Pluronic-Coated Biogenic Gold Nanoparticles for Colon Delivery of 5-Fluorouracil: In vitro and Ex vivo Studies

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Abstract

The aim of the study was to prepare 5-fluorouracil (5-FU)-loaded biogenic gold nanoparticles with pluronic-based coating (PFGNPs), their optimization (full factorial predicted OBPN-1) and in vitro-ex vivo evaluation. Several formulations were prepared, selected for optimization using Design Expert®, and compared for morphology, 5-FU release kinetics, compatibility, cell line toxicity, in vitro hemocompatibility, and ex vivo intestinal permeation across the rat duodenum, jejunum, and ileum. The pluronic-coated 5-FU-carrying GNPs were spherical, 29.11–178.21 nm in diameter, with a polydispersity index (PDI) range of 0.191–292, and a zeta potential (ZP) range of 11.19–29.21 (-mV). The optimized OBPN-1 (desirability = 0.95) demonstrated optimum size (175.1 nm), %DL as 73.8%, ZP as 21.7 mV, % drug release (DR) as 75.7%, and greater cytotoxicity (viability ~ 8.9%) against the colon cancer cell lines than 5-FU solution (~ 24.91%), and less hemocompatibility. Moreover, OBPN-1 exhibited 4.5-fold permeation across the rat jejunum compared with 5-FU solution. Thus, the PFGNPs exhibit high DL capacity, sustained delivery, hemocompatibility, improved efficacy, and enhanced permeation profiles compared with 5-FU solution and several other NPs preparations suggesting it is a promising formulation for effective colon cancer control with reduced side effects.

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Acknowledgements

The authors extend their appreciation to the Deputyship for Research & Innovation, “Ministry of Education” in Saudi Arabia for funding this research work through the project number (IFKSURG-1441-443).

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Correspondence to Wael A. Mahdi or Afzal Hussain.

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The original online version of this article was revised: During production, a type-setting error occurred in the acknowledgment section. The project number published was (IFKSURG-1442-443). The correct project number is (IFKSURG-1441-443).

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Mahdi, W.A., Hussain, A., Ramzan, M. et al. Pluronic-Coated Biogenic Gold Nanoparticles for Colon Delivery of 5-Fluorouracil: In vitro and Ex vivo Studies. AAPS PharmSciTech 22, 64 (2021). https://doi.org/10.1208/s12249-021-01922-1

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Key Words

  • biogenic gold nanoparticles
  • Design Expert®
  • colon cancer cell lines
  • hemolysis assessment
  • ex vivo permeation profiles