HUANG He-song1�� GONG Wei2�� ZHANG Hui2�� ZHENG Xiao-li3�� MEI Xing-guo2*
1. Hunan Academy of Chinese Medicine�� Changsha 410006�� China; 2.Institute of Pharmacology and Toxicology�� Academy of Military Medical Sciences�� Beijing 100850, China; 3.Shanghai Asiapioneer Pharmaceuticals�� Shanghai 201203, China
Abstract��
OBJECTIVE To prepare vinorelbine tartrate��VRT�� thermo-sensitive liposomes and establish methods for determining its VRT content and entrapment efficiency. METHODS VRT thermo-sensitive liposomes were prepared by pH-gradients method. VRT contents were determined by HPLC. Liposomes and free drug were separated by mini-column centrifugation. The influential factors of VRT elution including sephadex type�� elution solution�� and column height and elution volume were investigated. RESULTS Mean particle size of VRT thermo-sensitive liposomes was ��94.6��1.6��nm. VRT content was ��1.83��0.03�� mg��mL-1. The entrapment efficiencies of three batches of VRT thermo-sensitive liposomes were ��95.75��1.42��%�� ��91.12��1.21��% and ��94.10��2.03��%�� and the elution recoveries were ��98.3��2.42��%�� ��93.5��1.83��% and ��96.6��1.65��%. Sephadex G-25 was chosen to prepare mini-column. Elution solution were PBS�� 4 cm of column height was optimal�� and one of gradients-elution-volumes was ascertained. CONCLUSION The preparation technology of VRT liposomes was stable�� drug loading and entrapping capacity of VRT liposomes were well. The methods for determination of VRT content and entrapment efficiency were simple�� rapid and accurate. These studies can provide bases for further development of intravenous injection VRT thermo-sensitive liposomes.
2010, Vol. 45 
