title: An in vitro and in vivo study of gemcitabine-loaded albumin nanoparticles in a pancreatic cancer cell line.
abstract: OBJECTIVE
  Gemcitabine (Gem) is far from satisfactory as the first-line regimen for pancreatic cancer, and the emergence of albumin nanoparticles offers new hope for the delivery of Gem. In this study, Gem-loaded human serum albumin nanoparticles (Gem-HSA-NPs) were successfully synthesized, characterized, and tested on a BxPC-3 cell line both in vitro and in vivo.
  
  
  METHODS
  4-N-myristoyl-gemcitabine (Gem-C14) was obtained first by coupling myristoyl with the 4-amino group of Gem. The Gem-HSA-NPs were then prepared by nanoparticle albumin-bound technology and characterized for particle size, zeta potential, morphology, encapsulation efficiency, drug-loading efficiency, and release characteristics. Using both in vitro and in vivo studies, Gem-C14 and Gem-HSA-NPs were tested on the human pancreatic cancer cell line BxPC-3.
  
  
  RESULTS
  Gem-HSA-NPs showed an average particle size of 150±27 nm, and with an encapsulation rate of 82.99%±3.5% and a drug-loading rate of 10.42%±3.5%, they exhibited a favorable controlled- and sustained-release nature. In in vitro, Gem-C14 was equivalent in cytotoxicity to Gem. In in vivo, the Gem-HSA-NPs exhibited the strongest inhibitory effect on tumor growth but the lowest toxicity among the four groups.
  
  
  CONCLUSIONS
  The enhanced in vivo efficacy of Gem-HSA-NPs toward the pancreatic cancer cell line suggests their potential role for use in the clinical field.
authors.affiliation: Pancreatic Surgery Department, Huashan Hospital, Fudan University, Shanghai, People's Republic of China.
authors.forename: Xinzhe
authors.initials: X
authors.lastname: Yu
authors.affiliation: Pancreatic Disease Institute, Fudan University, Shanghai, People's Republic of China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Di
authors.affiliation: School of Pharmacy & Key Laboratory of Smart Drug Delivery, Fudan University, Shanghai, People's Republic of China.
authors.forename: Chao
authors.initials: C
authors.lastname: Xie
authors.affiliation: School of Pharmacy, The Second Military Medical University, Shanghai, People's Republic of China.
authors.forename: Yunlong
authors.initials: Y
authors.lastname: Song
authors.affiliation: Pancreatic Disease Institute, Fudan University, Shanghai, People's Republic of China.
authors.forename: Hang
authors.initials: H
authors.lastname: He
authors.affiliation: Pancreatic Surgery Department, Huashan Hospital, Fudan University, Shanghai, People's Republic of China.
authors.forename: Hengchao
authors.initials: H
authors.lastname: Li
authors.affiliation: The State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, Shanghai, People's Republic of China.
authors.forename: Xinming
authors.initials: X
authors.lastname: Pu
authors.affiliation: School of Pharmacy & Key Laboratory of Smart Drug Delivery, Fudan University, Shanghai, People's Republic of China.
authors.forename: Weiyue
authors.initials: W
authors.lastname: Lu
authors.affiliation: Pancreatic Disease Institute, Fudan University, Shanghai, People's Republic of China.
authors.forename: Deliang
authors.initials: D
authors.lastname: Fu
authors.affiliation: Pancreatic Surgery Department, Huashan Hospital, Fudan University, Shanghai, People's Republic of China.
authors.forename: Chen
authors.initials: C
authors.lastname: Jin
mesh_terms: D000818:Animals; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D005260:Female; D005434:Flow Cytometry; D006801:Humans; D020287:In Situ Nick-End Labeling; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010190:Pancreatic Neoplasms / Q000473:pathology*; D010316:Particle Size; D012709:Serum Albumin / Q000378:metabolism*; D040521:Subcutaneous Tissue / Q000187:drug effects / Q000473:pathology; D000093542:Gemcitabine
chemical_list: D012709:Serum Albumin; D003841:Deoxycytidine; D000093542:Gemcitabine
keywords: BxPC-3 cell line; albumin nanoparticles; gemcitabine; in vitro study; in vivo study; pancreatic cancer