Tissue distribution and pulmonary targeting studies of cefpiramide sodium-loaded liposomes.
The aim of this study was to evaluate the pharmacokinetics (PK), tissue distribution, and the specific drug targeting of cefpiramide sodium-loaded liposomes (CPMS-Lips) compared with cefpiramide sodium solution (CPMS-Sol) in mice. CPMS-Lips were prepared by reverse phase evaporation method. In the PK and biodistribution study, mice received a single intravenous (i.v.) injection of 152 mg/kg of either CPMS-Lips or CPMS-Sol. Plasma and tissues were treated using liquid-liquid extraction and determined using reversed-phase high-performance liquid chromatography (RP-HPLC). The results showed that the CPMS-Lips prepared in this study had an average diameter of 7.146 ± 0.29 μm. In the plasma, the bioavailability (F) and the mean residence times (MRT) of the CPMS-Lips were 2.8- and 4.5-fold larger, respectively, than those of CPMS-Sol. CPMS-Lips also showed a significant difference in the tissue distribution profile in mice when compared with the conventional. The value of the intake rate (r(e)) for the lung was 2.97, which was the highest among the tested tissues. Meanwhile, the ratio of targeting efficiency (Te(liposome)/Te(injection)) of lung to that of other tissues for CPMS-Lips elevated significantly. These showed that CPMS-Lips can improve the bioavailability and biodistribution of CPMS in the lung. In conclusion, the liposome was a promising sustained-release and drug-targeting system for antibiotic drugs.
Sun
Qingxue
Q
Pharmaceutical College in Shandong University, 44 Wen hua Xi Lu, Ji'nan 250012, Shandong Province, People's Republic of China.
Shi
Ming
M
Shao
Wei
W
Shi
Yang
Y
Xi
Yanwei
Y
Huang
Guihua
G
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002511:Cephalosporins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005260:Female; D007275:Injections, Intravenous; D008081:Liposomes; D008168:Lung / Q000378:metabolism*; D008297:Male; D051379:Mice; D014018:Tissue Distribution
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D003692:Delayed-Action Preparations; D008081:Liposomes; C036666:cefpiramide