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dc.contributor.authorSun, Hsienen_US
dc.contributor.authorSeshadri, Madhumathien_US
dc.contributor.authorLingard, Scotten_US
dc.contributor.authorMonaghan, Wayneen_US
dc.contributor.authorFaoagali, Joanen_US
dc.contributor.authorChan, Enochen_US
dc.contributor.authorMcDonald, Helenen_US
dc.contributor.authorHouston, Todden_US
dc.contributor.authorKing, Michelleen_US
dc.contributor.authorPeak, Ianen_US
dc.contributor.authorWilson, Jennyen_US
dc.contributor.authorHaywood, Alisonen_US
dc.contributor.authorSpencer, Briohnyen_US
dc.contributor.authorDunn, Perreaen_US
dc.contributor.authorGrant, Garyen_US
dc.date.accessioned2017-05-03T14:33:34Z
dc.date.available2017-05-03T14:33:34Z
dc.date.issued2011en_US
dc.date.modified2012-06-07T21:55:29Z
dc.identifier.issn1948982Xen_US
dc.identifier.doi10.3844/ajmsp.2011.1.8en_US
dc.identifier.urihttp://hdl.handle.net/10072/42966
dc.description.abstractAbstract: Problem statement: Cyclodextrin complexation has previously been shown to improve the solubility and dissolution properties of trimethoprim; however, no report provides an account of the effect cyclodextrin complexation has on the antibacterial activity of this agent. Approach: b-cyclodextrin and 2-hydroxypropyl b-cyclodextrin inclusion complexes of trimethoprim were prepared and confirmed by differential scanning calorimetry and proton nuclear magnetic resonance. The in-vitro antibacterial activity, in terms of minimum inhibitory concentrations, of cyclodextrin-drug complexes were compared to uncomplexed free trimethoprim by a broth-microdilution method against several sensitive and resistant Gram-positive and Gram-negative bacteria. The effect of complexation on the apparent permeability coefficients was also determined using a Caco-2 permeability assay to account for potential alterations in bioavailability that could influence in-vivo antibacterial activity. Results: Inclusion complexation of trimethoprim with both unsubstituted and hydroxylated versions of b-cyclodextrin produced a reduction in the MIC80 required to inhibit the growth of S. aureus ATCC 29213, S. pneumoniae ATCC 4961, S.epidermidis ATCC 14990 and E. coli ATCC 25922 (p>0.05). The effect was limited to bacteria normally susceptible to trimethoprim. Neither complex negatively affected the antibacterial activity of trimethoprim. Hydroxypropyl-b-cyclodextrin and b-cyclodextrin inclusion complexes significantly (p<0.01) increased the apparent intestinal permeability of trimethoprim by 39.8 and 56.1%, respectively. Considering the effect cyclodextrin inclusion complexation has on the antibacterial activity of trimethoprim, the improved intestinal permeability of these complexes has the potential to improve the in-vivo antibacterial activity of the agent by enhancing the steady-state concentration of the drug when dosed orally. Conclusion: These results would suggest that physical complexation with either of these cyclodextrins would provide a feasible strategy to improve the pharmaceutical and pharmacokinetic properties of trimethoprim.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_US
dc.format.extent146765 bytes
dc.format.mimetypeapplication/pdf
dc.languageEnglishen_US
dc.language.isoen_US
dc.publisherScience Publicationsen_US
dc.publisher.placeUnited Statesen_US
dc.relation.ispartofstudentpublicationYen_US
dc.relation.ispartofpagefrom1en_US
dc.relation.ispartofpageto8en_US
dc.relation.ispartofissue1en_US
dc.relation.ispartofjournalAmerican Journal of Microbiologyen_US
dc.relation.ispartofvolume2en_US
dc.rights.retentionYen_US
dc.subject.fieldofresearchBiological Sciences not elsewhere classifieden_US
dc.subject.fieldofresearchcode069999en_US
dc.titleAntibacterial Activity of b-Cyclodextrin and 2-Hydroxypropyl-b-Cyclodextrin Trimethoprim Complexesen_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.facultyGriffith Health, School of Pharmacyen_US
gro.rights.copyrightCopyright remains with the authors 2011. The attached file is reproduced here in accordance with the copyright policy of the publisher. For information about this journal please refer to the journal’s website or contact the authors.en_US
gro.date.issued2011
gro.hasfulltextFull Text


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