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Review
. 2020 Jul 30:15:5445-5458.
doi: 10.2147/IJN.S257700. eCollection 2020.

Recent Advances in Designing 5-Fluorouracil Delivery Systems: A Stepping Stone in the Safe Treatment of Colorectal Cancer

Elaheh Entezar-Almahdi  1 , Soliman Mohammadi-Samani  1   2 , Lobat Tayebi  3 , Fatemeh Farjadian  2
Affiliations
Review

Recent Advances in Designing 5-Fluorouracil Delivery Systems: A Stepping Stone in the Safe Treatment of Colorectal Cancer

Elaheh Entezar-Almahdi et al. Int J Nanomedicine. .

Abstract

5-Fluorouracil (5-FU) has become one of the most widely employed antimetabolite chemotherapeutic agents in recent decades. It is considered a first line antineoplastic agent for the treatment of colorectal cancer. Unfortunately, chemotherapy with 5-FU has several limitations, including its short half-life, high cytotoxicity and low bioavailability. In order to overcome the drawbacks of 5-FU and enhance its therapeutic efficiency, many scientific groups have focused on designing a new delivery system to successfully deliver 5-FU to tumor sites. We provide a comprehensive review on different strategies to design effective delivery systems, including nanoformulations, drug-conjugate formulations and other strategies for the delivery of 5-FU to colorectal cancer. Furthermore, co-delivery of 5-FU with other therapeutics is discussed. This review critically highlights the recent innovations in and literature on various types of carrier system for 5-FU.

Keywords: 5-fluorouracil; co-delivery; colorectal cancer; drug delivery; nanomedicine; nanoparticles.

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Conflict of interest statement

The authors declare no conflicts of interest in this article.

Figures

Figure 1
Figure 1
Some nanoparticulate DDSs.
Figure 2
Figure 2
Mechanism of action of 5-FU to inhibit thymidylate synthase. Abbreviations: FdUMP, fluorodeoxyuridine monophosphate; dUTP, deoxyuridine triphosphate; dTMP, deoxythymidine monophosphate; dTTP, deoxythymidine triphosphate methylene; THF, methylene tetrahydrofolate; DHF, dihydrofolate.
Figure 3
Figure 3
Synthesis of CEINs–PEI–5-FU–βCD–FA nanotheranostic agents. Note: Copyright © 2018 Chemistry Select. Reproduce from Kasprzak A, Gunka K, Fronczak M, Bystrzejewski M, Poplawska M. Folic acid-navigated and β-cyclodextrin-decorated carbon-encapsulated iron nanoparticles as the nanotheranostic platform for controlled release of 5-fluorouracil. Chemistry Select. 2018;3(38):10821–10830.
See this image and copyright information in PMC

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