Enhancement of the bioavailability of an antihypertensive drug by transdermal protransfersomal system: formulation and in vivo study

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorMorsi N.M.
dc.contributor.authorAboelwafa A.A.
dc.contributor.authorDawoud M.H.S.
dc.contributor.otherDepartment of Pharmaceutics and Industrial Pharmacy
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherCairo
dc.contributor.otherEgypt; Department of Pharmaceutics
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University for Modern Sciences and Arts
dc.contributor.otherDokki
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:40:56Z
dc.date.available2020-01-09T20:40:56Z
dc.date.issued2018
dc.descriptionScopus
dc.descriptionMSA Google Scholar
dc.description.abstractTimolol Maleate (TiM), a nonselective ?-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from poor oral bioavailability (50%) due to its first pass effect and a short elimination half-life of 4 h; resulting in its frequent administration. Transdermal formulation may circumvent these problems in the form of protransfersomes. The aim of this study is to develop and optimize transdermal protransfersomal system of Timolol Maleate by film deposition on carrier method where protransfersomes were converted to transfersomes upon skin hydration following transdermal application under occlusive conditions. Two 2 3 full factorial designs were employed to investigate the influence of three formulation variables which were; phosphatidyl choline: surfactant molar ratio, carrier: mixture and the type of SAA each on particle size, drug entrapment efficiency and release rate. The optimized formulation was evaluated regarding permeation through hairless rat skin and compared with oral administration of aqueous solution on male Wistar rats. Optimized protransfersomal system had excellent permeation rate through shaved rat skin (780.69 ?g/cm 2 /h) and showed six times increase in relative bioavailability with prolonged plasma profile up to 72 h. A potential protransfresomal transdermal system was successfully developed and factorial design was found to be a smart tool in its optimization. � 2017 Informa UK Limited, trading as Taylor & Francis Group.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=23039&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1080/08982104.2017.1295989
dc.identifier.doiPubMed ID 28264602
dc.identifier.issn8982104
dc.identifier.otherhttps://doi.org/10.1080/08982104.2017.1295989
dc.identifier.otherPubMed ID 28264602
dc.identifier.urihttps://t.ly/py7xb
dc.language.isoEnglishen_US
dc.publisherTaylor and Francis Ltden_US
dc.relation.ispartofseriesJournal of Liposome Research
dc.relation.ispartofseries28
dc.subjectAntihypertensiveen_US
dc.subjectdesign-experten_US
dc.subjectliposomesen_US
dc.subjectpermeationen_US
dc.subjectultra-flexible vesiclesen_US
dc.subjectphosphatidylcholineen_US
dc.subjectsurfactanten_US
dc.subjecttimolol maleateen_US
dc.subjectantihypertensive agenten_US
dc.subjectdrug carrieren_US
dc.subjectliposomeen_US
dc.subjectnanoparticleen_US
dc.subjecttimololen_US
dc.subjectanimal cellen_US
dc.subjectanimal experimenten_US
dc.subjectanimal tissueen_US
dc.subjectarea under the curve ratioen_US
dc.subjectArticleen_US
dc.subjectdrug absorptionen_US
dc.subjectdrug bioavailabilityen_US
dc.subjectdrug determinationen_US
dc.subjectdrug formulationen_US
dc.subjectdrug penetrationen_US
dc.subjectelimination half-lifeen_US
dc.subjectfactorial designen_US
dc.subjecthigh performance liquid chromatographyen_US
dc.subjecthydrationen_US
dc.subjectin vitro studyen_US
dc.subjectin vivo studyen_US
dc.subjectlipid bilayeren_US
dc.subjectmaleen_US
dc.subjectmaximum plasma concentrationen_US
dc.subjectnonhumanen_US
dc.subjectparticle sizeen_US
dc.subjectpharmacokinetic parametersen_US
dc.subjectpriority journalen_US
dc.subjectquantitative analysisen_US
dc.subjectraten_US
dc.subjectsustained drug releaseen_US
dc.subjecttime to maximum plasma concentrationen_US
dc.subjecttransdermal drug administrationen_US
dc.subjecttransdermal protransfersomal systemen_US
dc.subjectanimalen_US
dc.subjectbioavailabilityen_US
dc.subjectchemistryen_US
dc.subjectcutaneous drug administrationen_US
dc.subjectdrug formulationen_US
dc.subjectdrug releaseen_US
dc.subjectmetabolismen_US
dc.subjectoral drug administrationen_US
dc.subjectproceduresen_US
dc.subjectskinen_US
dc.subjectskin absorptionen_US
dc.subjectsurface propertyen_US
dc.subjectWistar raten_US
dc.subjectAdministration, Cutaneousen_US
dc.subjectAdministration, Oralen_US
dc.subjectAnimalsen_US
dc.subjectAntihypertensive Agentsen_US
dc.subjectBiological Availabilityen_US
dc.subjectDrug Carriersen_US
dc.subjectDrug Compoundingen_US
dc.subjectDrug Liberationen_US
dc.subjectLiposomesen_US
dc.subjectMaleen_US
dc.subjectNanoparticlesen_US
dc.subjectParticle Sizeen_US
dc.subjectPhosphatidylcholinesen_US
dc.subjectRats, Wistaren_US
dc.subjectSkinen_US
dc.subjectSkin Absorptionen_US
dc.subjectSurface Propertiesen_US
dc.subjectSurface-Active Agentsen_US
dc.subjectTimololen_US
dc.titleEnhancement of the bioavailability of an antihypertensive drug by transdermal protransfersomal system: formulation and in vivo studyen_US
dc.typeArticleen_US
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