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An in vitro and in vivo study of gemcitabine-loaded albumin nanoparticles in a pancreatic cancer cell line

Authors Yu XZ, Di Y, Xie C, Song YL, He H, Li HC, Pu XM, Lu WY, Fu DL, Jin C

Received 6 August 2015

Accepted for publication 16 September 2015

Published 30 October 2015 Volume 2015:10(1) Pages 6825—6834

DOI https://doi.org/10.2147/IJN.S93835

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Yashdeep Phanse

Peer reviewer comments 2

Editor who approved publication: Dr Lei Yang

Video abstract presented by Xinzhe Yu.

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Xinzhe Yu,1,* Yang Di,2,* Chao Xie,3 Yunlong Song,4 Hang He,2 Hengchao Li,1 Xinming Pu,5 Weiyue Lu,3 Deliang Fu,2 Chen Jin1

1Pancreatic Surgery Department, Huashan Hospital, 2Pancreatic Disease Institute, Fudan University, 3School of Pharmacy & Key Laboratory of Smart Drug Delivery, Fudan University, 4School of Pharmacy, The Second Military Medical University, 5The State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, Shanghai, People’s Republic of China

*These authors contributed equally to this work


Background and objectives: 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.
Materials and 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.
Conclusion: 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.

Keywords: pancreatic cancer, gemcitabine, albumin nanoparticles, BxPC-3 cell line, in vitro study, in vivo study

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