The characterization and biodistribution of cefoxitin-loaded liposomes.
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.
Wu
Pao-Chu
PC
School of Pharmacy, Kaohsiung Medical University, No. 100, Shih-Chuan 1st Road, Kaohsiung 807, Taiwan, ROC.
Tsai
Yi-Hung
YH
Liao
Chung-Cheng
CC
Chang
Jui-Sheng
JS
Huang
Yaw-Bin
YB
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D001646:Bile / Q000378:metabolism; D002440:Cefoxitin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D002784:Cholesterol / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004134:Dimyristoylphosphatidylcholine / Q000737:chemistry; D004355:Drug Stability; D005612:Freeze Drying; D008081:Liposomes; D008297:Male; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D013678:Technology, Pharmaceutical; D014018:Tissue Distribution
D000900:Anti-Bacterial Agents; D008081:Liposomes; D002440:Cefoxitin; D002784:Cholesterol; D004134:Dimyristoylphosphatidylcholine