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Body Project Atal

The document provides an overview of microencapsulation as a drug delivery system, detailing its advantages, disadvantages, applications, and various manufacturing techniques. It emphasizes the importance of microcapsules in enhancing drug stability, controlling release rates, and improving patient compliance. The paper also discusses the mechanisms of drug release and the materials used in microencapsulation, highlighting its potential in pharmaceutical and other industries.

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0% found this document useful (0 votes)
11 views23 pages

Body Project Atal

The document provides an overview of microencapsulation as a drug delivery system, detailing its advantages, disadvantages, applications, and various manufacturing techniques. It emphasizes the importance of microcapsules in enhancing drug stability, controlling release rates, and improving patient compliance. The paper also discusses the mechanisms of drug release and the materials used in microencapsulation, highlighting its potential in pharmaceutical and other industries.

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akash9149824238
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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SERIAL NO. TOPIC PAGE NO.

1. Introduction 2

2. Classification 3

1. 3. Reasons for microencapsulation 3

2. 4. Release mechanism 3-4

3. 5. Material used for microencapsulation 4-5

4. 6. Manufacturing technique for microcapsules 5

a) 6.1 Air suspension method 6-7

b) 6.2 Coacervation phase separation 7-8

c) 6.3 Multiorifice centrifugal process 8-9

d) 6.4 Pan coating 9-10

e) 6.5 Spray drying 10-11

f) 6.6 Solvent evaporation 11-12

g) 6.7 Polymerization 12-13

5. 7. Advantages 13-14

6. 8. Evaluation of microcapsules 14-17

7. 9. Conclusion 17-18

8. 10. References 18-20

RAYAT INSTITUTE OF PHARMACY Page 1


Abstract

Microparticles offer various significant advantages as drug delivery systems, including: (i) an
effective protection of the encapsulated active agent against (e.g. enzymatic) degradation, (ii) the
possibility to accurately control the release rate of the incorporated drug over periods of hours to
months, (iii) an easy administration (compared to alternative parenteral controlled release dosage
forms, such as macro-sized implants), and (iv) Desired, pre-programmed drug release profiles can
be provided which match the therapeutic needs of the patient. This article gives an overview on
the general aspects and recent advances in drug-loaded microparticles to improve the efficiency of
various medical treatments. An appropriately designed controlled release drug delivery system can
be a foot ahead towards solving problems concerning to the targeting of drug to a specific organ
or tissue, and controlling the rate of drug delivery to the target site. The development of oral
controlled release systems has been a challenge to formulation scientist due to their inability to
restrain and localize the system at targeted areas of gastrointestinal tract. Microparticulate drug
delivery systems are an interesting and promising option when developing an oral controlled
release system. The objective of this paper is to take a closer look at microparticles as drug delivery
devices for increasing efficiency of drug delivery, improving the release profile and drug targeting.
In order to appreciate the application possibilities of microcapsules in drug delivery, some
fundamental aspects are briefly reviewed.

Keywords: Drug delivery systems, Microcapsules, Controlled release, Microencapsulation

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1. INTRODUCTION
Microencapsulation is a process by which very tiny droplets or particles of liquid or solid material
are surrounded or coated with a continuous film of polymeric material. Microencapsulation
includes bi encapsulation which is more restricted to the entrapment of a biologically active
substance (from DNA to entire cell or group of cells for example) generally to improve its
performance or enhance its shelf life. Microencapsulation provides the means of converting liquids
to solids, of altering colloidal and surface properties, of providing environmental protection and
of controlling the release characteristics or availability of coated materials. Several of these
properties can be attained by macro packaging techniques; however, the uniqueness of
microencapsulation is the smallness of the coated particles and their subsequent use and adaptation
[1].
to a wide variety of dosage forms and not has been technically feasible Gelatin is a common
wall-forming material but synthetic polymers like polyvinyl alcohol, ethyl cellulose, polyvinyl
chloride and other materials also may be used. One of the advantages of microencapsulation is that
the administered dose of a drug is subdivided into small units that are spread over a large area of
the gastrointestinal tract, which may enhance absorption by diminishing localized drug
concentration. Custom-made microspheres and microcapsules are provided to customers in the
food, pharmaceutical, cosmetic, consumer and personal care products, agricultural, veterinary
medicine, industrial chemicals, biotechnology, biomedical and sensor industries [2].
2. ADVANTAGES
 Reliable means to deliver the drug to the target site with specificity, if modified and to maintain
the desired concentration at the site of interest without untoward effects.
 Solid biodegradable microspheres have the potential throughout the particle matrix for the
controlled release of drug.
 Microspheres received much attention not only for prolonged release, but also for targeting of
anticancer drugs to the tumor.
 The size, surface charge and surface hydrophilicity of microspheres have been found to be
important in determining the fate of particles in vivo.
 Studies on the macrophage uptake of microspheres have demonstrated their potential in targeting
drugs to pathogens residing intracellularly [18].

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Figure 1: Advantages of microencapsulation

3. DISADVANTAGES
 Microencapsulation techniques are of high cost.
 This causes reduction in Shelf life of hygroscopic drugs.
 Different dosage forms like tablets, capsules, lozenges cannot be encapsulated by single
microencapsulation process.
 Coating may not be uniform this can effect release pattern of a drug in the body.

Figure 2: Disadvantages of microencapsulation

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4. APPLICATIONS
The applications of micro-encapsulation are numerous. The ones mentioned below are some of the
most common ones.
 Adhesives
 Anticoating corrosives
 Carbonless copy paper
 E-paper or e ink
 Essential oils, flavours and other volatile bio actives for food or in feed additives
 Pesticides
 Pharmaceuticals, small molecules and recently also peptides and small proteins for oral or
sublingual delivery
 Phase change materials
 Powder perfume
 Scratch and sniff
 Self – healing material such as novel plastics that can automatically repair damage:
 Textiles
 Temperature release (controlled release) in baking
 Thermochromic dyes
 Time release technology for pharmaceuticals
 Visual indicators
 Selfhealing coatings
 DNA protection from degradation for product tracing and data storage
 Protection of bioactive compounds that are easily degradated under normal environmental
conditions.
5. Features of Microcapsule:
Microencapsulation is the packaging of small droplets of liquid or particles with a thin film.
Typically, the lowest particle size of microcapsules is 1µm and the largest size is 1mm.
Microcapsules consist of a core and a wall (or shell). The configuration of the core can be a
 Spherical or irregular particle,
 Liquid-phase suspended solid,
 Solid matrix,

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 Dispersed solid and
 Aggregates of solids or liquid forms.
6. Classification:
Microcapsules can be classified on three basic categories according to their morphology as
follows,
a) Mononuclear
b) Polynuclear and
c) Matrix types
Mononuclear (core-shell) microcapsules contain the shell around the core, while polynuclear
capsules have many cores enclosed within the shell. In matrix encapsulation, the core material is
distributed homogeneously into the shell material. In addition to these three basic morphologies,
microcapsules can also be mononuclear with multiple shells, or they may form clusters of
microcapsules [3].
7. REASONS FOR MICROENCAPSULATION
The primary reason for microencapsulation is found to be either for sustained or prolonged drug
release. This technique has been widely used for
 Masking taste and odor of many drugs to improve patient compliance.
 Can be used for converting liquid drugs in a freeflowing powder.
 The drugs, which are sensitive to oxygen, moisture or light, can be stabilized by
microencapsulation.
 Incompatibility among the drugs can be prevented by microencapsulation.
 Vaporization of many volatile drugs e.g. methyl salicylate and peppermint oil can be prevented by
microencapsulation.
 Many drugs have been microencapsulated to reduce toxicity and GI irritation including ferrous
sulphate and KCl.
 Alteration in site of absorption can also be achieved by microencapsulation.
 Toxic chemicals such as insecticides may be microencapsulated to reduce the possibility of
sensitization of factorial person.
 Bakan and Anderson reported that microencapsulated vitamin A palmitate had enhanced stability
[4].

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8. RELEASE MECHANISMS
Mechanisms of drug release from microspheres are as follows

a) Degradation controlled monolithic system

The drug is dissolved in matrix and is distributed uniformly throughout. The drug is strongly
attached to the matrix and is released on degradation of the matrix. The diffusion of the drug is
slow as compared with degradation of the matrix.

b) Diffusion controlled monolithic system


Here the active agent is released by diffusion prior to or concurrent with the degradation of the
polymer matrix. Rate of release also depend upon where the polymer degrades by homogeneous
or heterogeneous mechanism.
c) Diffusion controlled reservoir system
Here the active agent is encapsulated by a rate controlling membrane through which the agent
diffuses and the membrane erodes only after its delivery is completed. In this case, drug release is
unaffected by the degradation of the matrix.
d) Erosion
Erosion of the coat due to pH and enzymatic hydrolysis causes drug release with certain coat
material like glycerol mono stearate, beeswax and steryl alcohol etc [5].
9. MATERIAL USED FOR MICROENCAPSULATION
9.1 CORE MATERIALS
The core material, defined as the specific material to be coated, can be liquid or solid in nature.
The composition of the core material can be varied, as the liquid core can include dispersed and/or
dissolved materials. The solid core be active constituents, stabilizers, diluents, excipients, and
release-rate retardants or accelerators [6].
9.2 COATING MATERIALS
The coating material should be capable of forming a film that is cohesive with the core material;
be chemically compatible and nonreactive with the core material; and provide the desired coating
properties, such as strength, flexibility, impermeability, optical properties, and stability. The
coating materials used in microencapsulation methods are amenable, to some extent, to in situ
modification. The selection of a given coating often can be aided by the review of existing

RAYAT INSTITUTE OF PHARMACY Page 7


literature and by the study of free or cast films, although practical use of free-film information
often is impeded for the following reasons.
 Cast or free films prepared by the usual casting techniques yield films that are considerably thicker
than those produced by the microencapsulation of small particles; hence, the results obtained from
the cast films may not be extrapolate to the thin microcapsule coatings.
 The particular microencapsulation method employed for the deposition of a given coating
produces specific and inherent properties that are difficult to simulate with existing filmcasting
methods [7].
9.3 PROPERTIES OF CORE MATERIAL
 Stabilization of core material.
 Inert toward active ingredients.
 Controlled release under specific conditions.
 Film-forming, pliable, tasteless, stable.
 Non-hygroscopic, no high viscosity, economical.
 Soluble in an aqueous media or solvent, or melting.
9.4 EXAMPLES OF COATING MATERAIS
1. Water soluble resins -
Gelatin, Gum Arabic, Starch, Polyvinylpyrrolidone, Carboxymethylcellulose,
2. Water insoluble resins –
Ethylcellulose, Polyethylene, Polymethacrylate, Polyamide (Nylon),
3. Waxes and lipids –
Paraffin, Carnauba, Spermaceti, Beeswax, Stearic acid, Stearyl alcohol.
4. Enteric resins –
Shellac, Cellulose acetate phthalate, Zein [8].
10. MANUFACTURING TECHNIQUE FOR MICROCAPSULE
Microcapsules as bulk materials, in either dry powder or dispersed form, can be processed into
final product applications using common equipment such as V-blenders, tablet machines,
granulators, homogenizes, kneaders, hard gelatin capsule filling machines, or coating equipment
if deposition onto a substrate is desired9. There are many factors to consider when selecting the
encapsulation process and also various techniques are available for the encapsulation of core
materials. Broadly the methods are divided into two types (Figure 2), such as physical and

RAYAT INSTITUTE OF PHARMACY Page 8


chemical methods. Characterization of Reservoir (Solvent Exchange Method): A newer
Microencapsulation Technique On the other hand, it has been noticed that most proteins undergo
inactivation events such as degradation and aggregation within the micro particles during the
manufacturing process as well as the release period10-11. For this reason, the protein release is
typically incomplete despite substantial degradation of the polymer. Protein inactivation in the
micro particle system is largely due to extensive exposure of the protein to damaging
environments, such as large interfacial area between aqueous and organic phases (w/o),
hydrophobic polymers, and their acidic degradation products12-13, one of the recent examples
includes encapsulating proteins in hydro gels prior to polymeric microencapsulation, which was
found to be effective in preserving the protein stability and controlling the release rate14. In
addition to the formulation approaches, improvement of microencapsulation techniques has also
been attempted. The anhydrous microencapsulation process is one of the examples15. Recently, a
new microencapsulation technique called the solvent exchange method has been developed in an
attempt to address the above problems16. Briefly, the new method produces reservoir-type
microcapsules by inducing collision between drug-loaded aqueous drops and polymer- dissolved
organic solvent drops. The micro scaled liquid drops can be generated by different equipment such
as ink-jet nozzles17 and ultrasonic atomizers18. Protein release from traditional polymeric micro
particles is typically triphasic. The three phases are,
1. An initial burst-release of surface-bound and poorly encapsulated protein,
2. A second phase consisting of diffusion release and/or an induction period that does not release
protein,
3. Release due to the degradation of the polymer matrix [9].
10.1 Air-suspension coating
Air-suspension coating of particles by solutions or melts gives better control and flexibility. The
particles are coated while suspended in an upward-moving air stream. They are supported by a
perforated plate having different patterns of holes inside and outside a cylindrical insert. Just
sufficient air is permitted to rise through the outer annular space to fluidize the settling particles.
Most of the rising air (usually heated) flows inside the cylinder, causing the particles to rise rapidly.
At the top, as the air stream diverges and slows, they settle back onto the outer bed and move
downward to repeat the cycle. The particles pass through the inner cylinder many times in a few
minutes methods. The air suspension process offers a wide variety of coating materials

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candidates for microencapsulation. The process has the capability of applying coatings in the form
of solvent solutions, aqueous solution, emulsions, dispersions or hot melts in equipment ranging
in capacities from one pound to 990 pounds. Core materials comprised of micron or submicron
particles can be effectively encapsulated by air suspension techniques, but agglomeration of the
particles to some larger size is normally achieved [10].

Figure3: Air suspension technique


10.2 Coacervation-Phase Separation
i) Formation of three immiscible chemical phases – A liquid manufacturing vehicle phase, a core
material phase, and a coating material phase. To form the three phases, the core material
dispersed in a solution of the coating polymer, the solvent for the polymer being the liquid
manufacturing vehicle phase. The coating material phase, an immiscible polymer in a liquid state,
is formed by utilizing one of the methods of the methods of phase separation Coacervation, i.e.,
by changing the temperature of the polymer solution; or by adding a salt, nonsolvent, or
incompatible polymer to the polymer solution; or by inducing a polymer- polymer interaction.
ii) Deposition of the coating – It consists of depositing the liquid polymer coating upon the core
material. This is accomplished by controlled, physical mixing of the material in the manufacturing
vehicle. Deposition if the liquid polymer coating around the core material occurs if the polymer is
adsorbed at the interface formed between the core material and the liquid vehicle phase, and this
adsorption phenomenon is a prerequisite to effective coating. The continued deposition of the
coating material is promoted by a reduction in the total free interfacial energy of the system,
brought about by the decrease of the coating material surface area during coleasance of the liquid
polymer droplets.

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iii) Rigidization of the coating – It involves rigidizing the coating, usually by thermal,
crosslinking, or desolvation techniques, to form a self-sustaining microcapsules eg. Coaceration
Microencapsulation of Talc Particles with Poly (methyl methacrylate) by Pressure-Induced Phase
Separation of CO2-Expanded Ethanol Sol [11].

Fig: - Coacervation process


10.3 Multiorifice-Centrifugal Process
The apparatus contains a rotating cylinder a major and essential part of the device. Located within
the cylinder are three circumferential grooves. The upper and lower grooves, also located
circumferentially around the cylinder, carry the coating material in molten or solution form to the
respective grooves. The ridge of the coating material grooves serves as a weir over which the
coating material overflows when the volume of the upper and lower grooves is exceeded by the
volume of material pumped into the system. The coating materials under centrifugal force imparted
by the cylinder rotation flows outward along the side of the immediate groove into the countersunk
portion and form a film across the orifice. A counter rotating, mounted within the cylinder,
atomizes or disperses the core material fed through the centrally located inlet. The rotating disc
flings the particulate core material droplets or solid particles towards the orifice. The core material
serve arrives at the orifices and encounters the coating material membrane. The impact and
centrifugal force, generated by the rotating cylinder, hurls the core material through the enveloping
coating material, which is immediately regenerated by the continually overflowing coating
material. The embroynic microcapsules, upon leaving the orifice, are hardened, congealed, or

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voided of coating solution by passing them through a hot air stream to harden and congeal coating
[12].

Fig.:- Multiorifice-Centrifugal Process


10.4 Pan coating
The pan coating process, widely used in the pharmaceutical industry, is among the oldest industrial
procedures for forming small, coated particles or tablets. The particles are tumbled in a pan or
other device while the coating material is applied slowly.

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Figure4: Representation of pan coating process
In practice, the coating is applied as a solution, or as an atomized spray, to the desired solid core
material in the coating pans. Usually, to remove the coating solvent, warm air is passed over the
coated materials as the coatings are being applied in the coating pans. In some cases, final solvent
removal is accomplished in a drying oven [13].
10.5 Spray–drying
Spray drying serves as a microencapsulation technique when an active material is dissolved or
suspended in a melt or polymer solution and becomes trapped in the dried particle. The main
advantage is the ability to handle labile materials because of the short contact time in the dryer, in
addition, the operation is economical. In modern spray dryers the viscosity of the solutions to be
sprayed can be as high as 300mPa.s.
Spray drying and spray congealing processes are similar in that both involve dispersing the core
material in a liquified coating substance and spraying or introducing the core - coating mixture
into some environmental condition, whereby, relatively rapid solidification (and formation) of the
coating is affected. The principal difference between the two methods is the means by which
coating solidification is accomplished. Coating solidification in the case of spray drying is affected
by rapid evaporation of a solvent in which the coating material is dissolved. Coating solidification
in spray congealing methods, however, is accomplished by thermally congealing a molten coating
material or by solidifying a dissolved coating by introducing the coating - core material mixture
into a nonsolvent. Removal of the nonsolvent or solvent from the coated product is then
accomplished by sorption, extraction, or evaporation techniques. In case of spray drying is affected
by rapid evaporation of a solvent in which the coating material is dissolved. Coating solidification
in spray congealing methods, however, is accomplished by thermally congealing a molten coating
material or by solidifying a dissolved coating by introducing the coating - core material mixture
into a nonsolvent. Coating solidification in spray congealing methods, however, is accomplished
by thermally congealing a molten coating material or by solidifying a dissolved coating by
introducing the coating - core material mixture into a nonsolvent. Removal of the nonsolvent or
solvent from the coated product is then accomplished by sorption, extraction, or evaporation
techniques [14].

RAYAT INSTITUTE OF PHARMACY Page 13


Figure5: Spray Drying and Congealing
10.6 Solvent Evaporation
This technique has been used by companies including the NCR Company, Gavaert Photo -
Production NV, and Fuji Photo Film Co., Ltd. to produce microcapsules. The processes are carried
out in a liquid manufacturing vehicle. The microcapsule coating is dissolved in a volatile solvent,
which is immiscible with the liquid manufacturing vehicle phase. A core material to be
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 size microcapsule. The mixture is then heated (if necessary) to evaporate the solvent
for the polymer. In the case in which the core material is dispersed in the polymer solution, polymer
shrinks around the core. In the case in which core material is dissolved in the coating polymer
solution, a matrix - type microcapsule is formed. Once all the solvent for the polymer is evaporated,
the liquid vehicle temperature is reduced to ambient temperature (if required) with continued
agitation. At this stage, the microcapsules can be used in suspension form, coated on to substrates
or isolated as powders. The solvent evaporation technique to produce microcapsules is applicable
to a wide variety of liquid and solid core materials. The core materials may be either water - soluble
or water - insoluble materials. A variety of film - forming polymers can be used as coatings 2. Eg.
Evaluation of Sucrose Esters as Alternative Surfactants in Microencapsulation of Proteins by the
Solvent Evaporation Method [15].
10.7Polymerization
i. Interfacial polymerization

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In Interfacial polymerization, the two reactants in a polycondensation meet at an interface and
react rapidly. The basis of this method is the classical Schotten Baumann reaction between an acid
chloride and a compound containing an active hydrogen atom, such as an amine or alcohol,
polyesters, polyurea, polyurethane. Under the right conditions, thin flexible walls form rapidly at
the interface. A solution of the pesticide and a diacid chloride are emulsified in water and an
aqueous solution containing an amine and a polyfunctional isocyanate is added. Base is present to
neutralize the acid formed during the reaction. Condensed polymer walls form instantaneously at
the interface of the emulsion droplets.
ii. In-situ polymerization
In a few microencapsulation processes, the direct polymerization of a single monomer is carried
out on the particle surface. In one process, e.g. Cellulose fibers are encapsulated in polyethylene
while immersed in dry toluene. Usual deposition rates are about 0.5µm/min. Coating thickness
ranges 0.2-75µm. The coating is uniform, even over sharp projections[1

iii. Matrix polymer

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In a number of processes, a core material is imbedded in a polymeric matrix during formation of
the particles. A simple method of this type is spray-drying, in which the particle is formed by
evaporation of the solvent from the matrix material. However, the solidification of the matrix also
can be caused by a chemical change. Using this phenomenon, Chang prepares microcapsules
containing protein solutions by incorporating the protein in the aqueous diamine phase. Chang has
demonstrated the perm selectivity, by their ability to convert blood urea to ammonia, the enzyme
remaining within the microcapsules when incorporated [17].
11. EVALUATION OF MICROCAPSULE:
The characterization of the microparticulate carrier is an important phenomenon, which helps to
design a suitable carrier for the proteins, drug or antigen delivery. These microspheres have
different microstructures. These microstructures determine the release and the stability of the
carrier.
11.1 Sieve Analysis:
Separation of the microspheres into various size fractions can be determined by using a mechanical
sieve shaker. A series of five standard stainless steel sieves (20, 30, 45, 60 and 80 mesh) are
arrangedin the order of decreasing aperture size. Five grams of drug loaded microspheres are
placed on the upper-most sieve. The sieves are shaken for a period of about 10 min, and then the
particles on the screen are weighed [19] .

Fig: Motorized Sieve Shaker


11.2 Morphology of Microspheres
The surface morphologies of microspheres are examined by a scanning electron microscope (XL
30 SEM Philips, Eindhoven, and The Netherlands). The microspheres are mounted onto a copper
cylinder (10 mm in diameter, 10 mm in height) by using a double-sided adhesive tape. The

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specimens are coated at a current of 10 mA for 4 min using an ion sputtering device (JFC1100E,
Jeol, Japan) [20] .
11.3 Atomic Force Microscopy (Afm)
A Multimode Atomic Force Microscope from Digital Instrument is used to study the surface
morphology of the microspheres. The samples are mounted on metal slabs using double-sided
adhesive tapes and observed under microscope that is maintained in a constant temperature and
vibration-free environment [21] .

Fig.:Atomic Force Microscope


11.4 Particle Size:
Particle size determination approximately 30 mg microparticles is redispersed in 2–3 ml distilled
water, containing 0.1% (m/m) Tween20 for 3 min, using ultrasound and then transferred into the
small volume recirculating unit, operating at 60 ml/ s. The microparticle size can be determined
[22].
by laser diffractometry using a Malvern Mastersizer X (Malvern Instruments, UK)
11.5 Viscosity of the Polymer Solutions:
The absolute viscosity, kinematic viscosity, and the intrinsic viscosity of the polymer solutions in
different solvents can be measured by a U-tube viscometer(viscometer constant at 40 0C is 0.0038
mm2/s /s) at 25 ± 0.1 0C in a thermostaticbath. The polymer solutions are allowed tostand for 24
h prior to measurement toensure complete polymer dissolution [23].

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Fig.: Brookfield Viscometer
11.6 Density Determination:
The density of the microspheres can be measured by using a multi volume pychnometer.
Accurately weighed sample in a cup is placed into the multi volume pychnometer. Helium is
introduced at a constant pressure in the chamber and allowed to expand. This expansion results in
a decrease in pressure within the chamber. Two consecutive readings of reduction in pressure at
different initial pressure are noted. From two pressure readings the volume and density of the
microsphere carrier is determined [24].
11.7 Bulk Density
The microspheres fabricated are weighedand transferred to a 10-ml glass graduatedcylinder. The
cylinder is tapped using anautotrap (Quantach- rome, FL, USA) untilthe microsphere bed volume
is stabilised.The bulk density is estimated by the ratioof microsphere weight to the final volumeof
the tapped microsphere bed [25].
11.8 Capture Efficiency
The capture efficiency of the microspheres or the percent entrapment can be determined by
allowing washed microspheres to lyse. The lysate is thensubjected to the determination of active
constituents as per monograph requirement 19. The percent encapsulation efficiency is calculated
using following equation:

𝑎𝑐𝑡𝑢𝑎𝑙𝑐𝑜𝑛𝑡𝑒𝑛𝑡
%𝑒𝑛𝑡𝑟𝑎𝑝𝑚𝑒𝑛𝑡 = ∗ 100
𝑡ℎ𝑒𝑜𝑟𝑒𝑡𝑖𝑐𝑎𝑙𝑐𝑜𝑛𝑡𝑒𝑛𝑡

RAYAT INSTITUTE OF PHARMACY Page 18


11.9 Angle of Contact
The angle of contact is measured to determine the wetting property of a micro particulate carrier.
It determines the nature of microspheres in terms of hydrophilicity or hydrophobicity. This
thermodynamic property is specific to solid and affected by the presence of the adsorbed
component. The angle of contact is measured at the solid/air/water interface. The advancing and
receding angle of contact are measured by placing a droplet in a circular cell mounted above
objective of inverted microscope. Contact angle is measured at 200 C within a minute of deposition
of microspheres [26].
11.10 In Vitro Methods
There is a need for experimental methods which allow the release characteristics and permeability
of a drug through membrane to be determined. For this purpose, a number of in vitro and in vivo
techniques have been reported. In vitro drug release studies have been employed as a quality
control procedure in pharmaceutical production, in product development etc. Sensitive and
reproducible release data derived from physico chemically and hydro dynamically defined
conditions are necessary. The influence of technologically defined conditions and difficulty in
simulating in vivo conditions has led to development of a number of in vitro release methods for
buccal formulations; however no standard in vitro method has yet been developed. Different
workers have used apparatus of varying designs and under varying conditions, depending on the
shape and application of the dosage form developed [27] .
11.11 Dissolution Apparatus
Standard USP or BP dissolution apparatus have been used to study in vitro release profiles using
both rotating elements, paddle 20-22. Dissolution medium used for the study varied from 100-500
ml and speed of rotation from 50-100 rpm [28].

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12. CONCLUSION
Microencapsulation means packaging an active ingredient inside a capsule ranging in size from
one micron to several millimeters. The capsule protects the active ingredient from its surrounding
environment until an appropriate time. Then, the material escapes through the capsule wall by
various means, including rupture, dissolution, melting or diffusion. Microencapsulation is both an
art and a science. There's no ONE way to do it, and each new application provides a fresh
challenge. Solving these riddles requires experience, skill and the mastery of many different
technologies [29].

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13. REFERENCES
1. Leon L, Herbert A.L and Joseph L.K. The Theory And Practice of Industrial Pharmacy.3rd
edition. 1990. Varghese Publishing House. 1990. 412, 428.
2. James S. Encylopedia of Pharmaceutical Techonology, 3rd edition. Vol- 1325-1333.
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