5-Fluorouracil, innovative drug delivery systems to enhance bioavailability for topical use

Oliveira, Beatriz Ewert de; Amorim, Otávio Henrique Junqueira; Lima, Lonetá Lauro; Rezende, Rodrigo Alvarenga; Mestnik, Natalia Cammarosano; Bagatin, Ediléia; Leonardi, Gislaine Ricci

doi:10.1016/j.jddst.2020.102155

Cited by 28 publications

(30 citation statements)

References 72 publications

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“…Thus, a high dose needs to be administered to reach effective intracellular concentrations. It has a narrow therapeutic index with a high incidence of side effects ( Ewert de Oliveira et al, 2021 ). Some of the most common are mucositis, diarrhea, or myelosuppression.…”

Section: Peripheral Neuropathy: Neuropathic Painmentioning

confidence: 99%

Mechanisms of Chemotherapy-Induced Neurotoxicity

et al. 2022

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Since the first clinical trials conducted after World War II, chemotherapeutic drugs have been extensively used in the clinic as the main cancer treatment either alone or as an adjuvant therapy before and after surgery. Although the use of chemotherapeutic drugs improved the survival of cancer patients, these drugs are notorious for causing many severe side effects that significantly reduce the efficacy of anti-cancer treatment and patients’ quality of life. Many widely used chemotherapy drugs including platinum-based agents, taxanes, vinca alkaloids, proteasome inhibitors, and thalidomide analogs may cause direct and indirect neurotoxicity. In this review we discuss the main effects of chemotherapy on the peripheral and central nervous systems, including neuropathic pain, chemobrain, enteric neuropathy, as well as nausea and emesis. Understanding mechanisms involved in chemotherapy-induced neurotoxicity is crucial for the development of drugs that can protect the nervous system, reduce symptoms experienced by millions of patients, and improve the outcome of the treatment and patients’ quality of life.

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Section: Peripheral Neuropathy: Neuropathic Painmentioning

confidence: 99%

Mechanisms of Chemotherapy-Induced Neurotoxicity

et al. 2022

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“…As a broad‐spectrum anti‐tumor anthracycline, doxorubicin (DOX) has been being widely used to treat various cancers, such as thyroid, stomach, lung, and bone cancers 3 . And 5‐fluorouracil (5‐FU) as a pyrimidine derivative with broad‐spectrum antitumor activity, has also been widely applied in cancer chemotherapy 28 . The combination of DOX and 5‐FU in multi‐target therapy has shown superior antitumor activity to either one alone, indicating their synergistic inhibitory effect on tumor growth 29,30 .…”

Section: Introductionmentioning

confidence: 99%

“…3 And 5-fluorouracil (5-FU) as a pyrimidine derivative with broad-spectrum antitumor activity, has also been widely applied in cancer chemotherapy. 28 The combination of DOX and 5-FU in multi-target therapy has shown superior antitumor activity to either one alone, indicating their synergistic inhibitory effect on tumor growth. 29,30 As we know, DOX is hydrophobic and 5-FU is hydrophilic, so encapsulating the both into the different parts of the core-shell PNIPAM@GO microspheres is so appropriate to get a multi-target platform.…”

Section: Introductionmentioning

confidence: 99%

Fabrication of novel PNIPAM@GO microspheres loaded with dual drugs featuring on‐demand drug release capability

Jiang

Wang

et al. 2022

J of Applied Polymer Sci

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In this research, we successfully prepared a new kind of core‐shell microspheres (PNIPAM@GO) composed of hydrophilic poly (N‐isopropyl acrylamide) (PNIPAM) nanoparticles as the core and amphiphilic graphene oxide (GO) nanosheets as the shell through hydrogen bonding and self‐assembly in organic solvent. The temperature‐sensitive behavior of the PNIPAM core made its average size decrease from 888.3 nm to 630.3 nm with temperature increasing from 25°C to 50°C. And the GO shell could give PNIPAM@GO microspheres remarkable photothermal effects in water under NIR laser irradiation (808 nm) for 20 min. Further, doxorubicin (DOX) and 5‐fluorouracil (5‐FU) were loaded into the core and the shell with loading efficiency of 81% and 11%, respectively. By turning on/off NIR irradiation, the PNIPAM@GO microspheres could respond to the heat generated from GO shell by volume shrinkage, thus on‐demand controlling the drug release. The in vitro biological assessment verified that the samples prepared here were biocompatible. The developed platform shows a potential application in chemo‐photothermal therapy of cancers in the future.

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“…Likewise, a 2009 publication by Corporate Safety, Health & Environmental Protection, Switzerland, reported a figure of 1545 kg of 5-FU per year excreted into wastewater in Europe [17]. The use of carriers (nanoparticles and vesicles) that facilitate an efficient delivery system for this drug helps to improve this situation [18][19][20], although the definitive solution to the problem is still far from being obtained.…”

Section: Introductionmentioning

confidence: 99%

“…Likewise, the use of liposomes as carriers/encapsulating agents of 5-FU has been extensively studied [30][31][32] to both improve its bioavailability and reduce side effects, as compared to traditional formulations used under the form of creams and/or emulsions [33][34][35], for topical use in the treatment of different skin diseases [19,36]. Lakkakula et al [20] found that 5-FU could be encapsulated in the cavity of 2HP-β-cyclodextrin, forming a stable inclusion complex, although they did not report the extent of such complex formation.…”

Section: Introductionmentioning

confidence: 99%

Complexation of 5-Fluorouracil with β-Cyclodextrin and Sodium Dodecyl Sulfate: A Useful Tool for Encapsulating and Removing This Polluting Drug

Cabral

Fernandes

Joaquim

et al. 2022

Toxics

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The formation of complexes of the drug 5-fluorouracil (5-FU) with β-cyclodextrin (β-CD) and sodium dodecyl sulphate (SDS) was studied through experimental measurements of the ternary mutual diffusion coefficients (D11, D22, D12, and D21) for the systems {5-FU (component 1) + β-CD (component 2) + water} and {5-FU (component 1) + SDS (component 2) + water} at 298.15 K and at concentrations up to 0.05 mol dm−3 by using the Taylor dispersion method, with the objective of removing this polluting drug from the residual systems in which it was present. The results found showed that a coupled diffusion of 5-FU occurred with both β-CD and SDS, as indicated by the nonzero values of the cross-diffusion coefficients, D12 and D21, as a consequence of the complex formation between 5-FU and the β-CD or SDS species. That is, 5-FU was solubilized (encapsulated) by both carriers, although to a greater extent with SDS (K = 20.0 (±0.5) mol−1 dm3) than with β-CD (K = 10.0 (±0.5) mol−1 dm3). Values of 0.107 and 0.190 were determined for the maximum fraction of 5-FU solubilized with β-CD and SDS (at concentrations above its CMC), respectively. This meant that SDS was more efficient at encapsulating and thus removing the 5-FU drug.

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5-Fluorouracil, innovative drug delivery systems to enhance bioavailability for topical use

Cited by 28 publications

References 72 publications

Mechanisms of Chemotherapy-Induced Neurotoxicity

Mechanisms of Chemotherapy-Induced Neurotoxicity

Fabrication of novel PNIPAM@GO microspheres loaded with dual drugs featuring on‐demand drug release capability

Complexation of 5-Fluorouracil with β-Cyclodextrin and Sodium Dodecyl Sulfate: A Useful Tool for Encapsulating and Removing This Polluting Drug

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