title: Comparative protein binding of taxotere and SID530, a new docetaxel formulation with hydroxypropyl-beta-cyclodextrin, in human plasma in vitro.
abstract: The purpose of this study was to evaluate the plasma-protein binding of docetaxel in two different formulations, Taxotere and SID530, a new docetaxel formulation with hydroxypropyl-beta-cyclodextrin (HP-beta-CD), in human plasma in vitro, using equilibrium dialysis. Unbound docetaxel concentration in the human plasma was determined by LC-MS/MS analysis. SID530 showed a plasma-protein binding profile comparable to that of Taxotere in the clinically relevant concentration range of docetaxel. In both formulations, the unbound fraction of docetaxel increased in a concentration-dependent biphasic manner. The resulting data indicate that the excipient used in SID530, HP-beta-CD, generates similar effects as polysorbate 80 of Taxotere in terms of plasma-protein binding of docetaxel.
authors.affiliation: College of Pharmacy, Seoul National University, Seoul, Republic of Korea.
authors.forename: T K
authors.initials: TK
authors.lastname: Kim
authors.forename: H H
authors.initials: HH
authors.lastname: Yoo
authors.forename: E J
authors.initials: EJ
authors.lastname: Kim
authors.forename: J H
authors.initials: JH
authors.lastname: Sa
authors.forename: B-Y
authors.initials: BY
authors.lastname: Lee
authors.forename: J H
authors.initials: JH
authors.lastname: Park
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000097:blood*; D001798:Blood Proteins / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003956:Dialysis; D000077143:Docetaxel; D006801:Humans; D007202:Indicators and Reagents; D013058:Mass Spectrometry; D011208:Powders; D011485:Protein Binding; D015203:Reproducibility of Results; D043823:Taxoids / Q000008:administration & dosage / Q000097:blood*; D013810:Therapeutic Equivalency; D047392:beta-Cyclodextrins
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D001798:Blood Proteins; D007202:Indicators and Reagents; D011208:Powders; D043823:Taxoids; D047392:beta-Cyclodextrins; D000077143:Docetaxel; D000073738:2-Hydroxypropyl-beta-cyclodextrin