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1、Nanotechnology Based Drug DeliveryDr. Basavaraj K. Nanjwade M.Pharm., Ph.DAssociate ProfessorDepartment of PharmaceuticsJN Medical CollegeKLE UniversityBelgaum-59001020/03/20081anotechnologybaseddrugdelivery纳米药物递送ApplicationsofNanotechnology20/03/20082anotechnologybaseddrugdelivery纳米药物递送TargetedDrug
2、Delivery20/03/20083anotechnologybaseddrugdelivery纳米药物递送NanoparticlesforDrugDeliveryMetal-basednanoparticlesLipid-basednanoparticlesPolymer-basednanoparticlesBiologicalnanoparticles20/03/20084anotechnologybaseddrugdelivery纳米药物递送NanobiopharmaceuticalsIn In biopharmaceuticals, biopharmaceuticals, in in
3、 addition addition to to the the main main technologies technologies covered-liposomal, covered-liposomal, monoclonal monoclonal antibody-based, antibody-based, and and polymer-polymer-based based technologies technologies host host of of newer newer technologies technologies such such as as nanopar
4、ticles nanoparticles including including various various nanodimensional nanodimensional entities entities such such as as molecular molecular imprinted imprinted polymers, polymers, metallofullerenes, metallofullerenes, prodrug prodrug delivery, delivery, oral, oral, injectable injectable and and i
5、mplantable, implantable, pulmonary, pulmonary, and and transdermal transdermal and and transmucosal transmucosal delivery delivery have come up. have come up. 20/03/20085anotechnologybaseddrugdelivery纳米药物递送Drug Delivery Technology Important to Pharma Industry Drug Drug delivery delivery formulations
6、 formulations involve involve low low cost cost research research compared compared that that for for discovery discovery of of new molecule, new molecule, Minimizing Minimizing the the drug drug use use would would significantly significantly reduce reduce the the effective effective cost cost of o
7、f drug drug which which would give financial relief to the patients, would give financial relief to the patients, 20/03/20086anotechnologybaseddrugdelivery纳米药物递送 Delivery Delivery systems systems increase increase commercial commercial opportunity opportunity by by distinguishing distinguishing a a
8、drug drug from from competitive competitive threats threats posed posed by by “me “me too” too” drugs and drugs and Novel Novel means means of of delivery delivery particularly particularly using using nano-carriers, nano-carriers, can can allow allow branded branded drugs drugs to to be be rescued
9、rescued from from abyss abyss of of generic generic competition competition (may (may be be called called “resurrection “resurrection of of drug”). drug”). Drug Delivery Technology Important to Pharma Industry20/03/20087anotechnologybaseddrugdelivery纳米药物递送SOMESIGNIFICANTACHIEVEMENTSOFSOMESIGNIFICANT
10、ACHIEVEMENTSOFNANODEVICESNANODEVICES Development of one dose a day ciprofloxacin using Development of one dose a day ciprofloxacin using nanotechnologynanotechnology Tumor targeted taxol delivery using nanoparticles in Tumor targeted taxol delivery using nanoparticles in Phase 2 clinical trial stage
11、Phase 2 clinical trial stage Improved ophthalmic delivery formulation using Improved ophthalmic delivery formulation using smart hydrogel nanoparticlessmart hydrogel nanoparticles Oral insulin formulation using nanoparticles carriers.Oral insulin formulation using nanoparticles carriers. Liposomal b
12、ased Amphotericin B formulationLiposomal based Amphotericin B formulation20/03/20088anotechnologybaseddrugdelivery纳米药物递送CHALLENGES PreventionofdrugfrombiologicaldegradationPreventionofdrugfrombiologicaldegradation EffectiveTargetingEffectiveTargeting PatientCompliancePatientCompliance Costeffectiven
13、essCosteffectiveness ProductlifeextensionProductlifeextension20/03/20089anotechnologybaseddrugdelivery纳米药物递送PRIORITYAREAS Cancer NanotechnologyCancer Nanotechnology (i) (i) Diagnosis using Quantum Diagnosis using Quantum Dots Dots (ii) Tumor Targeted Delivery(ii) Tumor Targeted Delivery (iii) (iii)
14、ImagingImaging (iv) Cancer Gene Therapy (iv) Cancer Gene Therapy20/03/200810anotechnologybaseddrugdelivery纳米药物递送PRIORITYAREAS DNA Vaccines for parasitic, bacterial and DNA Vaccines for parasitic, bacterial and viral diseasesviral diseases Oral and pulmonary routes for systemic Oral and pulmonary rou
15、tes for systemic delivery of proteins and peptidesdelivery of proteins and peptides Nanotechnology in Tissue EngineeringNanotechnology in Tissue Engineering20/03/200811anotechnologybaseddrugdelivery纳米药物递送DrugDeliveryCarriers20/03/200812anotechnologybaseddrugdelivery纳米药物递送TargetingLigands20/03/200813
16、anotechnologybaseddrugdelivery纳米药物递送Liposomes20/03/200814anotechnologybaseddrugdelivery纳米药物递送Liposomes Theirexteriorlipidbilayerisverychemicallyreactive,therebyprovidingaTheirexteriorlipidbilayerisverychemicallyreactive,therebyprovidingameanstoconvenientlycouple“tags”onacovalentbasis.meanstoconvenie
17、ntlycouple“tags”onacovalentbasis. Such“tags”canbeantibodies,antigens,cellreceptors,nucleicacidSuch“tags”canbeantibodies,antigens,cellreceptors,nucleicacidprobes,etc.probes,etc. Thisprovidessignificantversatilityinassayformats(i.e.,immunoassay,Thisprovidessignificantversatilityinassayformats(i.e.,imm
18、unoassay,receptor-based,nucleicacidprobe,etc.)possible.receptor-based,nucleicacidprobe,etc.)possible. Withdiametersranginginsizefromapproximately50nmto800nm,Withdiametersranginginsizefromapproximately50nmto800nm,theiraqueouscoreencapsulatesuptomillionsofmoleculesofsignaltheiraqueouscoreencapsulatesu
19、ptomillionsofmoleculesofsignalgenerating“markers”thatcanbedetectedinavarietyofdifferentway.generating“markers”thatcanbedetectedinavarietyofdifferentway. AvarietyofdifferentencapsulantsarepossibleincludingvisuallyAvarietyofdifferentencapsulantsarepossibleincludingvisuallydetectabledyes(sincethelipidb
20、ilayeristransparent),opticallyanddetectabledyes(sincethelipidbilayeristransparent),opticallyandfluorometricallydetectabledyes,enzymes,andelectroactivecompounds.fluorometricallydetectabledyes,enzymes,andelectroactivecompounds. Thisprovidessignificantversatilityinthedetectionschemespossible.Thisprovid
21、essignificantversatilityinthedetectionschemespossible.20/03/200815anotechnologybaseddrugdelivery纳米药物递送Niosomes20/03/200816anotechnologybaseddrugdelivery纳米药物递送Niosomes Niosomes,non-ionicsurfactantvesicles,arewidelystudiedasanNiosomes,non-ionicsurfactantvesicles,arewidelystudiedasanalternativetoliposo
22、mesalternativetoliposomes ThesevesiclesappeartobesimilartoliposomesintermsoftheirThesevesiclesappeartobesimilartoliposomesintermsoftheirphysicalpropertiesphysicalproperties TheyarealsopreparedinthesamewayandunderavarietyofTheyarealsopreparedinthesamewayandunderavarietyofconditions,fromunilamellarorm
23、ultilamellarstructures.conditions,fromunilamellarormultilamellarstructures. Niosomesalleviatethedisadvantagesassociatedwithliposomes,Niosomesalleviatethedisadvantagesassociatedwithliposomes,suchaschemicalinstability,variablepurityofphospholipidsandsuchaschemicalinstability,variablepurityofphospholip
24、idsandhighcost.highcost. TheyhavethepotentialforcontrolledandtargateddrugdeliveryTheyhavethepotentialforcontrolledandtargateddrugdelivery NiosomesenhancedthepenetrationofdrugsNiosomesenhancedthepenetrationofdrugs20/03/200817anotechnologybaseddrugdelivery纳米药物递送Nanopowder20/03/200818anotechnologybased
25、drugdelivery纳米药物递送Nanopowder NanopowdersarepowderscomposedofNanopowdersarepowderscomposedofnanoparticles,thatisparticleshavinganaveragenanoparticles,thatisparticleshavinganaveragediameterbelow50nanometers(nm).diameterbelow50nanometers(nm). AjarofatruenanopowderwhenemptiedfromAjarofatruenanopowderwhe
26、nemptiedfromchestheighttotowardthefloorwilldisperseintochestheighttotowardthefloorwilldisperseintotheairbeforereachingthefloor.theairbeforereachingthefloor. Mostmanufacturersof“nanopowders”produceMostmanufacturersof“nanopowders”producemicropowderassembliesofnanoparticlesbutthemicropowderassembliesof
27、nanoparticlesbutthepowderitselfisrarelyananopowder.powderitselfisrarelyananopowder. SuchcompoundshavetwoormoredifferentSuchcompoundshavetwoormoredifferentcations(positivelychargedelements)intheircations(positivelychargedelements)intheirchemicalformula.Anexampleofacomplexchemicalformula.Anexampleofac
28、omplexcompoundiscalciumtitanate(CaTiO3).compoundiscalciumtitanate(CaTiO3).20/03/200819anotechnologybaseddrugdelivery纳米药物递送Nanocluster20/03/200820anotechnologybaseddrugdelivery纳米药物递送NanoclusterOneofthecentralthemesinnanoscienceOneofthecentralthemesinnanoscienceresearchistosynthesizehighqualityresearc
29、histosynthesizehighqualitynanoparticleswithprecisecontrolovernanoparticleswithprecisecontroloverparticlesize,shape,structure,andparticlesize,shape,structure,position.Forinorganicnanoparticles(e.g.metalForinorganicnanoparticles(e.g.metalandsemiconductor),tworegimesareofandsemiconductor),tworegimesare
30、ofparticularinterest,thatis,nanoclustersinparticularinterest,thatis,nanoclustersinasizerangefromsubnanometerto2nmasizerangefromsubnanometerto2nmandnanocrystals(typically2-100nm).andnanocrystals(typically2-100nm).20/03/200821anotechnologybaseddrugdelivery纳米药物递送Nanocrystals20/03/200822anotechnologybas
31、eddrugdelivery纳米药物递送Nanocrystals Whenthesizeofthematerialisreducedtolessthan100Whenthesizeofthematerialisreducedtolessthan100nanometers,therealmofquantumphysicstakesoverandnanometers,therealmofquantumphysicstakesoverandmaterialsbegintodemonstrateentirelynewproperties.materialsbegintodemonstrateentir
32、elynewproperties. Nano-designofdrugsbyvarioustechniqueslikemilling,Nano-designofdrugsbyvarioustechniqueslikemilling,highpressurehomogenization,controlledprecipitationetc.,highpressurehomogenization,controlledprecipitationetc.,areexploredtoproduce,drugnanocrystals,nanoparticles,areexploredtoproduce,d
33、rugnanocrystals,nanoparticles,nanoprecipitates,nanosuspensions(whichforeaseofnanoprecipitates,nanosuspensions(whichforeaseofunderstandingcommonlymentionedasnanocrystals).understandingcommonlymentionedasnanocrystals). AsdecreasedsizewillincreasethesolubilityofdrugsAsdecreasedsizewillincreasethesolubi
34、lityofdrugshence,thistechnologyisexploredtoincreaseoralhence,thistechnologyisexploredtoincreaseoralbioavailabilityofsparinglywatersolubledrugs.bioavailabilityofsparinglywatersolubledrugs.20/03/200823anotechnologybaseddrugdelivery纳米药物递送Micelle20/03/200824anotechnologybaseddrugdelivery纳米药物递送Micelle Mi
35、celleisanaggregateofamphipathicmoleculesinwater,withtheMicelleisanaggregateofamphipathicmoleculesinwater,withthenonpolarportionsintheinteriorandthepolarportionsattheexteriornonpolarportionsintheinteriorandthepolarportionsattheexteriorsurface,exposedtowater.surface,exposedtowater. Amphiphilicmolecule
36、sformmicelleaboveaparticularconcentrationwhichAmphiphilicmoleculesformmicelleaboveaparticularconcentrationwhichiscalledascriticalmicellarconcentration(CMC).iscalledascriticalmicellarconcentration(CMC). MicellesareknowntohaveananisotropicwaterdistributionwithintheirMicellesareknowntohaveananisotropic
37、waterdistributionwithintheirstructure,meanswaterconcentrationdecreasesfromthesurfacetowardsstructure,meanswaterconcentrationdecreasesfromthesurfacetowardsthecoreofthemicelle,withacompletelyhydrophobic(water-excluded)thecoreofthemicelle,withacompletelyhydrophobic(water-excluded)core.core. Hydrophobic
38、drugscanbeencapsulated/solubalized,intoinnercore.Hydrophobicdrugscanbeencapsulated/solubalized,intoinnercore. ThespatialpositionofasolubilizeddruginamicellewilldependonitsThespatialpositionofasolubilizeddruginamicellewilldependonitspolarity,nonpolarmoleculeswillbesolubilizedinthemicellarcore,andpola
39、rity,nonpolarmoleculeswillbesolubilizedinthemicellarcore,andsubstanceswithintermediatepolaritywillbedistributedalongthesubstanceswithintermediatepolaritywillbedistributedalongthesurfactantmoleculesincertainintermediatesurfactantmoleculesincertainintermediatepositions.positions.20/03/200825anotechnol
40、ogybaseddrugdelivery纳米药物递送Dendrimers20/03/200826anotechnologybaseddrugdelivery纳米药物递送Dendrimers ThesebranchedmacromoleculesareconstructedaroundaThesebranchedmacromoleculesareconstructedaroundasimplecoreunit.simplecoreunit. Dendrimershaveahighdegreeofmolecularuniformity,Dendrimershaveahighdegreeofmole
41、cularuniformity,narrowmolecularweightdistribution,specificsizeandnarrowmolecularweightdistribution,specificsizeandshapecharacteristics,andahighly-functionalizedshapecharacteristics,andahighly-functionalizedterminalsurface.terminalsurface. ThemanufacturingprocessisaseriesofrepetitivestepsThemanufactu
42、ringprocessisaseriesofrepetitivestepsstartingwithacentralinitiatorcore.Eachsubsequentstartingwithacentralinitiatorcore.Eachsubsequentgrowthsteprepresentsanewgenerationofpolymerwithgrowthsteprepresentsanewgenerationofpolymerwithalargermoleculardiameter,twicethenumberofreactivealargermoleculardiameter
43、,twicethenumberofreactivesurfacesites,andapproximatelydoublethemolecularsurfacesites,andapproximatelydoublethemolecularweightoftheprecedinggeneration.weightoftheprecedinggeneration.20/03/200827anotechnologybaseddrugdelivery纳米药物递送PolymericNanoparticles20/03/200828anotechnologybaseddrugdelivery纳米药物递送P
44、olymericNanoparticlesInrecentyears,biodegradablepolymericInrecentyears,biodegradablepolymericnanoparticleshaveattractedconsiderablenanoparticleshaveattractedconsiderableattentionaspotentialdrugdeliveryattentionaspotentialdrugdeliverydevicesinviewoftheirapplicationsindevicesinviewoftheirapplicationsi
45、ndrugtargetingtoparticulardrugtargetingtoparticularorgans/tissues,ascarriersofDNAorgans/tissues,ascarriersofDNAingenetherapy,andintheirabilitytoingenetherapy,andintheirabilitytodeliverproteins,peptidesandgenesdeliverproteins,peptidesandgenesthroughaperoralrouteofadministration.throughaperoralrouteof
46、administration.20/03/200829anotechnologybaseddrugdelivery纳米药物递送Carbon6020/03/200830anotechnologybaseddrugdelivery纳米药物递送Carbon60 C60aresphericalmoleculesabout1nminC60aresphericalmoleculesabout1nmindiameter,comprising60carbonatomsdiameter,comprising60carbonatomsarrangedas20hexagonsand12pentagons:thear
47、rangedas20hexagonsand12pentagons:theconfigurationofafootball.configurationofafootball. HencetheyfindapplicationasHencetheyfindapplicationasNanoPharmaceuticalswithlargedrugpayloadinNanoPharmaceuticalswithlargedrugpayloadintheircagelikestructure.theircagelikestructure. Ontheotherhandwithdevelopmentofv
48、ariousOntheotherhandwithdevelopmentofvariouschemicalsubstitutesforC60,itispossibletochemicalsubstitutesforC60,itispossibletodevelopfunctionalizedC60withbetterdrugdevelopfunctionalizedC60withbetterdrugtargetingpropertiestargetingproperties20/03/200831anotechnologybaseddrugdelivery纳米药物递送CarbonNanotube
49、20/03/200832anotechnologybaseddrugdelivery纳米药物递送CarbonNanotube CarbonnanotubesareadeptatenteringtheCarbonnanotubesareadeptatenteringthenucleiofcellsandmayonedaybeusedtonucleiofcellsandmayonedaybeusedtodeliverdrugsandvaccines.deliverdrugsandvaccines. ThemodifiednanotubeshavesofaronlybeenThemodifiedna
50、notubeshavesofaronlybeenusedtoferryasmallpeptideintothenucleiofusedtoferryasmallpeptideintothenucleioffibroblastcells.fibroblastcells. ButtheresearchersarehopefulthattheButtheresearchersarehopefulthatthetechniquemayonedayformthebasisfornewtechniquemayonedayformthebasisfornewanti-cancertreatments,gen
51、etherapiesandanti-cancertreatments,genetherapiesandvaccines.vaccines.20/03/200833anotechnologybaseddrugdelivery纳米药物递送EquipmentsforNanoparticles1.Homogenizer2.UltraSonicator3.Mills4.SprayMilling5.SupercriticalFluidTechnology6.Electrospray7.Ultracentrifugation8.Nanofiltration20/03/200834anotechnologybaseddrugdelivery纳米药物递送Homogenizer&UltraSonicator 20/03/200835anotechnologybaseddrugdelivery纳米药物递送MethodsofDrugDelivery20/03/200836anotechnologybaseddrugdelivery纳米药物递送THANK YOUE-mail:E-mail:20/03/200837anotechnologybaseddrugdelivery纳米药物递送anotechnologybaseddrugdelivery纳米药物递送
