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dc.creatorĐekić, Ljiljana
dc.creatorMarković, Bojan
dc.creatorMicov, Ana
dc.creatorTomić, Maja
dc.creatorPecikoza, Uroš
dc.creatorStepanović-Petrović, Radica
dc.date.accessioned2020-06-03T10:17:50Z
dc.date.available2020-06-03T10:17:50Z
dc.date.issued2020
dc.identifier.issn2190-393X
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/3589
dc.description.abstractThe study focused on formulation of carmellose sodium hydrogels and nonionic microemulsions with 5% and 10% of levetiracetam and investigation of drug concentration influence on their physicochemical characteristics and in-use stability as well as influence of drug concentration and carrier type on in vitro drug release and in vivo antihyperalgesic/antiedematous activity in a rat model of localized (intraplantar) carrageenan-induced inflammation. Hydrogels were pseudoplastic semisolids with thixotropy and pH 7.37–7.58. Microemulsions were low viscous Newtonian nanodispersions of oil droplets (13.11–15.11 nm) in water, with pH 4.01–4.64. Physical stability of the investigated systems was preserved over the 3-month storage under ambient conditions. Levetiracetam release followed zero order and Korsmeyer-Peppas models (R2 ≥ 0.99) reflecting the combined effects of drug concentration and carrier viscosity. All levetiracetam-loaded formulations produced significant reduction of hyperalgesia and paw swelling induced by carrageenan (p < 0.001). Their efficacy in exerting antihyperalgesic activity was significantly higher than that observed with the reference 5% ibuprofen hydrogel preparation (up to 6 h) (p < 0.001), while antiedematous activity was comparable with the reference product. No erythema and visible blood vessels were observed in a rat ear test. The study demonstrated percutaneous delivery of levetiracetam as useful and safe therapeutic option for localized inflammatory pain with potential to overcome the insufficient efficacy of topically applied nonsteroidal anti-inflammatory drugs in the form of a hydrogel. [Figure not available: see fulltext.]. © 2020, Controlled Release Society.
dc.publisherSpringer
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/146010/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175045/RS//
dc.rightsrestrictedAccess
dc.sourceDrug Delivery and Translational Research
dc.subjectAntihyperalgesic/antiedematous efficacy
dc.subjectHydrogel
dc.subjectLevetiracetam
dc.subjectMicroemulsion
dc.subjectPercutaneous delivery
dc.subjectAntihyperalgesic/antiedematous efficacy
dc.subjectHydrogel
dc.subjectLevetiracetam
dc.subjectMicroemulsion
dc.subjectPercutaneous delivery
dc.titlePercutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization
dc.typearticle
dc.rights.licenseARR
dcterms.abstractМицов, Aна; Марковић, Бојан; Пецикоза, Урош; Ђекић, Љиљана; Степановић-Петровић, Радица; Томић, Маја;
dc.identifier.wos000535379400001
dc.identifier.doi10.1007/s13346-020-00787-4
dc.identifier.scopus2-s2.0-85085338096
dc.type.versionpublishedVersion


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