2. Clase Microencapsulación

8/9/2019 2. Clase Microencapsulacin

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MICROENCAPSULACINMICROENCAPSULACIN2013_2


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Proceso de inclusin deslidos, lquidos, o inclusogases, en partculasmicroscpicas, donde se

cubren las sustancias concapas delgadas de unmaterial polimrico.

Qu es microencapsularQu es microencapsular

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Partculas de dimetro entre 3-800m:

microcpsulas o microesferas

Pueden servir para liberacin controlada

de principios activos

Pueden utiliarse para proteccin de

sustancias

!as Microesferasson consideradas polvos

de "lu#o libre


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COMPOSICIN DE LASCOMPOSICIN DE LAS

MICROPARTCULASMICROPARTCULAS

a$ %aterial de n&cleo

b$ 'apa o pared o cubierta dematerial

!as micropartculas constan de dos componentes:


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CLASSIICATION O MICROPARTICLECLASSIICATION O MICROPARTICLE


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CLASSIICATION O MICROPARTICLECLASSIICATION O MICROPARTICLE

1.Microspheres:()e active agent is dispersed ordissolved in an inert pol*mer.

2!Microcapsules: ()e active agent "orms a core +omore$ surrounded b* an inert di""usion barrier.


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Microspheres:

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Microcapsules:

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"Para #$e se microe%ca&s$'a("Para #$e se microe%ca&s$'a(

Proteccin del n&cleo de su entorno.

etardar la evaporacin de un n&cleo

voltil.

%e#ora de las propiedades de mane#ode un material pega#oso.

islamiento de un n&cleo reactivocontra el ataue umico.

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/nmascarar el sabor o el olor del n&cleo.

!iberacin controlada de "rmacos.

%anipulacin segura de los materialesticos.

!iberacin selectiva del p.a.

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"Para #$e se microe%ca&s$'a("Para #$e se microe%ca&s$'a(


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UNDAMENTAL CONSIDERATIONUNDAMENTAL CONSIDERATION))

Core ma*eria' Coa*i%+ ma*eria' ,e-ic'e

So'i. Li#$i.

Microe%ca&s$'a*io%

Po'/mers)

1aes

A#$eo$s

No%a#$eo$sesins

Proteins

Pol*sacc)arides


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1! orma*io% of three immiscible phasessolvent.a core material p)ase.a coating material p)ase.

2!Deposition of the coating ma*eria' o% *-ecore ma*eria'!

3. Rigidizing the coating *-erma' cross'i%i%+ or .eso'a*io% *ec-%i#$es4!

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Pasos .e' &rocesoPasos .e' &roceso ::


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5U6 SE DE7E TENER EN5U6 SE DE7E TENER EN

CUENTA)CUENTA)

nature o" t)e core and coating materials.

t)e stabilit* and release c)aracteristics o"t)e coated materials.

t)e microencapsulationmet)ods.

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CU7IERTA CU7IERTA coating materialscoating materials44

'an be liuidor solid

()e composition: dispersed and2or dissolved

material.

()e pol*mer s)ould be capable o" "orming a "ilmt)at is co)esiveit) t)e core material.

4t s)ould be c)emicall* compatible, non-reactiveit) t)e core material.

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5enerall* )*drop)ilic 2 )*drop)obic pol*mers2acombination o" bot) are used

number o" coating materials )ave been used

success"ull*:

-gelatin-polyinyl alcohol-ethyl cellulose-cellulose acetate phthalate! etc.

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CU7IERTA CU7IERTA coating materialscoating materials 44


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POL8MERSPOL8MERS

6(7!96(/(4'

BIODEGRADABLE

Ex:PolyanhydridesLactides, glycolides

NON-BIODEGRADABLE

Ex: epoxy polyers acrolein

PRO!EIN" Ex: al#$ins gelatin collagen

%ARBO&'DRA!E" Ex: starch carrageenan

%&E(I%ALL' (ODI)IED%ARBO&'DRA!E"

Ex: poly acryl dextran poly acryl starch


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MECANISMOS DE LI7ERACINMECANISMOS DE LI7ERACINDEL PRINCIPIO ACTI,ODEL PRINCIPIO ACTI,O

+!a pared se debe romper al momento del uso$:

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Por presin o tensin de corte.

Por "usin de la pared.

%ediante disolucin en condicionesparticulares, e#emp recubrimiento de unp.a entrico.


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Meca%ismos .e 'i9eraci:% .e'Meca%ismos .e 'i9eraci:% .e'&ri%ci&io ac*io&ri%ci&io ac*io

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por la accin de un disolvente

por ataue enimatico

por una reaccin umica

por )idrlisis o lenta desintegracin.


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PRINCIPALES T6CNICAS DEPRINCIPALES T6CNICAS DEMICROENCAPSULACINMICROENCAPSULACIN

ir suspension tec)niues+ 1urster$

'oacervation process

pra*dr*ing ; congealing

Pan coating

olvent evaporation

Pol*meriation

/trusion

ingle ; double emulsion tec)niues

upercritical "luid anti solvent met)od +$

6ole vibration tec)nolog*


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AIR SUSPENSIONAIR SUSPENSION


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AIR SUSPENSIONAIR SUSPENSION


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COACER

,ACI

N

SIMP

LE

COACER

,ACI

N

SIMP

LE


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!uido o slidoinmiscible

/mulsin o dispersin al 30@


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COACER

,ACIN

COMPLE>A

COACER

,ACIN

COMPLE>A


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+iii$ addition o" nonsolvent, e.g. addition o" isoprop*let)er to met)*l et)*l Ketone solution o" celluloseacetate but*rate

+iv$ addition o" incompatible pol*mer to t)e pol*mersolution, e.g. addition o" pol*butadiene to t)esolution o" et)*lcellulose in toluene

+v$ inducing pol*merLpol*mer interaction, e.g.interaction o" gum arabic and gelatine at t)eir iso-electric point.

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COACER,ATION P@ASECOACER,ATION P@ASESEPARATIONSEPARATION


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Seco%. s*e&Seco%. s*e&deposition o" liuid pol*mer upon t)e core material.

i%a''/i%a''/microcapsules are stabilied b* crosslinKing,desolvation or t)ermal treatment.

+rosslin/ing+rosslin/ing"ormation o" c)emical linKs beteen molecularc)ains to "orm a t)ree-dimensional netorK o"connected molecules.

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COACER,ATION P@ASECOACER,ATION P@ASESEPARATIONSEPARATION


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()e ulcanizationo" rubber I elemental sul"urcrosslinKing+eaK plastic to a )ig)l* resilient elastomer$.

+hitosanat p M.0 an e""ective cross-linKer&olyethylenimine 0&'# +p


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upercritical "luids are highly compressed gassest)at possess several advantageous properties o" bot)

liuids and gases. small c)ange in temperature or pressure causes alarge c)ange in t)e densit* o" supercritical "luids near

t)e critical point.

()e most idel* used being supercritical carbondioide+'D

=$, alKanes+'

=to '

E$, and nitrous oide

+6=

D$. 35

Po'/mer E%ca&s$'a*io% 9/ Ra&i.Po'/mer E%ca&s$'a*io% 9/ Ra&i.E&a%sio% ofE&a%sio% of S$&ercri*ica'S$&ercri*ica'

'$i.s'$i.s


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Hluido supercrtico contiene el ingredienteactivo * el material de la cubierta, a alta presin

luego es lanado a la presin atmos"rica atravs de una peue?a bouilla.

!a cada repentina de la presin )ace ue ladesolvatacin de la cubierta se deposite alrededorde la sustancia activa +n&cleo$ * "orma una capade recubrimiento.

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Ra&i. e&a%sio% ofRa&i. e&a%sio% ofs$&ercri*ica' so'$*io%s$&ercri*ica' so'$*io%


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()e active ingredient and t)e s)ell material must be ver*soluble in supercritical "luids.

Ner* "e pol*mers it) lo co)esive energ* densities+e.g., pol*dimet)*lsiloanes, pol*met)acr*lates$ aresoluble in supercritical "luids suc) as 'D=.

()e solubilit* o" pol*mers can be en)anced b* using co-solvents.

4n some cases nonsolvents are usedO t)is increases t)esolubilit* in supercritical "luids, but t)e s)ell materials donot dissolve at atmosp)eric pressure.

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Po'/mer E%ca&s$'a*io% 9/ Ra&i. E&a%sio% ofPo'/mer E%ca&s$'a*io% 9/ Ra&i. E&a%sio% ofS$&ercri*ica' '$i.sS$&ercri*ica' '$i.s

DisadantageDisadantage::


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Microe%ca&s$'a*io% 9/ ra&i. e&a%sio% ofMicroe%ca&s$'a*io% 9/ ra&i. e&a%sio% ofs$&ercri*ica' so'$*io%s RESS4!s$&ercri*ica' so'$*io%s RESS4!

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%icroencapsulation b* rapid epansion o"supercritical solutions +/$.

5as anti-solvent +5$ process

Particles "rom a gas-saturated solution+P5$

Po'/mer E%ca&s$'a*io% 9/ Ra&i.Po'/mer E%ca&s$'a*io% 9/ Ra&i.E&a%sio% of S$&ercri*ica' '$i.s!E&a%sio% of S$&ercri*ica' '$i.s!

MET@ODSMET@ODS


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4s capable "or microencapsulating liuids andsolids o" varied sie ranges, it) diverse coating

materials.

()e encapsulated product can be supplied as

- slurr* in t)e )ardening media

- dr* poder.

Production rates o" C0 to MC pounds per )our.40

M$'*iorifice ce%*rif$+a'M$'*iorifice ce%*rif$+a'

&rocess&rocess


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()e coating is applied as a solution or as anatomied spra* to t)e desired solid core material int)e coating pan.

7suall*, to remove t)e coating solvent, arm airis passed over t)e coated materials as t)e coatingsare being applied in t)e coating pans.

4n some cases, "inal solvent removal isaccomplis)ed in dr*ing oven.

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Pa% coa*i%+Pa% coa*i%+


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Pa% coa*i%+Pa% coa*i%+


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CO EXTRUSIONCO EXTRUSION


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COBETRUSIONCOBETRUSION


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SPRA8 DR8IN< ANDSPRA8 DR8IN< AND

SPRA8 CON


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'oating solidi"ication in s&ra/ .r/i%+ is e""ectedb* rapid eaporation of a solent in )ic) t)ecoating material is dissolved.

'oating solidi"ication in s&ra/ co%+ea'i%+met)od is accomplis)ed b*:-thermally congealing a molten coating

material or

-b* solidi"*ing a dissolved coating b* introducingt)e coating core material miture into anonsolent.

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SPRA8 DR8IN< AND SPRA8SPRA8 DR8IN< AND SPRA8CON


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emoval o" t)e nonsolvent or solvent "rom t)ecoated product is t)en accomplis)ed b* sorptionetraction or evaporation tec)niues.

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olvent evaporation tec)niues are carried out ina liuid manu"acturing ve)icle +D21 emulsion$)ic) is prepared b* agitation o" to immiscibleliuids.

()e process involves dissolving microcapsulecoating +pol*mer$ in a volatile solvent )ic) isimmiscible it) t)e liuid manu"acturing ve)iclep)ase.

core material +drug$ to be microencapsulated isdissolved or dispersed in t)e coating pol*mersolution.

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SOL,ENT E,APORATIONSOL,ENT E,APORATION


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1it) agitation, t)e core L coating material mitureis dispersed in t)e liuid manu"acturing ve)iclep)ase to obtain appropriate sie microcapsules.

gitation o" s*stem is continued until t)e solventpartitions into t)e aueous p)ase and is removedb* evaporation.

()is process results in )ardened microsp)eres)ic) contain t)e active moiet*.

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SOL,ENT E,APORATIONSOL,ENT E,APORATION


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A&&'ica*io%s ofA&&'ica*io%s ofmicroe%ca&s$'a*io%microe%ca&s$'a*io%

()e tec)nolog* )as been used idel* in t)e design

o" controlled release and sustained release dosage"orms.

(o masK t)e bitter taste o" drugs liKe Paracetamol,6itro"urantoin etc.

to reduce gastric and ot)er 5.4. tract irritations.

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CONTROLES 8


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Siee a%a'/sis

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Mor&-o'o+/,iscosi*/ of *-e &o'/mer so'$*io%s

De%si*/ .e*ermi%a*io%

7$' .e%si*/

Ca&*$re efficie%c/

A%+'e of co%*ac*

Disso'$*io%

Po'/mer so'$9i'i*/ i% *-e So'e%*s

CONTROLES 8CONTROLES 8

CARACTERIACINCARACTERIACIN


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Es*a &rese%*aci:% se 9as: e% 'os *ra9a;os .e)Es*a &rese%*aci:% se 9as: e% 'os *ra9a;os .e)

!Se%*-i' $mar / Sa%.ee& Mo''i.ai%!!Se%*-i' $mar / Sa%.ee& Mo''i.ai%!

GraciasGracias

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2. Clase Microencapsulación