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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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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, 11451, Saudi Arabia

    Wael A. Mahdi, Afzal Hussain & Sarah I Bukhari

  2. Department of Pharmaceutics, PCTE Institute of Pharmacy, PTU, Ludhiana, Punjab, India

    Mohd Ramzan

  3. Department of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, Punjab, India

    Mohd Ramzan

  4. Department of Pharmaceutical Science, HNB Garhwal University (A Central University), Srinagar, Uttarakhand, India

    Abdul Faruk

  5. Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Jharkhand, 835215, Ranchi, India

    Abhimanyu Dev

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  1. Wael A. Mahdi
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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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