Polymerizable Fab′ antibody fragments for targeting of anticancer drugs

Abstract
We have designed a new pathway for the synthesis of targeted polymeric drug delivery systems, using polymerizable antibody Fab′ fragments (MA-Fab′). The targeted systems can be directly prepared by copolymerization of the MA-Fab′, N-(2-hydroxypropyl)methacrylamide (HPMA) and drug-containing monomers. Both MA-Fab′ and the Fab′-targeted copolymers can effectively bind to target cells. An MA-Fab′ (from OV-TL 16 Ab) targeted HPMA copolymer containing mesochlorin e6 (Mce6) was synthesized by copolymerization of MA-Fab′, HPMA, and MA-GFLG-Mce6. The targeted copolymer exhibited a higher cytotoxicity toward OVCAR-3 human ovarian carcinoma cells than the nontargeted Mce6-containing copolymer or free Mce6. The targeted copolymer was internalized more efficiently by OVCAR-3 cells than the nontargeted copolymer.

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