Enhanced drug loading efficiency of contact lenses via salt-induced modulation - 论文 

AsianJournalofPharmaceuticalSciences14(2019)204–215

Availableonlineatwww.sciencedirect.comjournalhomepage:www.elsevier.com/locate/AJPSOriginalResearchPaper

Enhanceddrugloadingefficiencyofcontactlensesviasalt-inducedmodulation

QiangZhu,ShiruiMao?

SchoolofPharmacy,ShenyangPharmaceuticalUniversity,No.103,WenhuaRoad,Shenyang110016,China

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infoabstract

Lowdrugloadingefficiencyisoneofthemainobstacleshinderingtheapplicationofcontactlenses(CLs)asthecarrierforextendedoculardrugdelivery.Hereinthisstudy,asimpleandeffectivedrugloadingmethodbasedonsaltinducedmodulationwasproposedanddemon-stratedwithmechanismelucidation.Firstofall,usingpoly(2-hydroxyethylmethacrylate)(p-HEMA)asthecontactlensmaterial,betaxololhydrochloride,DiclofenacSodiumandBe-taxololBaseasthemodeldrugswithdifferentsolubility,influenceofsaltconcentration,salttype(sodiumsaltsofsulfate,chloride,andsulfocyanate)anddrugpropertiesintheloadingsolutionondrugloadingefficiencywasinvestigated.Mechanismofenhanceddrugloadingincontactlenswasfurtherexploredviastudyingtheinfluenceofsaltontheab-sorptionisotherm,drugsolubilityandwatercontentofCLs.ApplicabilityofthismethodtootherCLsmaterialswasalsoinvestigated.ItwasdemonstratedthatadjustingtheionicstrengthofloadingsolutionsresultedinsignificantincreaseofdrugloadinginCLs.Typeandconcentrationofthesaltsandsolubilityofthedrugwerethemainfactorsinfluencingenhancementratioofdrugloading.Themechanismforimproveddrugloadingwasrelatedtothereduceddrugsolubilityinloadingsolutionsandthereducedboundwatercontentincontactlenses.ModulationofdrugloadingbyadjustingionicstrengthwasalsoapplicabletootherCLsandthelighttransmittancewasnotaffected.Thismethodwasmoresuitableforsalt-formdrugswithhighsolubility.Insummary,adjustingionicstrengthofloadingso-lutionisaneconomicalandeffectivewaytoimprovedrugloadinginCLs,andthissimplemethodmayalsofindapplicationinotherhydrogelbaseddrugdeliverysystems.

?2018ShenyangPharmaceuticalUniversity.PublishedbyElsevierB.V.

ThisisanopenaccessarticleundertheCCBY-NC-NDlicense.

(http://creativecommons.org/licenses/by-nc-nd/4.0/)

Received26December2017Revised28March2018Accepted17May2018Availableonline1June2018Keywords:ContactlensesDrugloadingIonicstrengthAbsorptionisothermsDrugsolubilityBoundwatercontent

1.Introduction

Topicaldeliveryisthemostacceptedrouteofoculardrugap-plicationforitssimplicityandaffordableprice.Itisoftenusedtotreatanteriorsegmentdiseasessuchasglaucoma,dryeye,

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trachoma,althoughsomestudieshaveprovedthatdrugscanreachposteriorsegmentoftheeyethroughtopicalroute[1].Atpresentapproximately90%ofaqueousophthalmicformu-lationsareusedinthisway.However,drugsinstilledaseyedropsusuallyhavealowbioavailabilitylessthan5%dueto

Correspondingauthor.SchoolofPharmacy,ShenyangPharmaceuticalUniversity,No.103,WenhuaRoad,Shenyang110016,China.Tel.:+86-24-23986358.

E-mailaddress:maoshirui@syphu.edu.cn(S.Mao).

PeerreviewunderresponsibilityofShenyangPharmaceuticalUniversity.https://doi.org/10.1016/j.ajps.2018.05.002

1818-0876/?2018ShenyangPharmaceuticalUniversity.PublishedbyElsevierB.V.ThisisanopenaccessarticleundertheCCBY-NC-NDlicense.(http://creativecommons.org/licenses/by-nc-nd/4.0/)