Development of a liposomal nanoparticle formulation of 5-Fluorouracil for parenteral administration: Formulation design, pharmacokinetics and efficacy

Thomas, Anitha; Kapanen, Anita; Hare, Jennifer I.; Ramsay, Euan; Edwards, Katarina; Karlsson, Göran; Bally, Marcel B.

doi:10.1016/j.jconrel.2010.11.018

Cited by 60 publications

(48 citation statements)

References 27 publications

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“…In addition, 5-FU treatments lead to the development of drug resistance by tumor cells, thereby requiring high doses that lead to severe side effects, including gastrointestinal, haematological, neuronal and dermatological effects, pancytopenia, and cardiotoxicity (13). To overcome these limitations, 5-FU has been encapsulated into liposomes to prolong its circulation time, reduce the associated side effects, improve its therapeutic index and efficacy, and favor drug accumulation into tumors thanks to the enhanced permeation and retention effect (14)(15)(16)(17)(18).…”

Section: Introductionmentioning

confidence: 99%

Formulation and Pharmacokinetics of Thermosensitive Stealth® Liposomes Encapsulating 5-Fluorouracil

et al. 2014

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Section: Introductionmentioning

confidence: 99%

Formulation and Pharmacokinetics of Thermosensitive Stealth® Liposomes Encapsulating 5-Fluorouracil

et al. 2014

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“…The dermal/transdermal permeation of 5-FU through highly lipophilic human stratum corneum is too low because of its hydrophilic characteristics. Therefore, many attempts namely microemulsions (Gupta et al, 2005;Elmeshad & Tadros, 2011), transferosomes (Alvi et al, 2011), ethosomes (Zhang et al, 2012), niosomes (Cosco et al, 2009;Alvi et al, 2011), liposomes (Alvi et al, 2011;Thomas et al, 2011), nanoparticles (Zhu et al, 2009;Chauhan et al, 2012), iontophoresis (Fang et al, 2004;Singh & Jayaswal, 2008), phonophoresis (Meidan et al, 1999), electroporation (Fang et al, 2004) and use of chemical enhancers (Singh et al, 2005;Khan et al, 2011) have been made to increase transdermal/topical delivery of 5-FU. In the recent literatures, oil based nanocarriers like nanoemulsions and microemulsions showed significant advantages over other unstable dispersion like emulsions and suspensions in terms of enhanced solubilization, enhanced permeation, enhanced bioavailability and thermodynamic stability for transdermal/ topical delivery of many lipophilic drugs both in vitro as well as in vivo (Spernath et al, 2007;Elmaghraby, 2008;Hwangl et al, 2009;Shakeel et al, 2009Shakeel et al, , 2012Shakeel & Ramadan, 2010;Raza et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Chemoprevention of skin cancer using low HLB surfactant nanoemulsion of 5-fluorouracil: a preliminary study

et al. 2013

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Oral delivery of 5-fluorouracil (5-FU) is difficult due to its serious adverse effects and extremely low bioavailability. Therefore, the aim of present investigation was to develop and evaluate low HLB surfactant nanoemulsion of 5-FU for topical chemoprevention of skin cancer. Low HLB surfactant nanoemulsions were prepared by oil phase titration method. Thermodynamically stable nanoemulsions were characterized in terms of droplet size distribution, zeta potential, viscosity and refractive index. Selected formulations and control were subjected to in vitro skin permeation studies through rat skin using Franz diffusion cells. Optimized formulation F9 was subjected to stability and in vitro cytotoxic studies on melanoma cell lines. Enhancement ratio was found to be 22.33 in formulation F9 compared with control and other formulations. The values of steady state flux and permeability coefficient for formulation F9 were found to be 206.40 AE 14.56 mg cm À2 h À1 and 2.064 Â 10 À2 AE 0.050 Â 10 À2 cm h À1, respectively. Optimized formulation F9 was found to be physical stable. In vitro cytotoxicity studies on SK-MEL-5 cancer cells indicated that 5-FU in optimized nanoemulsion is much more efficacious than free 5-FU. From these results, it can be concluded that the developed nanoemulsion might be a promising vehicle for chemoprevention of skin cancer.

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“…One kind is chemical modification, such as synthesis of low molecular weight 5-FU derivatives, 24 conjugation with polymeric materials, 25 conjugation with peptide, 26 or modification with palmitic acid. 22 The other kind is based on nanocarriers, such as liposomes, 27 nanoparticles, 28 micelles, 29,30 and SLN. 31 Combining the advantages of these two strategies, we designed a novel platform: lipid prodrug NLC to codeliver 5-FU and CDDP.…”

Section: Introductionmentioning

confidence: 99%

Engineering of lipid prodrug-based, hyaluronic acid-decorated nanostructured lipid carriers platform for 5-fluorouracil and cisplatin combination gastric cancer therapy

Qu¹,

Zhou²,

Chen³

et al. 2015

IJN

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Purpose The first-line chemotherapy treatment protocol for gastric cancer is combination chemotherapy of 5-fluorouracil (5-FU) and cisplatin (CDDP). The aim of this study was to engineer prodrug-based nanostructured lipid carriers (NLC) platform for codelivery of 5-FU and CDDP to enhance therapy and decrease toxicity. Methods First, 5-FU-stearic acid lipid conjugate was synthesized by two steps. Second, 5-FU-stearic acid prodrug and CDDP were loaded in NLC. Finally, hyaluronic acid (HA) was coated onto NLC surface. Average size, zeta potential, and drug loading capacity of NLC were evaluated. Human gastric cancer cell line BGC823 (BGC823 cells) was used for the testing of in vitro cytotoxicity assays. In vivo antitumor activity of NLC was evaluated in mice bearing BGC823 cells model. Results HA-coated 5-FU-stearic acid prodrug and CDDP-loaded NLC (HA-FU/C-NLC) showed a synergistic effect in combination therapy and displayed the greatest antitumor activity than all of the free drugs or uncoated NLC in vitro and in vivo. Conclusion This work reveals that HA-coated NLC could be used as a novel carrier to code-liver 5-FU and CDDP for gastric cancer therapy. HA-FU/C-NLC could be a promising targeted and combinational therapy in nanomedicine.

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Development of a liposomal nanoparticle formulation of 5-Fluorouracil for parenteral administration: Formulation design, pharmacokinetics and efficacy

Cited by 60 publications

References 27 publications

Formulation and Pharmacokinetics of Thermosensitive Stealth® Liposomes Encapsulating 5-Fluorouracil

Formulation and Pharmacokinetics of Thermosensitive Stealth® Liposomes Encapsulating 5-Fluorouracil

Chemoprevention of skin cancer using low HLB surfactant nanoemulsion of 5-fluorouracil: a preliminary study

Engineering of lipid prodrug-based, hyaluronic acid-decorated nanostructured lipid carriers platform for 5-fluorouracil and cisplatin combination gastric cancer therapy

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