Phytosome

phytosome drug delivery system

1. PHYTOSOME
Presented by
ArabindaChangmai
M. Pharm 2
nd
sem
Department of pharmacy
Assam downtown university

2. CONTENT
INTRODUCTION
ADVANTAGE
DISADVANTAGE
PREPARATION METHOD
EVALUATION
DIFFERENCE BETWEEN PHYTOSOME AND LIPOSOME
APPLICATION
MARKETED PRODUCT
REFERENCE
Department of pharmacy, ADTU

3. INTRODUCTION
•Theterm‘Phyto’meansplantwhile‘Some’meanscell-
like.Phytosomeisnoveldrugdeliverysystemthat
combineshydrophilicbioactivephytoconstituentsof
herbs/herbalextractsandboundbyphospholipids.
•Morebioavailablethanasimple/conventionalherbal
extractduetoitsenhancedcapacitytocrossthelipid
richbiomembranesandreachcirculation.
•Astheyarebetterabsorbedandproducesbetterresults
•Appliedtostandardizedplantextracts,watersoluble
phytoconstituentsandmanypopularherbalextracts
including,grapeseed,olivefruitsandleaves,green
tea,ginsengetcintophospholipidstoproducelipid
compatiblemolecularcomplexes
Department of pharmacy, ADTU

4. •Thepresenceofasurfactanti.e.thephospholipidsinthemoleculetheseare
shieldedfromwater-triggereddegradation.
•Moleculesareanchoredthroughchemicalbondstothepolarcholinehead
ofthePC,itcanbedemonstratedbyspecificspectroscopictechniques.
Introduction (contd.)
Department of pharmacy, ADTU

5. ADVANTAGES
Markedenhancementofbioavailability.
Valuablecomponentsoftheherbalextractsareprotectedfromdestruction
bydigestivesecretionsandgutbacteria
Nocompromiseofnutrientsafety.
Doserequirementisreducedduetoabsorptionofchiefconstituent.
Phytosomesshowsbetterstabilityprofilebecausechemicalbondsare
formedbetweenphospholipidmoleculesandphytoconstituent
Phospholipidusedinthephytosomeprocessbesidesactingasacarrieralso
nourishestheskin,becauseitisessentialpartofcellmembrane.
Department of pharmacy, ADTU

6. DISADVANTAGE
•Phytoconstituentis quickly eradicated/ eliminated from phytosome.
Lowriskprofile:Thistechnologyhasnolarge-scaledrugdevelopmentrisk
sincethetoxicologicalprofilesofthephytosomalcomponentsarewell
documentedinthescientificliteratures.
Relativelysimpletomanufacturewithnocomplicatedtechnicalinvestment
requiredfortheproductionofPhytosomes.
Theypermeatethenon-lipophilicbotanicalextracttoallowbetter
absorptionfromtheintestinallumen,whichisotherwisenotpossible
Advantages (contd.)
Department of pharmacy, ADTU

7. PREPRATION METHOD
SolventEvaporationmethodisthemostcommontechniqueusedforthe
preparationofphytosomes
Phytosomesarepreparedbyreactingnaturalorsyntheticphospholipids
withactivecomponentslikebioflavonoid,flavolignanandpolyphenolic
constituents.
•Phospholipiddissolveinorganicsolvent
•SolutionofphospholipidinsolutioncontainingOrganicsolvent+Herbal
extract
•Drying
•ThinFilmFormation
•Hydrationofthinfilm
•Formationofphytosomecomplex(suspension)
•Isolationbyprecipitationwithnonsolvent(suchasaliphatichydrocarbons)
•Drying(Bylyophilizationorspraydrying)Figure1:FlowdiagramofPhytosome
preparation.
Department of pharmacy, ADTU

8. EVALUATION
Transitiontemperature:
Thetransitiontemperatureofthevesicularlipidsystemcanbesettled
viadifferentialscanningcalorimetry.
Entrapmentefficiency:
Theentrapmentefficiencyofaphytosomalpreparationcanbe
determinedbyexposingthepreparationtoultracentrifugation
method.
Vesiclesizeandzetapotential:
Theparticlesizeandzetapotentialofphytosomescanbeconfirmed
bydynamiclightscattering,whichusagesacomputerized
examinationsystemandphotoncorrelationspectroscopy.
Surfacetensionactivitymeasurement:
Thesurfacetensionactivityofthedruginaqueoussolutioncanbe
determinedbytheDuNouyringtensiometer.
Department of pharmacy, ADTU

9. Visualization:
Visualizationofphytosomescanbeaccomplishedusingscanning
electronmicroscopy(SEM)andbytransmissionelectronmicroscopy.
Vesiclestability:
Thesteadinessofvesiclescanbemeasuredbycalculatingthesizeand
structureofthevesiclesovertime.ThemeansizeiscalculatedbyDLS
andstructuralchangesaremonitoredbytem.
Spectroscopicevaluation
Toconfirmtheformationofacomplexortostudythereciprocal
interactionbetweenthephyto-constituentsandthephospholipidH1
NMR,C13NMR,FTIRareused
InvitroandInvivoevaluations
Modelsofin-vitroandin-vivoevaluationsareselectedonthebasisof
theexpected therapeuticactivityofbiologicallyactive
phytoconstituentspresentinthephytosome.
Evaluation (contd.)
Department of pharmacy, ADTU

10. Difference between Liposome and
phytosome
Slno Phytosome Liposome
1 Inphytosome,thephosphatidylcholineand
theplantcomponentsactuallyforma1:1or
a2:1molecularcomplexdependingonthe
substance(s)complexes.
Aliposomeisformedbymixingawater
solublesubstancewithphosphatidylcholine
indefiniteratiounderspecificconditions.
2 Phytosomeinvolveschemicalbonds. Here,nochemicalbondisformed;the
phosphatidylcholinemoleculessurround
thewatersolublesubstance.
3 Phytosomearemuchbetterabsorbedthan
liposomesshowingbetterbioavailability.
Bioavailabilityofliposomesislessthan
phytosomes.
Department of pharmacy, ADTU

11. Structure difference between phytosomeand liposome
Department of pharmacy, ADTU

12. APPLICATION OF PHYTOSOMES
•SilymarinPhytosome
•MostofthephytosomesarefocusedtoSilybummarianumwhichcontains
premierliver-protectantflavonoids.
•Thefruitofthemilkthistleplant(S.marianum,FamilySteraceae)contains
flavonoidsknownforhepato-protectiveeffects.
•Silymarinhasbeenshowntohavepositiveeffectsintreatingliverdiseasesof
variouskinds,includinghepatitis,cirrhosis,fattyinfiltrationoftheliver(chemical
andalcoholinducedfattyliver)andinflammationofthebileduct.Silymarin
Phytosome
•Phytosomesof grape seed
•Grapeseedphytosomeiscomposedofoligomericpolyphenolsofvarying
molecularsizecomplexedwithphospholipids.
•Themainpropertiesofprocyanidinflavonoidsofgrapeseedareanincreasein
totalantioxidantcapacityandstimulationofphysiologicaldefensesofplasma.
Department of pharmacy, ADTU

13. Application (contd.)
•Phytosomeofgreentea
•Greentealeaves(Theasinensis)ischaracterizedbypresenceofapolyphenolic
compoundepigallocatechin3-O-gallateasthekeycomponent.
•Thesecompoundsarepotentmodulatorsofseveralbiochemicalprocesslinked
tothebreakdownofhomeostasisinmajorchronic-degenerativediseasessuch
ascancerandatherosclerosis.
•Greenteaalsofurnishesuswithanumberofbeneficialactivitiessuchas
antioxidant,anticarcinogenic,antimutagenic,hypocholesterolemic,cardio
protectiveeffects.
•Phytosomesofcurcumin
•Maitietal.developedthephytosomesofcurcumin(flavonoidfromturmeric,
Curcumalongalinn)andnaringenin(flavonoidfromgrape,Vitisvinifera).
•Phytosomeofnaringeninproducedbetterantioxidantactivitythanthefree
compoundwithaprolongeddurationofaction
Department of pharmacy, ADTU

14. MARKETED PRODUCT
Sr. No. Trade name Phytoconstituents complex Indications
1 Silybinphytosome Silybin fromSilibium marianum Hepatoprotective,
Antioxidant.
2 Grape seed
(Leucoselect) phytosome
Procyanidinsfromvitisvinifera Antioxidant,
Anticancer.
3 Ginseng phytosome Ginsenosides fromPanax ginseng Immunomodulator
4 Hawthorn phytosome Flavonoids fromCrataegus species Antihypertensive,
Cardioprotective.
5 Sericoside phytosome Sericoside fromTerminalia sericea Skin improver, Anti-
Wrinkles
6 Ginko select phytosome Flavonoids fromGinko biloba Anti aging,Protects
Brain and Vascular
liling
7 Olea select phytosome Polyphenols fromOlea europea Anti–hyperlipidemic,
Anti-inflammatory
8 Green select phytosome Epigallocatechin fromThea sinensis Anti-cancer,
Antioxidant
Department of pharmacy, ADTU