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Microemulsion 141121085401 Conversion Gate02 PDF
Microemulsion 141121085401 Conversion Gate02 PDF
Guided By:
Dr. Tejal Mehta,
Head of Department,
Pharmaceutical Technology & Biopharmaceutics
Prepared By:
Ishani Pandit,
M.Pharm, Sem -1,
Pharmaceutical Technology & Biopharmaceutics
14MPH109.
Content:
2
Introduction
History
Basic aspects of Microemulsion
Theories of Microemulsion
Phase behaviour of Microemulsion
Components of Microemulsion
Types of Microemulsiom
Preparation of Microemulsion
Characterization of Microemulsion
Advantages, disadvantages & Applications
Evaluation of Microemulsion
Marketed Preparations 11/21/2014
conclusion
3 Introduction
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4 Continue…
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5 History
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6 Basic aspects of Microemulsion
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7
If a co-surfactant is used, it may sometimes be represented at a
fixed ratio to surfactant as a single component, and treated as a
single “pseudo-component”.
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8 Comparison between Emulsion &
microemulsion
EMULSION MICROEMULSION
Thermodynamically unstable. Thermodynamically stable.
In due time phases it is separate out. In due time phases it is not separate out.
It is cloudy. It is transparent.
Require large input of energy during its Require low input of energy during its
preparation. relatively low cost.
preparation. higher cost.
Droplet size 20-200 nm
Droplet size > 500 nm
Interfacial tension: ultra low
Interfacial tension: high
Low viscosity with Newtonian behavior.
High viscosity
Dynamic (constantly fluctuating
Stable microstructure interface)
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9
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10
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11
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12 Theory of Microemulsion
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13 Continue…
The free energy of microemulsion formation can be considered to
depend on the extent to which surfactant lowers the surface
tension of oil-water interface and the change in entropy of the
system such that :
ΔGf = γ ΔA – T ΔS
ΔGf = Free energy formation.
γ = Surface tension of oil-water interface.
ΔA = Change in interfacial area on microemulsion.
ΔS = Change in entropy of system.
T = Temperature.
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14 Phase Behaviour of Microemulsion
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15 Continue…
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16 Continue…
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18 Continue…
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Components of Microemulsion
19
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20 Oil Component
As compare to long chain alkanes, short chain oil penetrate the tail
group region to a greater extent and resulting in increased negative
curvature (and reduced effective HLB).
Following are the different oil are mainly used for the formulation
of microemulsion:
1. Saturated fatty acid-lauric acid, myristic acid,capric acid
2. Unsaturated fatty acid-oleic acid, linoleic acid,linolenic acid
3. Fatty acid ester-ethyl or methyl esters of lauric, myristic and oleic
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21 Continue…
The main criterion for the selection of oil is that the drug should
have high solubility in it.
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22
Surfactants
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23 Co-surfactants
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24 Continue…
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25
Types of Microemulsiom
O/W Microemulsion
W/O Microemulsion
Bi continuous Microemulsion
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26 Preparation of Microemulsion
Drug has to dissolve in to oil phase(lipophilic part) of
microemulsion.
Water phase is combined with the surfactant and then cosurfactant
is added slowly with constant stirring until the system is become
transparent.
The amount of surfactant and co-surfactant to be added and the
parent oil phase that can be incorporated is determined with the
help of pseudo ternary phase diagram.
Ultrasonicator can finally used to achieve the desired range for the
dispersed phase.
It is then allow to equilibrate.
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27 Continue…
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28
Figure shows the pseudo-ternary phase diagram with the area inside the frame
assigned on the phase diagram showing the micro-emulsion region. The area
outside the frame indicates a turbid region with multiphase systems. It could be
noted that the area of micro-emulsion region was considerably large since 1-
butanol acted as a co-surfactant and interacted with the surfactant monolayer to
increase the flexibility of the interfacial film.
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Phase
29 Behaviour
Studies
Viscosity Scattering
Measurement Technique
Characterization
Interfacial Nuclear
Tension, Magnetic
Electric Resonance
Conductivity Studies
Electron
Microscopic
studies
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30 1. Phase Behaviour Studies
This study is very much essential for the determination of
surfactant by using phase diagram which provide information on
the boundaries of the different phases as the function of
composition variables and temperature and more important
structural organization can also be inferred.
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2. Scattering Technique
31
In this technique Small Angle X-ray Scattering(SAXS), Small Angle Neutron
Scattering(SANS) and static as well as dynamic light scattering are widely
applied technique in the study of microemulsion.
In this technique, the intensity of scattered radiation I(q) is maesured as
a function of scattering vector q,
q = (4π/λ) sin θ/2
θ = Scattering Angle.
λ = Wavelength of Radiation.
Small Angle X-ray Scattering technique and Static Light Scattering
techniques both are used to determine the microemulsion droplet size
and shape.
Dynamic Light Scattering is used to analyse the fluctuation in the 11/21/2014
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33 4. Electron Microscopic Studies
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5. . INTERFACIAL TENSION, ELECTRICAL
34 CONDUCTIVITY AND VISCOSITY MEASUREMENTS
Formation and properties of micro emulsion can be studied by the
measuring of Interfacial Tension. Ultra low values of Interfacial
Tension are correleated with phase behaviour, particularly the
existance of surfactant phase or middle phase micro emulsion in
equilibrium with aqueous and oil phase.
To determine the nature of the continuous phase and to detect
phase inversion phenomena the electrical conductivity
measurement are highly useful.
Viscosity measurements can indicates the presence of rod like or
warm like reverse micelles. It is used to determine the
hydrodynamic radius of droplets, as well as interaction b/w droplets
and deviations from spherical shape by fitting the results to
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appropriate models.
35
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36 Advantages:
Increase the rate of absorption
Eliminates variability in absorption
Helps solubilize lipophilic drug
Provides a aqueous dosage form for water insoluble drugs
Increases bioavailability
Various routes like tropical, oral and intravenous can be used to deliver the
product.
Rapid and efficient penetration of the drug moiety
Helpful in taste masking
Provides protection from hydrolysis and oxidation as drug in oil phase in o/w
micro-emulsion is not exposed to attack by water and air.
Liquid dosage form increases patient compliance.
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Micro-
emulsions in Oral drug
biotechnolo delivery.
gy
Applications
Ocular and
Topical drug
pulmonary
delivery.
delivery.
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39 Parenteral Administration:
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40 Oral Drug Delivery system:
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41 Topical drug Delivery System:
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42 Occular & Pulmonary Delivery:
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43 Microemulsion in Biotechnology:
Deltalipid (10%, Soya oil (10%/20%) Egg Phospholipids --- Glycerol (2.5%)
20%) (1.2%/1.2%) NaOH
Oleic Acid (0.3%)
Intralipid (10/20) Soya oil (10%/20%) 3-sn-PC from Egg --- Glycerol (2.5%)
yolk NaOH
(0.6% / 1.2%)
Intralipid 30 Soya oil 30% 3-sn-PC from Egg --- Glycerol (1.67%)
yolk (30%) NaOH
Lipofundin MCT Soya oil + Middle Egg Phospholipids --- Glycerol (2.5%)
(10%/20%) chain Triglycerides (min 68% 3-sn-PC) NaOH
(5%/10% each) (0.8 % / 1.2%) Sod. Olate
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α Tocopherol
Proprietary Name Oil Phase (w/v) Emulsifier (w/v) Active Other Ingredients
Ingredients
49 (w/v)
Diazepam Lipuro (1% Soya Oil + Middle Egg Lecithin Diazepam Glycerol
/ 2%) Chain Triglycerides (1% / 2%) Sod. Oleate
NaOH
Disoprivan Soya Oil 3-sn-PC Propofol Glycerol
(1% / 2%) (1% / 2%) NaOH
Etomidat Lipuro Soya Oil + Middle Egg Lecithin Etomidate Glycerol
Chain Triglycerides Sod. Oleate
NaOH
Lipotalon Soya Oil (10%) Egg Phospholipids Dexamethason Glycerol
(1.2%) e-21-palmitate
(0.4%)
Propofol Abbot 1% Soya Oil Egg Lecithin Propofol (1%) Glycerol
NaOH
Stesolid Soya Oil Phospholipids Diazepam (3%) Glycerol, Acetylated
from egg yolk Monoglycerides, NaOH
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50 Conclusion
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51
Thank You
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