In vivo distribution of 5-Fluorouracil after peritumoral implantation using a biodegradable micro-device in tumor-bearing mice

Zheng, Na; Zhou, Meng; Liu, Wen

doi:10.1007/s13318-012-0111-z

Cited by 3 publications

(4 citation statements)

References 22 publications

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“…However, 5-Fu and curcumin have their shortcomings, such as toxicity and very low bioavailability, so much work was focused on the development of nano-carriers to overcome these short-comings. 35,36 It was reported that there was a synergism between 5-Fu and curcumin, 37 which was also testified in our study. The nano-carrier could increase the endocytosis of plain drugs, which would further enhance the effect of synergism between 5-Fu and curcumin.…”

Section: Cytotoxicity Of Ldh-5-fu and Sln-curcumin And The Synergeticsupporting

confidence: 75%

Synergetic Effect of SLN-Curcumin and LDH-5-Fu on SMMC-7721 Liver Cancer Cell Line

Zhu

Wu²,

Yu³

et al. 2013

Cancer Biotherapy and Radiopharmaceuticals

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Curcumin and 5-Fluorouracil (5-Fu) have been reported to have anticancer potentials and show certain synergetic effect on some cancer cell lines. However, the poor bioavailability and rapid metabolism limited their medical application. In this study, we encapsulated curcumin with solid lipid nanoparticles (SLN), 5-Fu with Layered double hydroxides (LDHs) separately and tested its properties and anticancer potentials. SLN-curcumin and LDH-5-Fu were determined to be 100 and 60 nm by Transmission Electron Microscopy detection, and the loading efficiency were 28%±2.5% and 16.7%±1.8%, individually. Furthermore, SLN-curcumin and LDH-5-Fu showed a significantly synergetic effect on SMMC-7721 cell stronger than plain drugs together, of which the Idrug loaded nano-carriers was only 0.315. FACS analysis revealed that the combination of SLN-curcumin and LDH-5-Fu induced 80.1% apoptosis in SMMC-7721 cells, which were 1.7-folds of the sum of the two plain drug loaded carriers. The results demonstrated the significant synergetic anticancer potentials of nano-encapsulated curcumin and 5-Fu, which could be further explored for the treatment of other carcinoma.

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Section: Cytotoxicity Of Ldh-5-fu and Sln-curcumin And The Synergeticsupporting

confidence: 75%

Synergetic Effect of SLN-Curcumin and LDH-5-Fu on SMMC-7721 Liver Cancer Cell Line

Zhu

Wu²,

Yu³

et al. 2013

Cancer Biotherapy and Radiopharmaceuticals

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“…Mice were prophylactically treated with 5-FU (10 mg/kg or 40 mg/kg) in combination with or without daptomycin (DAP). All drug concentrations were within the human therapeutic dosage range ( 41 ). In order to assess if the effect of 5-FU is mediated by inhibition of AI-2 production, we simultaneously administered synthetic AI-2 (DPD).…”

Section: Resultsmentioning

confidence: 99%

5-Fluorouracil blocks quorum-sensing of biofilm-embedded methicillin-resistantStaphylococcus aureusin mice

Sedlmayer

Woischnig

Unterreiner

et al. 2021

Nucleic Acids Research

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Antibiotic-resistant pathogens often escape antimicrobial treatment by forming protective biofilms in response to quorum-sensing communication via diffusible autoinducers. Biofilm formation by the nosocomial pathogen methicillin-resistant Staphylococcus aureus (MRSA) is triggered by the quorum-sensor autoinducer-2 (AI-2), whose biosynthesis is mediated by methylthioadenosine/S-adenosylhomocysteine nucleosidase (MTAN) and S-ribosylhomocysteine lyase (LuxS). Here, we present a high-throughput screening platform for small-molecular inhibitors of either enzyme. This platform employs a cell-based assay to report non-toxic, bioavailable and cell-penetrating inhibitors of AI-2 production, utilizing engineered human cells programmed to constitutively secrete AI-2 by tapping into the endogenous methylation cycle via ectopic expression of codon-optimized MTAN and LuxS. Screening of a library of over 5000 commercial compounds yielded 66 hits, including the FDA-licensed cytostatic anti-cancer drug 5-fluorouracil (5-FU). Secondary screening and validation studies showed that 5-FU is a potent quorum-quencher, inhibiting AI-2 production and release by MRSA, Staphylococcus epidermidis, Escherichia coli and Vibrio harveyi. 5-FU efficiently reduced adherence and blocked biofilm formation of MRSA in vitro at an order-of-magnitude-lower concentration than that clinically relevant for anti-cancer therapy. Furthermore, 5-FU reestablished antibiotic susceptibility and enabled daptomycin-mediated prevention and clearance of MRSA infection in a mouse model of human implant-associated infection.

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“…Advances in lithographic technology have enabled the fabrication of PLGA microdevices. 10,169,170 In one study a micromold was fabricated by casting polydimethylsiloxane (PDMS) onto a lithographically patterned SU-8 mold. The PDMS mold was used to fabricate 5-FU-loaded PLGA microdevices with honeycomb structures and 5-FU was injected as a fine powder into the chamber.…”

Section: -Fu-loaded Plga Formulationsmentioning

confidence: 99%

“…10 This group of researchers also conducted another study to observe the pharmacokinetics of 5-FU released from this device. 170 Mice administered with 5-FU via IP injection (7.2 mg/mice) had a peak plasma concentration (C max ) of 0.83 µg/ml and time to peak plasma concentration (T max ) at 0.5 hours. The plasma concentration was lower than the limit of detection (50 µg/ml) within 2 hours.…”

Section: -Fu-loaded Plga Formulationsmentioning

confidence: 99%

Fabrication and Use of Poly(d,l-lactide-co-glycolide)-Based Formulations Designed for Modified Release of 5-Fluorouracil

Leelakanok¹,

Geary²,

Salem³

2018

Journal of Pharmaceutical Sciences

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5-fluorouracil (5-FU) is a chemotherapeutic agent that has been used for the treatment of a variety of malignancies since its initial introduction to the clinic in 1957. Owing to its short biological half-life, multiple dosings are generally required to maintain effective 5-FU plasma concentrations throughout the therapeutic period. Clinical studies have shown that continuous 5-FU administration is generally superior to bolus injection as exhibited by lower toxicities and increased therapeutic efficacy. Optimal therapeutic efficacy, however, is often compromised by the limiting therapeutic index. Whilst oral formulations are also used, these suffer from the drawbacks of variable bioavailability and first-pass metabolism. As a result, sustained release formulations of 5-FU have been investigated in an effort to mimic the kinetics of continuous infusion particularly for situations where local delivery is considered appropriate. The biocompatible, biodegradable, and highly tunable synthetic polymer, poly(d,l-lactide-co-glycolide) (PLGA), is widely used as a vector for sustained drug delivery, however, issues such as insufficient loading and inappropriate burst release kinetics have dogged progress into the clinic for small hydrophilic drugs such as 5-FU. This review provides introductory information about the mechanism of action, pharmacokinetic and physicochemical properties, and clinical use of 5-FU that have contributed to the development of PLGA-based 5-FU release platforms. In addition, this review provides information on fabrication methods used for a range of 5-FU-loaded PLGA formulations and discusses factors affecting the release kinetics of 5-FU as well as the in vitro and in vivo antitumor or antiproliferative efficacy of these platforms.

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In vivo distribution of 5-Fluorouracil after peritumoral implantation using a biodegradable micro-device in tumor-bearing mice

Cited by 3 publications

References 22 publications

Synergetic Effect of SLN-Curcumin and LDH-5-Fu on SMMC-7721 Liver Cancer Cell Line

Synergetic Effect of SLN-Curcumin and LDH-5-Fu on SMMC-7721 Liver Cancer Cell Line

5-Fluorouracil blocks quorum-sensing of biofilm-embedded methicillin-resistantStaphylococcus aureusin mice

Fabrication and Use of Poly(d,l-lactide-co-glycolide)-Based Formulations Designed for Modified Release of 5-Fluorouracil

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