Repaglinide-loaded long-circulating biodegradable nanoparticles_ Rational approach for the management of type 2 diabetes mellitus英文资料

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1、JournalofDiabetes1(2009)29–35ORIGINALARTICLERepaglinide-loadedlong-circulatingbiodegradablenanoparticles:Rationalapproachforthemanagementoftype2diabetesmellitusSheleshJAINandSwarnlataSARAFInstituteofPharmacy,PanditRavishankarShuklaUniversity,Raipur,IndiaCorrespondenceAbstractSwarnla

2、taSaraf,InstituteofPharmacy,PanditRavishankarShuklaUniversity,Background:Repaglinide(RPG)isanoralhypoglycemicagentwithexcel-Raipur492010,Chhattisgarh,India.lentbioavailability(90–98%)andashortplasmahalf-life(2–6h).AfullTel:+917712262832doseofRPGisrequiredbeforeeachmeal;hence,therapy

3、maybecomeFax:+917712262832inconvenient.Thus,theaimofthepresentstudywastodesignanovelEmail:swarnlatasaraf@gmail.comdeliverysystemtomaintainpeakplasmalevelsofRPGforthelong-termmanagementofdiabetesmellitus.Received8April2008;revised21SeptemberMethods:Twonanoparticleformulationswereprep

4、aredbycombining2008;accepted4October2008.RPGwithpoly(lactic-co-glycolic)acidaloneorasacopolymerwithmeth-doi:10.1111/j.1753-0407.2008.00001.xoxypolyethyleneglycol(RPGNP1andRPGNP2,respectively);bothformu-lationsweresubjectedtoinvitroandinvivocharacterization.Invivocharacterizationwasp

5、erformedinastreptozotocin(STZ)-induceddiabeticmalealbinorats.Results:ThemeanparticlesizeoftheRPGNP1andRPGNP2formula-tionswas387.8±11.9and310.2±12.4nm,respectively,withazetapotentialof)27.4±0.7and)15.7±0.5mV,respectively.TheentrapmentefficiencyanddrugcontentofRPGNP1(58.7±1.3%and27.4±2

6、.3%,respectively)wasbetterthanthatofRPGNP2(45.8±1.2%and24.3±1.1%,respectively).BloodglucoselevelsofRPGNP1-andRPGNP2-treatedSTZ-diabeticratswerereducedsignificantly(tonormallevels)comparedwithuntreatedSTZ-diabeticrats(P<0.05),buttherewasnodifferencebetweenthetwotreatmentgroups(P>0.05)

7、.However,whereasRPGNP1waseffectiveforaperiodofonly24h,RPGNP2waseffectiveforupto1week.Conclusions:TheresultsofthepresentstudyshowthatRPGNP2effec-tivelymanagestype2diabetesmellitusforupto1week.Surface-modifiedNPscouldbeusedtoimprovepatientcompliancewithdrugtreatmentasaresultofdecreased

8、dosingfrequency.Key