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Development of a li...
Development of a liposomal nanoparticle formulation of 5-Fluorouracil for parenteral administration : Formulation design, pharmacokinetics and efficacy
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- Thomas, Anitha M. (författare)
- Experimental Therapeutics, BC Cancer Agency, Vancouver, BC, Canada
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- Kapanen, Anita I. (författare)
- Experimental Therapeutics, BC Cancer Agency, Vancouver, BC, Canada
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- Hare, Jennifer I. (författare)
- Experimental Therapeutics, BC Cancer Agency, Vancouver, BC, Canada
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- Ramsay, Euan (författare)
- Center for Drug Research and Development, 364-2259 Lower Mall, Vancouver, BC, Canada
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- Edwards, Katarina (författare)
- Uppsala universitet,Fysikalisk kemi
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- Karlsson, Göran (författare)
- Uppsala universitet,Fysikalisk kemi
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- Bally, Marcel B. (författare)
- Faculty of Pharmaceutical Sciences, University of British Columbia, Canada
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(creator_code:org_t)
- Elsevier BV, 2011
- 2011
- Engelska.
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Ingår i: Journal of Controlled Release. - : Elsevier BV. - 0168-3659 .- 1873-4995. ; 150:2, s. 212-219
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 5-Fluorouracil (5-FU) is a small, very membrane permeable drug that is poorly retained within the aqueous compartment of liposomal nanoparticles (LNP). To address this problem a novel method relying on formation of a ternary complex comprising copper, low molecular weight polyethylenimine (PEI) and 5-FU has been developed. More specifically, in the presence of entrapped copper and PEI, externally added 5-FU can be efficiently encapsulated (>95%) in DSPC/Chol (1,2-Distearoyl-sn-Glycero-3-Phosphocholine/cholesterol; 55:45mol%) liposomes (130-170nm) to achieve drug-to-lipid ratios of 0.1 (mol:mol). Drug release studies completed using this LNP formulation of 5-FU demonstrated significant improvements in drug retention in vitro and in vivo. Plasma concentrations of 5-FU were 7- to 23-fold higher when the drug was administered intravenously to mice as the LNP 5-FU formulation compared to free 5-FU. Further, the therapeutic effects of the LNP 5-FU formulation, as determined in a HT-29 subcutaneous colorectal cancer model where treatment was given QDx5, was greater than that which could be achieved with free 5-FU when compared at equivalent doses. This is the first time an active loading method has been described for 5-FU. The use of ternary metal complexation strategy to encapsulate therapeutic agents may define a unique platform for preparation of LNP drug formulations.
Ämnesord
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Nyckelord
- Copper
- Polyethylenimine
- Complexation
- 5-fluorouracil
- Nanoparticle liposomes
- Colorectal cancer
- Chemistry
- Kemi
- Chemistry
- Kemi
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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