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Enhancement of in vitro and in vivo microdialysis recovery of SB‐265123 using Intralipid ® and Encapsin ® as perfusates
Author(s) -
Ward Keith W.,
Medina Sarah J.,
Portelli Samm T.,
Mahar Doan Kelly M.,
Spengler Michael D.,
Ben Michael M.,
Lundberg David,
Levy Mark A.,
Chen Emile P.
Publication year - 2003
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.332
Subject(s) - in vivo , microdialysis , in vitro , chemistry , chromatography , biochemistry , biology , microbiology and biotechnology
Abstract This study was conducted to compare the ability of two potential microdialysis perfusates to enhance the recovery of SB‐265123, a lipophilic, highly protein‐bound compound, both in vitro and in vivo . Initial in vitro experiments established that the recovery of SB‐265123 by microdialysis using normal saline as a perfusate was poor (1.7%). Different concentrations of Intralipid ® and Encapsin ® also were evaluated in an identical in vitro setting, to determine enhancement of recovery. In vitro recovery was enhanced to approximately 24 and 65% with 5 and 20% Intralipid ® , and to approximately 59 and 62% with 5 and 20% Encapsin ® , respectively. A rat in vivo study was conducted with 20% Encapsin ® to confirm the in vitro observations. In the in vivo study, 75–80% recovery of free SB‐265123 was achieved using 20% Encapsin ® as a perfusate. The results from this study indicate that for SB‐265123, a lipophilic, highly protein‐bound molecule, Encapsin ® is an efficient recovery enhancer in vitro . The results from this investigation further demonstrate that a recovery enhancer may be useful for in vivo applications, even with a compound that is highly bound to plasma protein. Copyright © 2002 John Wiley & Sons, Ltd.