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dc.contributor.authorKhengar, R. H.
dc.contributor.authorJones, S. A.
dc.contributor.authorTurner, R. B.
dc.contributor.authorForbes, B.
dc.contributor.authorBrown, Marc
dc.date.accessioned2013-09-02T12:45:00Z
dc.date.available2013-09-02T12:45:00Z
dc.date.issued2007-12
dc.identifier.citationKhengar , R H , Jones , S A , Turner , R B , Forbes , B & Brown , M 2007 , ' Nail swelling as a pre-formulation screen for the selection and optimisation of ungual penetration enhancers ' , Pharmaceutical Research , vol. 24 , no. 12 , pp. 2207-2212 . https://doi.org/10.1007/s11095-007-9368-3
dc.identifier.issn0724-8741
dc.identifier.otherPURE: 627668
dc.identifier.otherPURE UUID: 83c1b2ff-438e-49e2-bbd0-3453f5a81c07
dc.identifier.otherWOS: 000250722500004
dc.identifier.otherScopus: 35948959948
dc.identifier.urihttp://hdl.handle.net/2299/11470
dc.description.abstractIntroduction. Targeting drug treatment to fungal infections that reside within or below the nail plate is problematic due to the highly restrictive barrier of the human nail. To optimise topical formulations for ungual drug delivery, inclusion of an effective penetration enhancer (PE) is imperative. At present, in vitro nail permeation studies can take weeks or months in order to obtain any meaningful data because the lack of a simple in vitro model to identify and develop nail PEs makes the selection and optimisation of novel PEs an empirical and inefficient process. The aim of this study was to compare three methods for pre-formulation screening of putative ungual PEs and then to select the most suitable technique for screening candidates that may enhance the permeation of therapeutic agents through the human nail. Methods. Three screening techniques were evaluated; nail swelling (weight increase of human nail clippings), horse hoof swelling (weight increase of horse hoof clippings) and nail penetration of a radiolabelled permeability probe. Four test PEs were evaluated using each screening method and nail swelling was identified as a simple, rapid, economic, relevant and reliable technique. This screen was then used to evaluate 20 potential PEs. Thioglycolic acid (TA), hydrogen peroxide (H2O2) and urea H2O2 produced the greatest nail weight increases; 71.0 +/- 4.6%, 69.2 +/- 6.6%, and 69.0 +/- 9.9 respectively. To confirm the relationship between human nail swelling and altered ungual barrier function, a permeation study was performed in human nails using caffeine as a model penetrant. Results and Discussion. Human nails pre-treated with TA in vitro had a 3.8-fold increase in caffeine flux compared to the control (TA-free solution). This study illustrated the potential to use human nail clipping swelling as a surrogate marker of PE activity for topical ungual drug delivery.en
dc.format.extent6
dc.language.isoeng
dc.relation.ispartofPharmaceutical Research
dc.subjectnail
dc.subjectonychomycosis
dc.subjectpenetration enhancers
dc.subjectungual
dc.subjectwater uptake
dc.subjectPHYSICOCHEMICAL CHARACTERIZATION
dc.subjectPERCUTANEOUS-ABSORPTION
dc.subjectHOMOLOGOUS ALCOHOLS
dc.subjectPERMEATION
dc.subjectPLATE
dc.subjectWATER
dc.subjectONYCHOMYCOSIS
dc.subjectCICLOPIROX
dc.subjectHAIR
dc.subjectPERMEABILITY
dc.titleNail swelling as a pre-formulation screen for the selection and optimisation of ungual penetration enhancersen
dc.contributor.institutionDepartment of Pharmacy
dc.contributor.institutionSchool of Life and Medical Sciences
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.contributor.institutionCentre for Research into Topical Drug Delivery and Toxicology
dc.contributor.institutionPharmaceutics
dc.contributor.institutionSkin and Nail Group
dc.contributor.institutionAirway Group
dc.contributor.institutionBioadhesive Drug Delivery Group
dc.contributor.institutionNanopharmaceutics
dc.contributor.institutionPharmaceutical Analysis and Product Characterisation
dc.description.statusPeer reviewed
dc.relation.schoolSchool of Life and Medical Sciences
dcterms.dateAccepted2007-12
rioxxterms.versionofrecordhttps://doi.org/10.1007/s11095-007-9368-3
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


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