The characterization and biodistribution of cefoxitin-l...

The characterization and biodistribution of cefoxitin-loaded liposomes

The characterization and biodistribution of cefoxitin-loaded liposomes
1 March 2004
Received 30 June 2003; revised 14 October 2003; accepted 22 October 2003. ; Available online 14 December 2003.
Pao-Chu Wu, Yi-Hung Tsai, Chung-Cheng Liao, Jui-Sheng Chang and Yaw-Bin Huang
International Journal of Pharmaceutics
Volume 271, Issues 1-2
ScienceDirect
School of Pharmacy, Kaohsiung Medical University, No. 100, Shih-Chuan 1st Road, Kaohsiung 807, Taiwan, ROC
Abstract
To conquer the clinical restriction of relative short half-life and poor tissue retaining activities, liposomes containing cefoxitin were prepared using three methods in this study. The physicochemical properties including cefoxitin encapsulation percentage, vesicle size, stability, as well as the in vivo biodistribution were studied. The highest entrapment percentage was observed by using reverse phase evaporation method, and the molar ratio of cefoxitin to phospholipids was 1:3, DMPC to cholesterol was 2:1, respectively. From the result of stability, the freeze-drying powder and then stored in the frozen condition of cefoxitin-loaded liposome was an ideal storage state. Accordingly, the formulation by reverse-phase evaporation method was selected to investigate the biodistribution of cefoxitin-loaded liposome and compared to free cefoxitin in rats. It was observed that the cefoxitin levels and the duration retained in the liver, spleen, and pancreas of liposome-injected animals were higher and longer than that of free cefoxitin-injected animals. The drug concentrations of bile after post-injection of liposomal cefoxitin at 0.5, 1 and 2 h were all approximately 2.7 times higher than that of free cefoxitin injection group.
Author Keywords: Cefoxitin; Liposome; Stability; Biodistribution

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