STAVUDINEGASTRO-RETENTIVEMICROSPHERESOFDGALACTURONICACID SODIUM:FORMULATION,CHARACTERIZATION,INVITRO ANDINVIVOEVALUATION
DOI:
https://doi.org/10.48047/Keywords:
:Stavudine,Gastro-retentivemicrospheres,Ionotropicgelationmethod,Dgalacturonicacidsodium,Sodiumalginate,Guargum, Locust bean gum, Xanthan gumAbstract
Theprimeobjectiveofthepresentstudywastoformulatesustainedreleasemicrospheresofstavudinewhichwillretarddru
greleasefromdosageform,reducesthefrequencyofdrugadministration,minimizingtheadverseeffectstherebyincreasi
ngthepatientcompliance.Sustainedreleasemicrospheresofstavudine(STV),theFDAapproveddrugforthetreatmentofHIVinfections,areadministeredeitheraloneorincombinationwithotherantiretroviral
agents.STVistypicallyadministeredorallyasacapsuleandanoralsolution.ThesideeffectsofSTVaredosedependentan
dareductionofthetotaladministereddosereducestheseverityofthetoxicity.Microencapsulationimprovesthedrugabso
rptionandminimizessideeffectsduetothelocalizedbuildupofdrugsagainstthegastrointestinalmucosa.Sustainedreleas
emicrosphereswerepreparedbyionotropicgelationmethodusingDGalacturonicacidsodium(sodiumalginate)andnaturalpolymerssuchasguargum,locustgumandxanthangum.Thesem
icrosphereswereevaluatedforyield,entrapmentefficiency,andinvitroreleasekineticsandIinvivopharmacokineticstud
ies.FT-IR and DSC results proved that there was no interaction found between drug and polymer. Scanning
electron microscopy results of optimized microspheres showed discrete, spherical microspheres.
Theresultsshowedthatyield,entrapmentefficiencywasinfluencedbypolymerconcentrationandstirringspeed.Results
oftheinvitrostudyshowedthatthedesiredreleaseratewasachievedbyMF4formulationreleasingdrugupto12h.
