Sustained release of 5-fluorouracil from polymeric nanoparticles

P. A. McCarron, A. D. Woolfson, S. M. Keating

Research output: Contribution to journalArticle

60 Citations (Scopus)

Abstract

The use of biodegradable nanoparticles loaded with 5-fluorouracil was investigated as a potential means to sustain the release of this drug. Nanoparticles prepared from four biodegradable polymers were loaded with 5-fluorouracil using three loading concentrations of drug and three different concentrations of added polymer. Washing particles using a centrifugation/re-suspension with ultrasound protocol was found to dislodge the majority of drug, resulting in an over-estimation of incorporation efficiency and low levels of strongly entrapped drug. Increasing the initial 5-fluorouracil concentration before polymer/monomer addition increased the drug loading in both washed and unwashed particles. Increasing the amount of polymer used to make nanoparticles did not increase loadings, but did produce increased amounts of unusable polymer waste. Drug release from nanoparticles was evaluated using a Franz cell diffusion apparatus, which showed an initial burst effect followed by a slower release phase over 24 h. Indeed, nanoparticles prepared from poly(lactide-co-glycolide) released 66% of their 5-fluorouracil payload over this period. It was concluded that 5-fluorouracil-loaded nanoparticles could be readily included into a hydrogel-based delivery system to provide sustained drug release for trans-epithelial drug-delivery applications.
LanguageEnglish
Pages1451-1459
JournalJOURNAL OF PHARMACY AND PHARMACOLOGY
Volume52
Issue number12
DOIs
Publication statusPublished - 1 Dec 2000

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Fluorouracil
Nanoparticles
Pharmaceutical Preparations
Polymers
Polyglactin 910
Biodegradable polymers
Centrifugation
Hydrogel
Drug delivery
Washing
Suspensions
Monomers
Ultrasonics

Cite this

McCarron, P. A. ; Woolfson, A. D. ; Keating, S. M. / Sustained release of 5-fluorouracil from polymeric nanoparticles. In: JOURNAL OF PHARMACY AND PHARMACOLOGY. 2000 ; Vol. 52, No. 12. pp. 1451-1459.
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Sustained release of 5-fluorouracil from polymeric nanoparticles. / McCarron, P. A.; Woolfson, A. D.; Keating, S. M.

In: JOURNAL OF PHARMACY AND PHARMACOLOGY, Vol. 52, No. 12, 01.12.2000, p. 1451-1459.

Research output: Contribution to journalArticle

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AB - The use of biodegradable nanoparticles loaded with 5-fluorouracil was investigated as a potential means to sustain the release of this drug. Nanoparticles prepared from four biodegradable polymers were loaded with 5-fluorouracil using three loading concentrations of drug and three different concentrations of added polymer. Washing particles using a centrifugation/re-suspension with ultrasound protocol was found to dislodge the majority of drug, resulting in an over-estimation of incorporation efficiency and low levels of strongly entrapped drug. Increasing the initial 5-fluorouracil concentration before polymer/monomer addition increased the drug loading in both washed and unwashed particles. Increasing the amount of polymer used to make nanoparticles did not increase loadings, but did produce increased amounts of unusable polymer waste. Drug release from nanoparticles was evaluated using a Franz cell diffusion apparatus, which showed an initial burst effect followed by a slower release phase over 24 h. Indeed, nanoparticles prepared from poly(lactide-co-glycolide) released 66% of their 5-fluorouracil payload over this period. It was concluded that 5-fluorouracil-loaded nanoparticles could be readily included into a hydrogel-based delivery system to provide sustained drug release for trans-epithelial drug-delivery applications.

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