Preparation and Entrapment Efficiency of Vinorelbine Tartrate Thermo-sensitive Liposomes
HUANG He-song1, GONG Wei2, ZHANG Hui2, ZHENG Xiao-li3, MEI Xing-guo2*
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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
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.
HUNG He-song;GONG Wei;ZHNG Hui;ZHENG Xio-li;MEI Xing-guo.
Preparation and Entrapment Efficiency of Vinorelbine Tartrate Thermo-sensitive Liposomes[J]. Chinese Pharmaceutical Journal, 2010, 45(16): 1250-1254
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