Preparation and evaluation of inhalable itraconazole chitosan based polymeric micelles 英文参考文献.docVIP
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Preparation and evaluation of inhalable itraconazole chitosan based polymeric micelles 英文参考文献
Moazenietal.DARUJournalofPharmaceuticalSciences2012,20:85
/content/20/1/85
RESEARCH ARTICLE
OpenAccess
Preparationandevaluationofinhalable
itraconazolechitosanbasedpolymericmicelles
EsmaeilMoazeni1,KambizGilani1*,AbdolhosseinRouholaminiNajafabadi1,MohamadrezaRouini2,NasirMohajel1,
MohsenAmini3andMohammadAliBarghi4
Abstract
Background:Thisstudyevaluatedthepotentialofchitosanbasedpolymericmicellesasananocarriersystemfor
pulmonarydeliveryofitraconazole(ITRA).
Methods:Hydrophobicallymodifiedchitosanweresynthesizedbyconjugationofstearicacidtothehydrophilic
depolymerizedchitosan.FTIRand 1HNMRwereusedtoprovethechemicalstructureandphysicalpropertiesofthe
depolymerizedandthestearicacidgraftedchitosan.ITRAwasentrappedintothemicellesandphysicochemical
propertiesofthemicelleswereinvestigated.Fluorescencespectroscopy,dynamiclaserlightscatteringand
transmissionelectronmicroscopywereusedtocharacterizethephysicochemicalpropertiesoftheprepared
micelles.Theinvitropulmonaryprofileofpolymericmicelleswasstudiedbyanair-jetnebulizerconnectedtoa
twinstageimpinger.
Results:Thepolymericmicellespreparedinthisstudycouldentrapupto43.2±2.27μgofITRApermilliliter.All
micellesshowedmeandiameterbetween120–200nm.Thecriticalmicelleconcentrationofthestearicacidgrafted
chitosanwasfoundtobe1.58×10-2mg/ml.Thenebulizationefficiencywasupto89%andthefineparticlefraction
(FPF)variedfrom38%to47%.Themicelleshadenoughstabilitytoremainencapsulationofthedrugduring
nebulizationprocess.
Conclusions:Invitrodatashowedthatstearicacidgraftedchitosanbasedpolymericmicelleshasapotentialtobe
usedasnanocarriersfordeliveryofitraconazolethroughinhalation.
Keywords:Polymericmicelles,Itraconazole,Chitosan,Nebulization,Pulmonarydrugdelivery
Background
While amphotericin is an effective drug for treatment
Invasive pulmonary fungal infection is major infectious offungalinfections,itsadverseeffectsreducesitspoten-
diseaseamongimmunosuppressedpatients.Difficultyof tialusesandparticularinteresthasbeenfocusedonthe
early clinica
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