BP 704T: NOVEL, DRUG DELIVERY SYSTEMS(Theory)

Unit-||

Microencapsulation
Microencapsulation is defined as a process of enclosing or enveloping solids, liquids or
even gases within second material with a continuous coating of polymeric materials yielding
microscopic particles (ranging from less than l micron to several hundred microns in size). In

this process, smalldiscrete solid particles or small liquid droplets and dispersions arc surrounded
and enclosed by applying thin coating for the purposes of providing environmental protection
and controlling the release characteristics or availability of coated active ingredients.
Microencapsulation process is widely employed to modify and delayed drug release form
different pharmaceutical dosage forms. The materials enclosed or enveloped within the
microcapsules are known as core materials or pay-load materials or nucleus, and the enclosing
materials are known as coating materials or wall material or shell or membrane.

Microparticles:
"Microparticles" refers to the particles having the diameter range of 1-1000 um,
irrespective of the precise exterior and/or interior structures.
Microspheres:
"Microspheres" particularly refers to the spherically shaped microparticles within the

broad category of microparticlcs.

Microcapsules:
"Microcapsules" refers to microparticles having a core surrounded by the coat or wall

material(s) distinctly different from that of the core or pay-load or nuclcus, which may bc solid.
liquid, or even gas.
Microcapsules can be classified on three types (Fig, 1):
around the corc.
i). Mononuclcar: Containing the shell
 particles
circulatingupward particulate
microencapsulation:
Methods of microencapsulation:
Disadvantages of microencapsulation:
Advantages of
coating a suspension:Ai(ar) ii).techniques.
Expensive
ii). i). v). iv). iii). iî). i).
Microencapsulation Microencapsulation
moving encapsulated
materials. This delaying
FormulationmodifySurfaceLiquids
Providing iii). i ).
material flow of (Fig. core Matrix
Polynuclcar:
causes
2). encapsulated
releaseof and as and
air materials well type:
is the Within reduction delayed
of environmentalgases
sprayed stream. Mononuclear
sustained as DistributedHaving
particles colloidal can
the in drug
to The a by coating in be Fig.
he coating many
shelf-life
supporting air
tthrough controlledrelease changed
protection 1: Microcapsules
Classificationof
chamber characteristics homogeneously
moving suspension may Classification cores
chamber, active form
the Polynuclear
air not of into to
eneioscd
particles, design hygroscopic release
coating-zone stream be agents different solid the
particulate method uniform of
encapsulated
and dosage various
particles microcapsulesof into with
and or
During its pharmaceutical
core the
the
consists andagents. in
portion
operating
core spray materials. forms active in shell shcll.
cach this the active Matrix
type
materials can material.
coating-
pass the of coating of can agents form
parameters the be
dosage agents
through influence of
can
done microcapsules.
are dispersing
on or
forms be
coating-zone, the
-chamber, suspended the bychangea. core
influence air the modifying
suspended of release materials.
solids
where a on
ra o of or
2
 interface. used.
encapsulated. material
microencapsulation. corethe
separation Also
can liquidDropletscoatingmaterial
(b)
monomerssystem,
polymer and
The Coacervation
Microencapsulation
equipments
Important of i). i ). i).
methodneceSsary
are concentrated deposition
the
microcapsules.to Formation
phase The
When liquid
formDeposition
Rigidizing receiveS
solutions drying
be the and phase The
of
jacketed dissolvedcoating vehicle liquid the of a Fig. supporting
rate a
polymer can coating by
of3separation: coat
the
coating immiscible 2: is
tanks be
phasepolymer liquid coacervation Air particles
Core chamber
Drying Spraying
nozzle Hotalr directlv and
in
material material
solutionsinduccd (Fig. suspension Microcapsules suspension
Feed air this
with the usuallypolymer
liquid coating strennuns
relatd Cyclic
variable iS so 3). phase.phases: phase
an wil that In by
phasefor thermal,coating method tnprocess
vehicle a
separation the
speed
mmiscible form phase manyaround
microencapsulation liquid
and cases, on for temperature is
agitators. phase separation the the repcated
t0
cross manufacturing
coalescetophysical microencapsulation
method
polymer, interface dry
and linking core
material. of the
depending
subsequently
polymerized of consists
it or or the
product
the formed
coacervationby may yield chemical desolvation phase, supporting
polymers
occur.wil of3 on
betwo a between while
a the
added changes core steps:
phase it
alf purposc
the
techniques material is
directlyliquid- Streaim being
in
the core of
3 at
 HASE

SEAMRANON

Droplets Coacervate
Dropeta
Aiyner Sadin

MEMORANE

FORMATKN

Pobanenc

microencapsulation
Fig. 3: Coacervation phase separation method for

(c) Pan coating:

microencapsulation
For relatively large particles, which are greater than 600 u in size,
industry for
can be done by pan coating method, which is being widely used in pharmaceutical
the preparation of controlled release particulates. In this method, various spherical
Core

materials, such as nonpareil sugar seeds are coated with a variety of polymers (Fig. 4). In
practice, the coating is applied as a solution or as an atomized spray to the desired solid core
material in the coating pan. Generally, warm air is passed over the coated materials as the
coatings are being applied in the coating pans to remove the coating solvent. In some cases, the
process of final solvent removal is accomplished in the drying oven.
Inlet

Exhaust

Tablet bed

Fig. 4: Pan coating method for microencapsulao

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 (d) Fluidized-bed technology
Fluidized-bed technology method for microcncapsulation is used for the encapsulation of
solid core materials, including liquids absorbed into porous solids. This microencapsulation
be
method is expansively employed to encapsulate pharmaceuticals. Solid particles to
encapsulated are sUspended on a jet of air and aforward arc covered by a spray of liquid coating
cooling or
material. The capsules are traveled to where their shells are solidified by
an area
solvent vapor1zation. The processes of suspending. spraving, and cooling are repeated until the
attainment of the desired thickness of the caneule.rall This is known as Wurster process when

the spray nozzle is located at the bottom of the fluidized-bed of particles.

(e) Spray drying and spray congealing:

are almost similar in
Spray drying and spray congealing methods of microencapsulation
coating agent and
that both the methods entail the dispersion of core material in a liquefied
environmental condition, whereby
spraying or introducing the core coating mixture into some
The main difference in
relatively rapid solidification of the coating is influenced (Fig. 5).
by which the coating solidification
between these two microencapsulation methods are the means
solidification is influenced by the quick
is carried out. In spray drying method, the coating
spray congealing method,
evaporation of a solvent, in which the coating material is dissolved. In
congealing of molten coating material
the coating solidification is accomplished by the thermal
or solidifying adissolved coating by introducing
the coating core material mixture into a non
coated product is often done by sorption
solvent. Removal of non-solvent or solvent from the
extraction or evaporation. Nozzle Gas Flow
Feed FloW

Bag Filter
HTwo Fluid Nozzle
c Exhaust Ar

Cyclone
Drying
Healer Chamber

Collection
Vessel
Feed
drying method for microcncapsulation
Fig. 5: Spray
 () Multiorifio cenritugation microencapsulation utilizes the centrifugal forces to
methodfor
Multionific-centrifugation membrane. Various processing variables of multiorific-
enveloping
hurl a core particle
trough an rate of the core and
(i)rotational speed of the cylinder, (ii) flow
include
centrifugation method concentration. viscosity and surfacc tension of the core material. The
oating materials, and (ii) for microencapsulating liquids and solids of
varied
multiorifice-centrifugal method is capable
coating
materials. The encapsulated product can be supplied as slurry in
SIZe ranges with diverse
the hardening media or as dry powder.

(g) Sohent Evaporation

manufacturing vehicle (O/W
Solvent evaporation method is appropriate for liquid
The solvent evaporation
emulsion), which is prepared by agitation of two immiscible liquids.
volatile solvent, which is
method involves dissolving microcapsule coating (polymer) in a
(drug) to be
immiscible with the liquid manufacturing vehicle phase. A core material
microencapsulated is dissolved or dispersed in the coating polymer solution. With agitation, the
core-coating material mixture is dispersed in the liquid manufacturing vehicle phase to obtain
the appropriate sized microcapsules. Agitation of system is continued until the solvent partitions
into the aqueous phase and is removed by evanoration. This process results in hardened
microcapsules. Several techniques can be used to achieve dispersion of the oil phase in the
ContinuOus phase. The most common method is the 3se of a propeller style blade attached to a
variable speed motor.
Various process variables namely rate of solvent evaporation for the coating polymer(s),
temperature cycles and agitation rates inflhuenee the mehods of forming dispersions. The most
important factors that should bc considered for the preparation of microcapsules by solvent

evaporation method include choice of vebicle haee and golvent for the polymer coating, and
solvent recovery systems. The solvent microencapsulation is applicable
evaporation method for
to a wide variety of liquid and solid cOre materials. The core materials may be either water
soluble or water insoluble materials. Avariety of film forming polymers can be used as coatings.

(h) Polymerization:

6
 monomer solid-liquid, microcapsule
the
cross-linkingvarious When
Applications:applications.
solid-gas. or andmaterial
1.
cross-linking
Interfacial () therctore, interface
7. 5. 4. 3. 2. the The
6. Microencapsulation functional In is
Microencapsulation techniques.
Through irritation.
Gastric that
TheMicroencapsulation forms Different
Substance
Microcncapsulation microcapsules.
dosage
forms to form of reaction
containing intertacial dispersed.polymerization
the coatings,
taste by method the existing
microencapsulation, irritant drugs modifyingapplications groups is polymerization
can of
will
performed active The
in-between
be bitter of croSs-linking m
drugs microencapsulation of continuous coreor situ.
stored overcomethe be
can drug the hydrogen Themethod
can selectively delaying can or can of
are microencapsulation
also be protein, at
to beemployed candidates used the reaction method
a
long useo being Corethe
1quids be interface atoms method
proolems absorbed release to leading of
to employed inol
mes microencapsulated formulate is material
oceurs microcncapsulalOn
deerease to ana can is of material
ald of to
replaced
of .o
witnout or gases be in
encapsulated verymicroencapsulation,
the an at ahe
tacky in and
the masked the to various are:
formulate versatile emulsion, the
supporting reaction
the formation by
any can intestine
granulations
volatility. addition a
intcrfaccs continuous a
substantial be sustained biosourced
changed by to active of
employing enteric-coated
reduce rather for of the phase monomeriC
A of pharmaceutical aacid of
and oily agents membrane. liquid-l1quid, isphase,
microencapsulated into than controlled chloride polymer, the
evaporation. th e usually
in protective from to
medicines
direct solid the or small units
microcncapsulation chances wherein
stomach,dosage forms,socore The reacts
with
the a
particles release like liquid pos
compression. materials. or bifunctional nquan
to of interfacial a
cosmetic protein.
volatile tableted gastric dosage or
in gas, core
the
7
 active agents
S. Microencapsulation provides environmental protection to the encapsulated
from various environmental issues, Sue ds ight, heat, humidity, oxidation, etc.
9. The hygroscopic characteristics of many Core materials can be reduced by

microencapsulation.
10. The separations of incompatible substances can be achieved by microencapsulation. For
example, pharmaceutical eutectics can be separated by microencapsulation. This is a case
where direct contact of materials brings about liquid formation. The stability
enhancement of incompatible aspirin-chlorpheniramine maleate mixture is accomplished
by microencapsulating both of then before mixing.
11. Microencapsulation is used to lessen the potential danger of toxic substance handling.
The toxicity owing to handling of herbicides, insecticides, pesticides and fumigants, etc.,
can be usefully lessened after microencapsulation.

References:
[1].Allen LV, Popovich NG, Ansel HC. Pharmaceutical Dosage Forms and
Systems. Delhi, India: BI Publication: 2005. Drug Delivery
[2].Lachman LA, Liberman HA, Kanig JL. The Theory and Practice of Industrial
Mumbai, India: Varghese Publishing House, 1976. Pharmacy.
[3].Benita Microencapsulation: Methods and Undustrial applications, Marcel
S.
New York, 1996. Dekker, Inc.,
[4]. Singh MN, Hemant KS, Ram M, Shivakumar HG.
technique for controlled drug delivery, Res Pharm Sci. Microencapsulation: A promising
[5]. Sachan NK, Singh B, Rao
KR.
2010;5(2):65-77.
Controlled drug delivery
microencapsulation. Malaysian J Pharm Sci. through
[6]. Kiyoyama S, Shiomori K, 2006:4:65-81.
of their morphology. J Kawano Y,, Hatate Y. Preparation of microcapsules and control
Microencapsulation. 2003;20:497