• Lipidsolutioninorganicphase;insulinsolutioninaqueousphase

• Mix,liposomeform,extrusiontoreducesize,dialysisor

• Diafiltrationtoeliminatetheorganicsandfreeinsulin

• Concentrateifnecessary

•

LIPOSOME DRUG DELIVERY SYSTEMS

Structure• Asphericalvesicleofphospholipid

bilayerswithaqueouscoreencapsulatesactivedrugs

• Increasecirculationtimeandbioavailability,reducetoxicity,targettospecificorgan/tissue

Surface Modification• Stealthliposome:PEGonthesurface

reducingtheproteinbinding,increasecirculationtime,andreducingtoxicity

• Targeting:peptides,antibodiesandsmallmoleculesonthesurfaceguidestheliposometothespecificsiteofaction

• Triggerrelease:theencapsulateddrugcanbereleasebyexternaltriggers,suchasUltrasound,light,pH,orglucose,etc.

Application• Commercialdrugs:SuchasAnti-cancer

drugDoxil;Anti-fungaldrugAmbisome;andAntiviralvaccineEpaxal,etc.

• Canencapsulatesmallmolecules,peptides,protein,siRNA,RNA,etcfordifferentindications

Case Study 1 - Preparation of Insulin-Encapsulated Liposome

Mixed,(extrusion),dialysis/diafiltration,concentrateifnecessary

Lipid, Cholesterol, DSPE-PEG 0.3 mg/ml insulin, size 300nm

Sample

Pump

Filtrate

InsulininAqueous

LipidMixtureAinOrganicSolvent

InsulinencapsulatedLiposome

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Case Study 2 - Preparation of Insulin-Encapsulated Functionalized Liposome

Case Study 3 - AVT preparation for the treatment of diabetes

• SynthesizedDSPE-PEG-functionalgroupcompoundsinhighyields

• Preparedsurfacefunctionalizedliposomewithencapsulatedinsulin,encapsulationefficiency>90%,insulinconcentration1mg/ml

insulin

Surface Functional Group

• AgglomerateVesicle(AVT)wasformedbytwotypesofliposomeswithfunctionalgroups(boronateanddiols)onthesurfacethatformcovalentchemicalbonds

• Insulinconcentration1mg/mlSize<100um

• GlucosecleavesAVT• Proprietarytechnologyof

SensulinLLC

AVT Formation

Glucose Cleaves AVT

T = 0, 48um T = 24 hours, 19um

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AVT as smart insulin delivery system. High glucose concentration will disassemble the AVT and release more insulin.

Liposome A

Liposome B

A-B AVT, 70um

LIPOSOME DRUG DELIVERY SYSTEMS