang4, XIU Xian1,2,3, WEI Na1,2,3, LI Chun-lei1,2,3*
1 Hebei Pharmaceutical Technology and Engineering Research Center,Shijiazhuang 050035,China; 2 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co ,Ltd,Shijiazhuang 050035,China; 3 State Key Lab of Novel Pharmaceutical Preparations and Excipients,Shijiazhuang 050035,China; 4 Jiangsu Institute for Medical Equipment Testing,Nanjing 210013,China
Abstract��
Objective To prepare the paclitaxel liposomes and evaluate its physicochemical property,toxicity and pharmacodynamics. METHODS SPC,mPEG2000-DSPE and paclitaxel were dissolved in chloroform in a mole ratio of 100:0.5:5. Oil phase and water phase were mixed and skived. The emulsion was homogenized to form liposomes. The mean diameter of liposomes was determined by dynamic light scattering (DLS) techniques. Low-speed centrifugation was employed to determine encapsulation efficiency (EE). The maximum tolerated doses (MTD) was determined in normal KM mice,and antitumor effect was evaluated in H22/KM mice xenograft tumor model. RESULTS The mean diameter of paclitaxel liposomes was ��140±10�� nm. The EE was over 95 % when the molar ratio of paclitaxel to SPC ranged from 3% to 6%. The MTDs of Pac-lipo and Pac-free in male KM mice were 64.8 and 29.4 mg·kg-1,respectively. Pac-lipo inhibited H22 tumor weight dose-dependently��CONCLUSION Pac-lipo had a high EE,and could increase the therapeutic index significantly,compared with Pac-free.
ZHANG Lan-,
,
LI Yan-Hui- etc
.Preparation of Liposomal Paclitaxel and Its Toxicity and Antitumor Effect[J] Chinese Pharmaceutical Journal, 2013,V48(6): 446-449
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2013, Vol. 48 
