title: Development and characterization of folic acid-conjugated chitosan nanoparticles for targeted and controlled delivery of gemcitabinein lung cancer therapeutics.
abstract: The present study was designed to investigate the tumor-targeting potential of gemcitabine (GEM)-loaded surface-tailored chitosan (CS)/poly (ethylene glycol) nanoparticles (FA-PEG-GEM-NPs). The nanoparticles encapsulated with GEM were prepared, characterized, and tethered with folic acid. The developed formulations were characterized with respect to particle size/poly-dispersity index, shape, and zeta potential analysis. The in vitro study shows the sustained drug-release kinetics during 48 h. The present result shows remarkable cytotoxicity rendered by GEM when delivered through FA-PEG-GEM-NPs formulation. The microscopic assessment is suggestive of significant uptake of FA-PEG-GEM-NPs in comparison with the unmodified PEG-GEM-NPs and free drug. Finally, our results advocate for the sizeable compatibility, comparatively less organ toxicity, and higher anti-tumor activity of ligand-anchored and PEGylated CS nanoparticles in vitro and corroborated by in vivo investigations. In conclusion, it is interpreted that surface-tailored nanoparticles are capable to ferry bioactives selectively and specifically to tumor sites with the interception of minimal side effects, thereby suggesting their potential application in cancer therapeutics.
authors.affiliation: a Department of Respiratory Medicine , Liaocheng People's Hospital , Liaocheng , China.
authors.forename: Fengqiang
authors.initials: F
authors.lastname: Wang
authors.affiliation: a Department of Respiratory Medicine , Liaocheng People's Hospital , Liaocheng , China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.affiliation: b Department of Gastroenterology , Liaocheng People's Hospital , Liaocheng , China.
authors.forename: Qingzhu
authors.initials: Q
authors.lastname: Ma
authors.affiliation: a Department of Respiratory Medicine , Liaocheng People's Hospital , Liaocheng , China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Cao
authors.affiliation: a Department of Respiratory Medicine , Liaocheng People's Hospital , Liaocheng , China.
authors.forename: Bo
authors.initials: B
authors.lastname: Yu
mesh_terms: D000072283:A549 Cells; D000818:Animals; D001692:Biological Transport; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D065546:Drug Liberation; D005492:Folic Acid / Q000737:chemistry*; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D014018:Tissue Distribution; D000093542:Gemcitabine
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D003841:Deoxycytidine; D011092:Polyethylene Glycols; D048271:Chitosan; D005492:Folic Acid; D000093542:Gemcitabine
keywords: Chitosan; biocompatibility; cancer targeting; folic acid; gemcitabine; ligands; polyethylene glycol; receptors