Zhao Zhiying, Xie Jun, Liu Wenyi, Zhou Jianping
College of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Zhongguo Zhong Yao Za Zhi. 2011 Feb;36(4):450-4.
To develop HCPT liposome with small diameter and to study the tissue distribution of the HCPT liposome in rats.
Modified solvent-injection method was used to prepare HCPT liposome. The entrapment efficiency, morphology, size and zeta potential were also investigated. The transformation temperature and the ratio of cholesterol to phospholipids were determined by fluorescence spectrophotometry. HCPT liposome and HCPT injection (5 mg x kg(-1)) were injected by tail vein in mice, respectively. The tissue concentrations of HCPT were determined by LC-MS/MS.
Under selected process conditions, the HCPT liposomes were spherical and integrated with the mean entrapment efficiency of (96.83 +/- 2.32)%, the size of (180.5 +/- 4.5) nm and the zeta potential of--(32.1 +/- 1.3) mV. It showed that the optimum proportion of cholesterol to phospholipids was 1.5: 10, the optimum transformation temperature was 32.5 degrees C; HCPT liposome at a dose of 5 mg x kg(-1) led to higher concentration and longer duration of action compared with HCPT injection on market.
HCPT liposome prepared by solvent-injection method was characteristic of small mean diameter, high encapsulation efficiency and long circulation in vivo.
制备小粒径的羟基喜树碱脂质体，并研究其在大鼠体内的组织分布。
采用改良溶剂注入法制备羟基喜树碱脂质体，考察其包封率、形态、粒径及zeta电位，用荧光分光光度法测定相变温度及胆固醇与磷脂的比例。将羟基喜树碱脂质体和羟基喜树碱注射液（5mg·kg⁻¹）分别经尾静脉注入小鼠体内，用液相色谱-串联质谱法测定羟基喜树碱的组织浓度。
在选定的工艺条件下，羟基喜树碱脂质体呈球形且完整，平均包封率为（96.83±2.32）%，粒径为（180.5±4.5）nm，zeta电位为-（32.1±1.3）mV。结果表明，胆固醇与磷脂的最佳比例为1.5∶10，最佳相变温度为32.5℃；与市售羟基喜树碱注射液相比，5mg·kg⁻¹剂量的羟基喜树碱脂质体在体内的浓度更高，作用时间更长。
溶剂注入法制备的羟基喜树碱脂质体具有平均粒径小、包封率高、体内循环时间长的特点。
