Dual targeting of l-carnitine-conjugated nanoparticles to OCTN2 and ATB^0,+ to deliver chemotherapeutic agents for colon cancer therapy.

ABSTRACT: l-Carnitine, obligatory for oxidation of fatty acids, is transported into cells by the Na⁺-coupled transporter OCTN2 and the Na⁺/Cl^--coupled transporter ATB^0,+. Here we investigated the potential of L-carnitine-conjugated poly(lactic-co-glycolic acid) (PLGA) nanoparticles (LC-PLGA NPs) to deliver chemotherapeutic drugs into cancer cells by targeting the nanoparticles to both OCTN2 and ATB^0,+. The cellular uptake of LC-PLGA NPs in the breast cancer cell line MCF7 and the colon cancer cell line Caco-2 was increased compared to unmodified nanoparticles, but decreased in the absence of co-transporting ions (Na⁺ and/or Cl^-) or in the presence of competitive substrates for the two transporters. Studies with fluorescentl

SUBMITTER: Kou L 

PROVIDER: S-EPMC8241000 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature