title: AS1411 aptamer tagged PLGA-lecithin-PEG nanoparticles for tumor cell targeting and drug delivery.
abstract: Liposomes and polymers are widely used drug carriers for controlled release since they offer many advantages like increased treatment effectiveness, reduced toxicity and are of biodegradable nature. In this work, anticancer drug-loaded PLGA-lecithin-PEG nanoparticles (NPs) were synthesized and were functionalized with AS1411 anti-nucleolin aptamers for site-specific targeting against tumor cells which over expresses nucleolin receptors. The particles were characterized by transmission electron microscope (TEM) and X-ray photoelectron spectroscopy (XPS). The drug-loading efficiency, encapsulation efficiency and in vitro drug release studies were conducted using UV spectroscopy. Cytotoxicity studies were carried out in two different cancer cell lines, MCF-7 and GI-1 cells and two different normal cells, L929 cells and HMEC cells. Confocal microscopy and flowcytometry confirmed the cellular uptake of particles and targeted drug delivery. The morphology analysis of the NPs proved that the particles were smooth and spherical in shape with a size ranging from 60 to 110 nm. Drug-loading studies indicated that under the same drug loading, the aptamer-targeted NPs show enhanced cancer killing effect compared to the corresponding non-targeted NPs. In addition, the PLGA-lecithin-PEG NPs exhibited high encapsulation efficiency and superior sustained drug release than the drug loaded in plain PLGA NPs. The results confirmed that AS1411 aptamer-PLGA-lecithin-PEG NPs are potential carrier candidates for differential targeted drug delivery.
authors.affiliation: Bio Nano Electronics Research Center, Graduate School of Interdisciplinary New Science, Toyo University Kawagoe, Saitama, Japan.
authors.forename: Athulya
authors.initials: A
authors.lastname: Aravind
authors.forename: Prashanti
authors.initials: P
authors.lastname: Jeyamohan
authors.forename: Remya
authors.initials: R
authors.lastname: Nair
authors.forename: Srivani
authors.initials: S
authors.lastname: Veeranarayanan
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Nagaoka
authors.forename: Yasuhiko
authors.initials: Y
authors.lastname: Yoshida
authors.forename: Toru
authors.initials: T
authors.lastname: Maekawa
authors.forename: D Sakthi
authors.initials: DS
authors.lastname: Kumar
mesh_terms: D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D052157:Aptamers, Nucleotide; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics*; D005434:Flow Cytometry; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D054709:Lecithins / Q000737:chemistry / Q000493:pharmacokinetics*; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry*; D009838:Oligodeoxyribonucleotides / Q000737:chemistry / Q000493:pharmacokinetics*; D056951:Photoelectron Spectroscopy; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics*; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013056:Spectrophotometry, Ultraviolet
chemical_list: C513936:AGRO 100; D000970:Antineoplastic Agents; D052157:Aptamers, Nucleotide; D004337:Drug Carriers; D054709:Lecithins; D009838:Oligodeoxyribonucleotides; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols