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1、NanoformulationsofadefovirdipivoxilDrugDevelopmentandIndustrialPharmacy,2012;EarlyOnline:1–11©2012InformaHealthcareUSA,Inc.S.Dodiyaetal.ISSN0363-9045print/ISSN1520-5762onlineDOI:10.3109/03639045.2012.694889DrugDevelopmentandIndustrialPharmacy2012ReseaRchaRtIcle00Solidlipidnanoparticlesandn
2、anosuspensionofadefovir00dipivoxilforbioavailabilityimprovement:formulation,1characterization,pharmacokineticandbiodistribution11studies01March2012ShamsunderDodiya1,SandipChavhan1,ArunaKorde2andKrutikaK.Sawant126April20121DrugDeliveryLaboratory,TIFACCentreofRelevanceandExcellenceinNDDS,Pha
3、rmacyDepartment,15May2012FacultyofTechnologyandEngineering,TheMaharajaSayajiraoUniversityofBaroda,Vadodara,Indiaand2RadiolabellingDivision,BhabhaAtomicResearchCentre,Mumbai,India0363-90451520-5762abstractThepresentstudywasaimedatdevelopingcolloidalformulationslikesolidlipidnanoparticles(SL
4、N)and©2012InformaHealthcareUSA,Inc.nanosuspension(NS)forimprovingbioavailabilityofadefovirdipivoxil(AD),anucleosidereversetranscriptaseinhibitorwhichdisplayspoororalbioavailability.SLNswerepreparedbysolventinjectionmethodwhileNSwaspreparedbypearlmillingmethod.Thepreparedformulationswerecha
5、racterizedforphysicochemicalparameters10.3109/03639045.2012.694889suchasparticlesize,ζpotential,drugcontent,X-rayDiffraction(XRD),DifferentialScanningCalorimetry(DSC).Pharmacokineticandbiodistributionstudieswereperformedinmicetoevaluateinvivofateoftheformulations.TheSLNsshowedparticlesizeo
6、f267±18nmandentrapmentefficiencyof73.5±2.12%.TheparticlesizeobtainedforNSwas393±13nmagainst710±70μmforbulkdrug,whichledtosignificantimprovementinsaturationsolubility.DSCandXRDstudiesofNSandSLNshowedreductionincrystallinitywhileinvitrostudiesshowedimproveddissolutionForpersonaluseonly.ratei
7、nbothcases.Pharmacokineticsstudiesoforallyadministeredformulationsinmiceexhibitedhigherplasmaconcentrationcomparedtoplaindrug.Biodistributionstudiesshowedhigheraccumulationofdruginliver,kidneys,intestineandstomach.ThehigherconcentrationofADinliverafter24hrhigh
