Preparation and biological evaluation of polymerizable antibody Fab ' fragment targeted polymeric drug delivery system

Authors
Lu, ZR Shiah, JG Kopeckova, P Kopecek, J
Citation
Zr. Lu et al., Preparation and biological evaluation of polymerizable antibody Fab ' fragment targeted polymeric drug delivery system, J CONTR REL, 74(1-3), 2001, pp. 263-268
Citations number
11
Categorie Soggetti
Pharmacology & Toxicology
Journal title
JOURNAL OF CONTROLLED RELEASE
ISSN journal
01683659 → ACNP
Volume
74
Issue
1-3
Year of publication
2001
Pages
263 - 268
Database
ISI
SICI code
0168-3659(20010706)74:1-3<263:PABEOP>2.0.ZU;2-Q
Abstract
A new polymerizable antibody Fab ' fragment with a PEG spacer (MA-PEG-Fab ' ) was prepared from OV-TL 16 antibody, specific against the OA-3 antigen ex pressed on most human ovarian carcinomas. The MA-PEG-Fab ' possessed a high er reactivity in the copolymerization with N-(2-hydroxypropyl)methacrylamid e (HPMA) than the polymerizable Fab ' fragment MA-Fab ' with a short spacer , The MA-PEG-Fab ' was copolymerized with HPMA and MA-Gly-Phe-Leu-Gly-Mce(6 ) producing an Fab ' targeted HPMA copolymer-Mce(6) conjugate. The number a nd weight average molecular weights of the copolymer were 164 000 and 271 0 00 Da, respectively. About two MA-PEG-Fab ' fragments per chain were incorp orated in the copolymer conjugates. Preliminary in vivo antitumor studies i ndicated that the Fab ' targeted conjugates showed a higher efficacy of tum or growth inhibition in nude mice than the non-targeted conjugate. (C) 2001 Elsevier Science BY. All rights reserved.