title: Poly(l-lysine)-graft-folic acid-coupled poly(2-methyl-2-oxazoline) (PLL-g-PMOXA-c-FA): a bioactive copolymer for specific targeting to folate receptor-positive cancer cells.
abstract: In this study, we present the preparation, characterization and application of a novel bioactive copolymer poly(l-lysine)-graft-folic acid-coupled poly(2-methyl-2-oxazoline) (PLL-g-PMOXA-c-FA), which has a specific interaction with folate receptor (FR)-positive cancer cells. Glass surface immobilized with PLL-g-PMOXA-c-FA was demonstrated to be adhesive to FR-positive cancer cells (HeLa, JEG-3) while nonadhesive to FR-negative ones (MCF-7, HepG2) in 3 h. The specific interaction between conjugated FA on the substrate and FRs on the cells could hardly be inhibited unless a high concentration (5 mM) of free FA was used due to the multivalent nature of it. The FA functionality ratio of the copolymer on the substrate had a significant influence on the adhesion of HeLa cells, and our experiments revealed that the affinity of the substrate to the cells declined dramatically with the decrease of functionality ratio. This was believed to be caused by the polydispersity of PMOXA tethers, as supported by GPC and ToF-SIMS data. As a proof of concept in the application of our material, we demonstrated successful recovery of HeLa cells from mixture with MCF-7 (1:100) on the copolymer-coated glass, and our results showed that both high sensitivity (95.6 ± 13.3%) and specificity (24.3 ± 8.6%) were achieved.
authors.affiliation: Division of Biomedical Engineering, The Hong Kong University of Science and Technology , Hong Kong, China.
authors.forename: Yin
authors.initials: Y
authors.lastname: Chen
authors.forename: Wenbin
authors.initials: W
authors.lastname: Cao
authors.forename: Junli
authors.initials: J
authors.lastname: Zhou
authors.forename: Bidhari
authors.initials: B
authors.lastname: Pidhatika
authors.forename: Bin
authors.initials: B
authors.lastname: Xiong
authors.forename: Lu
authors.initials: L
authors.lastname: Huang
authors.forename: Qian
authors.initials: Q
authors.lastname: Tian
authors.forename: Yiwei
authors.initials: Y
authors.lastname: Shu
authors.forename: Weijia
authors.initials: W
authors.lastname: Wen
authors.forename: I-Ming
authors.initials: IM
authors.lastname: Hsing
authors.forename: Hongkai
authors.initials: H
authors.lastname: Wu
mesh_terms: D015374:Biosensing Techniques / Q000295:instrumentation / Q000379:methods*; D045744:Cell Line, Tumor; D058975:Folate Receptor 1 / Q000737:chemistry* / Q000378:metabolism; D005492:Folic Acid / Q000737:chemistry*; D006801:Humans; D007700:Kinetics; D009369:Neoplasms / Q000737:chemistry* / Q000378:metabolism; D011073:Polyamines / Q000737:chemistry*; D011107:Polylysine / Q000737:chemistry*; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D058975:Folate Receptor 1; D011073:Polyamines; D011108:Polymers; C117403:poly(2-methyl-2-oxazoline); D011107:Polylysine; D005492:Folic Acid
keywords: bioactive copolymer; cancer cells; folic acid; poly(2-methyl-2-oxazoline); specific targeting