Microemulsion :
A novel drug carrier system
Guided by : Dr Sachin Rathod
Asst Professor
Presented by : Y Subhasish Singha
MPharm (IP) 1st semester
Agenda Overview
01
02
03
04
05
06
07
08
INTRODUCTION
HISTORY
MICROEMULSION TYPES
PREPARATION METHODS
EQUIPMENTS USED
INFLUENTIAL FACTORS
EVALATION PARAMETERS
APPLICATIONS
INTRODUCTION
Microemulsions are thermodynamically stable, isotropic systems composed of
water and oil phases mixed with a surfactant, often combined with a co-
surfactant. The co-surfactant, typically a short- to medium-chain alcohol,
reduces the interfacial tension between the two immiscible phases, allowing
the formation of microemulsions with droplet sizes ranging from 10 to 140 nm.
These unique properties make microemulsions highly effective for drug
delivery, particularly in topical applications. Their low viscosity, transparency,
and ability to solubilize poorly soluble drugs enhance the delivery of active
agents into the skin, improving solubilization and bioavailability compared to
conventional vehicles like lotions or creams.
HISTORY
The microemulsion concept was introduced as early as 1940's by
Hoar and Schulman who generated a clear single-phase solution
by titrating a milky emulsion by hexanol.
Schulman and co-worker (1959) subsequently coined the term
microemulsion.
In the year 1970, research in microemulsion reached on a larger
scale.
W h a t i s M i c r o e m u l s i o n ? ? ?
Micro-emulsion is homogenous,
transparent, thermodynamically
stable dispersions of water and
oil, stabilized by a surfactant,
usually in combination with a
co-surfactant."
Microemulsions are small scale versions
of emulsion.
The droplet sizes are very small,
typically 100 Å which is about 100 times
smaller than typical emulsion droplet
sizes.
Fig : Microemulsion structure
ALTERNATIVE NAMES :
Microemulsions are also called as
Transparent emulsion
Swollen micelle
Micellar solution
Solubilized oil
Microemulsion in our life
ADVANTAGES OF MICROEMULSIONS
These are thermodynamically stable.
Require minimum energy for formation.
Ease of manufacturing.
Improved drug solubilization and bioavailability.
Wide applications in colloidal drug delivery systems.
The formation of microemulsion is reversible.
Improve the efficacy of a drug & Minimum side effects.
• Use of large concentration of surfactant and co-surfactant
necessary for the stabilizing micro droplets.
• Limited solubilizing capacity for high melting substances.
• Microemulsion stability is influenced by environmental parameters
such as, temperature & pH. These parameters change upon
microemulsion delivery to the patients.
DISADVANTAGES OF MICROEMULSIONS
Feature Microemulsions Traditional Emulsions
Droplet Size 10-200 nm 1-20 µm
Appearance Clear or translucent Cloudy or opaque
Preparation Low energy input, can form spontaneously
High energy input required (e.g., high shear
mixing)
Stability Generally more stable due to smaller droplets
Less stable, as larger droplets can coalesce
over time
Surfactant Requirement
Typically requires surfactants and co-
surfactants for stabilization
Surfactants are used, but the system is less
delicate
Form
Can form in a single phase (oil and water
mixed)
Requires separate oil and water phases
Comparison between microemulsions and traditional emulsions
E M U L S I O N MICROEMULSION
Microemulsions are of 3 types. They are :
O/W Microemulsion
W/O Microemulsion
Bi-continuous microemulsion
O/W Microemulsion where in droplets are dispersed in the
continuous aqueous phase.
W/O Microemulsion where in water droplets are dispersed in the
continuous oil phase.
Bi-continuous microemulsion where in micro domains of oil &
water are inter dispersed within the system.
In all the three types of microemulsions, the interface is stabilized
by an appropriate combination of surfactants and/or co-
surfactants.
PREPARATION METHODS OF MICROEMULSIONS :
Following are the different methods used for the
preparation of the microemulsions :
1) Phase titration method
2) Phase inversion method
PHASE-TITRATION METHOD :
Dilution of an oil-surfactant mixture with water. [W/O]
Dilution of a water surfactant mixture with oil.[O/W]
Mixing of all components at once, in some systems, the
order of ingredients addition may determine whether a
microemulsion forms are not.
PHASE-INVERSION METHOD :
Temperature range in which an o/w microemulsions inverts to a w/o
type.
• Using non-surfactants: polyoxyethylene are very susceptible to
temperature. With increase in the temperature, polyoxyethylene group
becomes dehydrated, altering critical packing parameter which results
in the phase inversion.
• For ionic surfactants: increasing temperature, increase the
electrostatic repulsion between the surfactant headgroups thus causing
reversal of film curvature. Hence, the effect of temperature is opposite
to the effect seen with non-ionic surfactants.
EQUIPMENTS USED
Colloidal Mill
It is a machine that reduces the size
of particles in a liquid or the size of
droplets in an emulsion. It uses a
high-speed rotor to push a fluid
through small holes in a stationary
stator. The size of the holes can be
adjusted to control the level of
shear, which determines the size of
the resulting particles.
A rotor-stator mill, also known as a
rotor-stator mixer, is a device that uses
a rotating rotor and a stationary stator
to mix, disperse, and homogenize
materials
Rotor-stator
HOMOGENIZER
Homogenizer is a mixer used to
create a uniform and even mixture
by forcing material through a
narrow, confined space.
BRAND NAME DRUG COMPANY DOSAGE FORM CATEGORY
Douxoseborrhea Phytosphingosine Sogeval Spray Emollient
Retamax Retinol Skin Health inc Cream Emollient
White glow SPF25 Lotus Herbal Cream Emollient
Tray bell Cocoa extract Alcantra Shampoo Cleansing
MARKETED PREPARATIONS
Factors affecting microemulsion formation
PACKING RATIO
PROPERTY OF SURFACTANT
PROPERTY OF OIL PHASE
TEMPERATURE
CHAIN LENGTH
NATURE OF CO-SURFACTANT
EVALUATION PARAMETERS STUDIES :
Phase behaviour
Size and shape
Rheology
Conductivity
Zeta potential
Drug release studies
Physical stability study
Applications of Microemulsion
Oral bioavailability enhancement poorly water soluble drugs
Protection against Biodegradation
Solid State formulation
Supersaturable Microemulsion System
Ocular Drug delivery System
Parenteral Drug Delivery System
Topical Drug Delivery System
Mucosal Drug Delivery System
Transdermal Drug Delivery System
CONCLUSION :
Microemulsions are potentially quite powerful alternative carrier system
for delivery because of high solubilization capacity, transparency,
thermodynamic stability, ease of preparation, and high diffusion and
absorption rates through skin, when compared to solvent without the
surfactant system.
A number of factors must be considered when using microemulsions as
drug delivery system such as surfactant, co-surfactant, oils, PH, HLB,
temperature etc.
REFERENCES :
• The Theory and practice of Industrial pharmacy., Leon
Lacham, Herbert A.Liberman special Indian edition 2009,pg.no:
507-530.
• Shaji,J.,Reddy, M.S.; Microemulsion as drug delivery
system,Pharma Times,
• Razdan,R.,Devarajan,P.V.; Microemulsions Indian Drugs,
2003,pg.no: 139-146.
Thank You

Microemulsion | A Novel Drug Carrier System | Mpharm | Industrial Pharmacy.pdf

  • 1.
    Microemulsion : A noveldrug carrier system Guided by : Dr Sachin Rathod Asst Professor Presented by : Y Subhasish Singha MPharm (IP) 1st semester
  • 2.
    Agenda Overview 01 02 03 04 05 06 07 08 INTRODUCTION HISTORY MICROEMULSION TYPES PREPARATIONMETHODS EQUIPMENTS USED INFLUENTIAL FACTORS EVALATION PARAMETERS APPLICATIONS
  • 3.
    INTRODUCTION Microemulsions are thermodynamicallystable, isotropic systems composed of water and oil phases mixed with a surfactant, often combined with a co- surfactant. The co-surfactant, typically a short- to medium-chain alcohol, reduces the interfacial tension between the two immiscible phases, allowing the formation of microemulsions with droplet sizes ranging from 10 to 140 nm. These unique properties make microemulsions highly effective for drug delivery, particularly in topical applications. Their low viscosity, transparency, and ability to solubilize poorly soluble drugs enhance the delivery of active agents into the skin, improving solubilization and bioavailability compared to conventional vehicles like lotions or creams.
  • 4.
    HISTORY The microemulsion conceptwas introduced as early as 1940's by Hoar and Schulman who generated a clear single-phase solution by titrating a milky emulsion by hexanol. Schulman and co-worker (1959) subsequently coined the term microemulsion. In the year 1970, research in microemulsion reached on a larger scale.
  • 5.
    W h at i s M i c r o e m u l s i o n ? ? ? Micro-emulsion is homogenous, transparent, thermodynamically stable dispersions of water and oil, stabilized by a surfactant, usually in combination with a co-surfactant."
  • 6.
    Microemulsions are smallscale versions of emulsion. The droplet sizes are very small, typically 100 Å which is about 100 times smaller than typical emulsion droplet sizes. Fig : Microemulsion structure
  • 7.
    ALTERNATIVE NAMES : Microemulsionsare also called as Transparent emulsion Swollen micelle Micellar solution Solubilized oil
  • 8.
  • 9.
    ADVANTAGES OF MICROEMULSIONS Theseare thermodynamically stable. Require minimum energy for formation. Ease of manufacturing. Improved drug solubilization and bioavailability. Wide applications in colloidal drug delivery systems. The formation of microemulsion is reversible. Improve the efficacy of a drug & Minimum side effects.
  • 10.
    • Use oflarge concentration of surfactant and co-surfactant necessary for the stabilizing micro droplets. • Limited solubilizing capacity for high melting substances. • Microemulsion stability is influenced by environmental parameters such as, temperature & pH. These parameters change upon microemulsion delivery to the patients. DISADVANTAGES OF MICROEMULSIONS
  • 11.
    Feature Microemulsions TraditionalEmulsions Droplet Size 10-200 nm 1-20 µm Appearance Clear or translucent Cloudy or opaque Preparation Low energy input, can form spontaneously High energy input required (e.g., high shear mixing) Stability Generally more stable due to smaller droplets Less stable, as larger droplets can coalesce over time Surfactant Requirement Typically requires surfactants and co- surfactants for stabilization Surfactants are used, but the system is less delicate Form Can form in a single phase (oil and water mixed) Requires separate oil and water phases Comparison between microemulsions and traditional emulsions
  • 12.
    E M UL S I O N MICROEMULSION
  • 13.
    Microemulsions are of3 types. They are : O/W Microemulsion W/O Microemulsion Bi-continuous microemulsion
  • 14.
    O/W Microemulsion wherein droplets are dispersed in the continuous aqueous phase. W/O Microemulsion where in water droplets are dispersed in the continuous oil phase. Bi-continuous microemulsion where in micro domains of oil & water are inter dispersed within the system. In all the three types of microemulsions, the interface is stabilized by an appropriate combination of surfactants and/or co- surfactants.
  • 15.
    PREPARATION METHODS OFMICROEMULSIONS : Following are the different methods used for the preparation of the microemulsions : 1) Phase titration method 2) Phase inversion method
  • 16.
    PHASE-TITRATION METHOD : Dilutionof an oil-surfactant mixture with water. [W/O] Dilution of a water surfactant mixture with oil.[O/W] Mixing of all components at once, in some systems, the order of ingredients addition may determine whether a microemulsion forms are not.
  • 17.
    PHASE-INVERSION METHOD : Temperaturerange in which an o/w microemulsions inverts to a w/o type. • Using non-surfactants: polyoxyethylene are very susceptible to temperature. With increase in the temperature, polyoxyethylene group becomes dehydrated, altering critical packing parameter which results in the phase inversion. • For ionic surfactants: increasing temperature, increase the electrostatic repulsion between the surfactant headgroups thus causing reversal of film curvature. Hence, the effect of temperature is opposite to the effect seen with non-ionic surfactants.
  • 18.
    EQUIPMENTS USED Colloidal Mill Itis a machine that reduces the size of particles in a liquid or the size of droplets in an emulsion. It uses a high-speed rotor to push a fluid through small holes in a stationary stator. The size of the holes can be adjusted to control the level of shear, which determines the size of the resulting particles.
  • 19.
    A rotor-stator mill,also known as a rotor-stator mixer, is a device that uses a rotating rotor and a stationary stator to mix, disperse, and homogenize materials Rotor-stator
  • 20.
    HOMOGENIZER Homogenizer is amixer used to create a uniform and even mixture by forcing material through a narrow, confined space.
  • 21.
    BRAND NAME DRUGCOMPANY DOSAGE FORM CATEGORY Douxoseborrhea Phytosphingosine Sogeval Spray Emollient Retamax Retinol Skin Health inc Cream Emollient White glow SPF25 Lotus Herbal Cream Emollient Tray bell Cocoa extract Alcantra Shampoo Cleansing MARKETED PREPARATIONS
  • 22.
    Factors affecting microemulsionformation PACKING RATIO PROPERTY OF SURFACTANT PROPERTY OF OIL PHASE TEMPERATURE CHAIN LENGTH NATURE OF CO-SURFACTANT
  • 23.
    EVALUATION PARAMETERS STUDIES: Phase behaviour Size and shape Rheology Conductivity Zeta potential Drug release studies Physical stability study
  • 24.
    Applications of Microemulsion Oralbioavailability enhancement poorly water soluble drugs Protection against Biodegradation Solid State formulation Supersaturable Microemulsion System Ocular Drug delivery System Parenteral Drug Delivery System Topical Drug Delivery System Mucosal Drug Delivery System Transdermal Drug Delivery System
  • 25.
    CONCLUSION : Microemulsions arepotentially quite powerful alternative carrier system for delivery because of high solubilization capacity, transparency, thermodynamic stability, ease of preparation, and high diffusion and absorption rates through skin, when compared to solvent without the surfactant system. A number of factors must be considered when using microemulsions as drug delivery system such as surfactant, co-surfactant, oils, PH, HLB, temperature etc.
  • 26.
    REFERENCES : • TheTheory and practice of Industrial pharmacy., Leon Lacham, Herbert A.Liberman special Indian edition 2009,pg.no: 507-530. • Shaji,J.,Reddy, M.S.; Microemulsion as drug delivery system,Pharma Times, • Razdan,R.,Devarajan,P.V.; Microemulsions Indian Drugs, 2003,pg.no: 139-146.
  • 27.