@article{oai:nagasaki-u.repo.nii.ac.jp:00023142,
 author = {Teshima, Mugen and Kawakami, Shigeru and Fumoto, Shintaro and Nishida, Koyo and Nakamura, Junzo and Nakashima, Mikiro and Nakagawa, Hiroo and Ichikawa, Nobuhiro and Sasaki, Hitoshi},
 issue = {7},
 journal = {Biological & Pharmaceutical Bulletin},
 month = {Jul},
 note = {We investigated the pharmacokinetic behavior of palmitoyl prednisolone (Pal-PLS) and its liposomes with L-α-distearoylphosphatidylcholine (DSPC) and cholesterol (Chol) with or without L-α-distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG 2000) after their intravenous administration in rats. Pal-PLS rapidly disappeared from the systemic circulation and prednisolone (PLS) was regenerated after the administration of DSPC/Chol liposomes. PEGylated liposomes including DSPE-PEG 2000, however, successfully maintained high blood concentrations of Pal-PLS and PLS. The blood profiles of drugs after the administration of liposomal Pal-PLS were analyzed according to a two-compartment model. The larger content of DSPE-PEG 2000 in DSPC/Chol liposomes showed a lower first order elimination rate constant from the central compartment (Kel) and clearance (CL). The area under the concentration?time curve (AUC) of Pal-PLS and PLS in PEGylated liposomes was larger than DSPC/Chol liposomes. The mean resident time (MRT) of Pal-PLS and PLS was also prolonged by PEGylated liposomes. Although DSPC/Chol liposomes showed a high distribution of Pal-PLS in the liver and spleen, PEGylated liposomes significantly decreased the liver distribution of Pal-PLS. The biliary and urinary excretions of drugs for 240 min after drug administration were less than 1% of the administrated dose in any formulations. In conclusion, PEGylated liposomes, including Pal-PLS, are useful for maintain the PLS concentration in the blood after intravenous administration., Biological & Pharmaceutical Bulletin v.29(7) p.1436-1440, 2006},
 pages = {1436--1440},
 title = {PEGylated Liposomes Loading Palmitoyl Prednisolone for Prolonged Blood Concentration of Prednisolone},
 volume = {29},
 year = {2006}
}