title: Confocal Raman microspectroscopic study of folate receptor-targeted delivery of 6-mercaptopurine-embedded gold nanoparticles in a single cell.
abstract: We investigate the cellular uptake behaviors and efficacy of folate-coated gold nanoparticles (AuNPs) for the targeted drug delivery system in human cancer cells. Folate-conjugated AuNPs embedded with a purine analogue cancer drug of 6-mercaptopurine (6MP) were assembled via a 1-ethyl-3-[3-dimethylaminopropyl] carbodiimide hydrochloride (EDC) coupling reaction between the amino group of 4-aminobenzenethiol (ABT) and the carboxyl group of folic acid. The assembly of folate and 6MP on AuNPs has been examined by absorption spectroscopy, transmission electron microscopy (TEM), and confocal Raman spectroscopy. The internalization of the conjugated AuNPs inside the folate receptor-positive HeLa and KB cells was checked by TEM and dark-field microscopy (DFM) combined with label-free confocal spectroscopy over the depth variable z at a micrometer resolution. DFM live cell imaging of folate-conjugated AuNPs in HeLa cells indicated that the targeted AuNPs appeared to attach on the cell surfaces and enter into the cell with an hour. The cell viability was also compared to estimate the efficacy of folate-conjugated AuNP delivery systems. Folate receptor-targeted AuNP systems appeared to decrease cancer cell viability both in vitro and in vivo more than did the use of the 6MP-coated AuNPs drug without any targeting systems.
authors.affiliation: Department of Chemistry, Soongsil University, Seoul, Korea.
authors.forename: Jin
authors.initials: J
authors.lastname: Park
authors.forename: Won Il
authors.initials: WI
authors.lastname: Jeon
authors.forename: So Yeong
authors.initials: SY
authors.lastname: Lee
authors.forename: Kwang-Su
authors.initials: KS
authors.lastname: Ock
authors.forename: Ji Hye
authors.initials: JH
authors.lastname: Seo
authors.forename: Jinho
authors.initials: J
authors.lastname: Park
authors.forename: Erdene-Ochir
authors.initials: EO
authors.lastname: Ganbold
authors.forename: Keunchang
authors.initials: K
authors.lastname: Cho
authors.forename: Nam Woong
authors.initials: NW
authors.lastname: Song
authors.forename: Sang-Woo
authors.initials: SW
authors.lastname: Joo
mesh_terms: D000042:Absorption / Q000187:drug effects; D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems / Q000379:methods*; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism*; D005492:Folic Acid / Q000378:metabolism; D006046:Gold / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D008297:Male; D015122:Mercaptopurine / Q000494:pharmacology*; D053768:Metal Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D013059:Spectrum Analysis, Raman / Q000379:methods*
chemical_list: D058973:Folate Receptors, GPI-Anchored; D006046:Gold; D005492:Folic Acid; D015122:Mercaptopurine