A Review On Formulation and Evaluation of Microemulsion

International Journal of Pharmaceutical Research and Applications
Volume 7, Issue 6 Nov-Dec 2022, pp: 1644-1654 www.ijprajournal.com ISSN: 2456-4494
A Review on Formulation and Evaluation of Microemulsion

1
bhavani, 2Jeeva , 3Karthick,4Raghul, 5Pravin Kumar, 6Vijay
(1)
Professor ,Psv College Of Pharmaceutical Science And Research Krishnagiri , india
(2,3,4,5,6)
Ug Students , Psv College Of Pharmaceutical Science And Research Krishnagiri , india
correspondingauthour:bhavani
---------------------------------------------------------------------------------------------------------------------------------------
Submitted: 10-12-2022 Accepted: 23-12-2022
--------------------------------------------------------------------------------------------------------------------------
ABSTRACT: microemulsions as drug carrier system with other
Microemulsions are one of the best candidates as possible applications.
novel drug delivery system because of their long Key words: Microemulsions, thermodynamically
shelf life, improved drug solubilization with ease of stable, amphiphile, solubilization
preparation and administration. Microemulsions are
thermodynamically stable and optically isotropic I. DEFINITION
liquid solutions of oil, water and amphiphile. They • The term micro emulsion introduced by
have emerged as novel vehicles for drug delivery Schulman and co works.
which allow controlled or sustained release for The term "micro emulsion" refers to a
ocular, percutaneous, topical, transdermal, and thermodynamically stable Iso-tropically clear
parenteral administration of medicaments. dispersion of two immiscible liquids, such as
Microemulsions can be easily distinguished from oil and water, stabilized by an interfacial film
normal emulsions by their low viscosity, of surfactant molecules.
transparency and more accurately their
• A micro-emulsion is considered to be a
thermodynamic stability. Microemulsions have
thermodynamically or kinetically stable liquid
great range of applications and uses such as in dispersion of an oil phase and a water phase, in
pharmaceuticals, agrochemicals, cutting oils,
combination with a surfactant.
biotechnology, food, cosmetics, analytical
applications, environmental detoxification etc. The • The particle size of micro-emulsion range
main objective of this review paper is to discuss about 10 nm to 300 nm .because of the small
particle sizes of micro-emulsion appears as
clear or translucent solution.
DIFFERENTIATION:
DOI: 10.35629/7781-070616441654 Impact Factor value 7.429 | ISO 9001: 2008 Certified Journal Page 1644
Advantages: • Ability to carry both hydrophilic and

• Thermodynamically stable, long shelf life liphophilic drug
• Micro-emulsion act as super solvent for drug • Easy to prepare require no significant energy
• Potential reservoir of liphophilic or hydrophilic • Low viscosity
drug • Helpful in test masking
• Due small droplet size it has large interfacial
area of globule so drug is rapidly released in
external phase when absorption takes place
Disadvantages: interphase.
• Require large amount of surfactant and co When micro emulsion is formed the
surfactant for stabilizing droplets change in A is verylarge due to the large number of
• Limited solubility for high melting substances very small dropletsformed. In order for a micro
emulsion to be formed(transient) negative value
• Stability influenced by environmental was required, it is recognizedthat while value of A
parameter such as temperature and pH
is positive at all times, it is very smalland it is
offset by the entropic component. The
dominantfavorable entropic contribution is very
Theories of Micro Emulsion Formation
large dispersionentropy arising from the mixing of
one phase in the otherin the form of large number
Historically, three approaches have been used to
of small droplets. Howeverthere are also expected
explainmicro emulsion formation and stability.
to be favorable entropiccontributions arising from
They are asfollows-
other dynamic processes suchas surfactant
diffusion in the interfacial layer andmonomer-
micelle surfactant exchange. Thus a negativefree
1- Interfacial or mixed film theories. energy of formation is achieved when
2- Solubilization theories. largereductions in surface tension are accompanied
3- Thermodynamic treatments.-0 bysignificant favorable entropic change. In such
The free energy of micro emulsion formation can cases, microemulsion is spontaneous and the
be considered to depend on the extent to which resulting dispersion isthermodynamically stable
surfactantlowers the surface tension of the oil water
interface andchange in entropy of the system such Formulation of Micro-emulsion Composition:
that, The Major component in micro emulsion system
Gf = γ a - T S are-
Where,
Gf = free energy of formation 1) Oil phase
A = change in interfacial area of micro emulsion 2) Surfactant (primary surfactant)
S = change in entropy of the system T =
temperature 3) Co-surfactant (secondary surfactant)
γ = surface tension of oil water 4) Co-solvent
Component Example
1)-saturated fatty acid- lauric acid, carpic acid

2)unsaturated fatty acid-oleic acid, linolic acid, linolenic acid
Oil
3)fatty acid ester-ethyl or methyl ester of lauric, oleic acid and
myristic acid
Surfactant 1-polyoxyethylene/polysorbate/tween 20,40,60,80

2-sorbitan monolaurate, eggs lecithin
3-sodium dodecyl sulphate
Co-surfactant 1-ethanol, Propanol, butanol, isopropanol, Pentanol, hexanol

2-polyoxyethylene-10-oelyl ether
3-sodium monohexyl phosphate
4-cinnamic alcohol, cinamic alcohol
Preparation Method of Micro-Emulsion: are essentialaspects of the study. As quaternary

Following are the method used for the preparation phase diagram (fourcomponent system) is time
of themicro emulsion: consuming and difficult tointerpret, pseudo ternary
1) Phase titration method phase diagram is oftenconstructed to find the
2) Phase inversion method different zones including microemulsion zone, in
which each corner of the diagramrepresents 100%
Phase Titration Method: of the particular component. The regioncan be
Micro emulsions are prepared by the separated into w/o or o/w micro emulsion bysimply
spontaneous emulsification method (phase titration considering the composition that is whether it isoil
method) and can be depicted with the help of phase rich or water rich.
diagrams. Construction of phase diagram is a Observations should be madecarefully so that the
useful approach to study the complex series of metastable systems are not included.
interactions that can occur when different
components are mixed. Micro emulsions are
formed along with various association structures
(including emulsion, micelles, lamellar, hexagonal,
cubic, and various gels and oily dispersion)
depending on thechemical composition and
concentration of each component. The
understanding of their phase equilibriumand
demarcation
of the phase
boundaries
Phase Inversion Method: system crosses a point of zero

Phase inversion of micro emulsions spontaneouscurvature and minimal surface tension,
occurs as a result ofaddition of excess of the promoting the formation of finely dispersed oil
dispersed phase or in responseto temperature. droplets. This method isreferred to as phase
During phase inversion drastic physicalchanges inversion temperature (PIT) method.Instead of the
occur including changes in particle size that temperature, other parameters such as
canaffect drug release both in vivo and in vitro. saltconcentration or pH value may be considered as
Thesemethods make use of changing the wellinstead of the temperature alone. Additionally,
spontaneouscurvature of the surfactant. For non- atransition in the spontaneous radius of curvature
ionic surfactants, thiscan be achieved by changing can beobtained by changing the water volume
the temperature of thesystem, forcing a transition fraction. Bysuccessively adding water into oil,
from an o/w micro emulsionat low temperatures to initially water dropletsare formed in a continuous
a w/o micro emulsion at highertemperatures oil phase. Increasing thewater volume fraction
(transitional phase inversion). Duringcooling, the changes the spontaneouscurvature of the surfactant
from initially stabilizing a w/omicro emulsion to atthe o/w interface resulting in a discontinuous
an o/w micro emulsion at the inversionlocus. microemulsion at the inversion.
Shortchain surfactants form flexible monolayer
Micro-emulsion as Nano-templates
EVALUATION OF MICROEMULSION emulsions composed of oil phase (LO: short-chain

1. Phase behaviour alcohol = 1:1, w/w), nonionic surfactant (Tween
80) and water were constructed to evaluate the
2. Size and shape impact of co-surfactant type on the dilute ability of
3. Rheology micro-emulsion systems. The solubilization of LO
4. Conductivity was improved in the presence of 1, 3-butylene
glycol. For this reason, microstructural inversion of
5. Zeta potential a water titration line D82 was investigated by dye
6. PH diffusion, conductivity, viscosity and DSC. Micro-
7. Drug release studies emulsions transition from W/O to bi-continuous
occured at 20% water content, and then to O/W
8. Physical stability study structure at 50% water content. In the bi-
continuous phase, the viscosity reduced rapidly by
Phase behavior: the rise of temperature. The structure transition
Lavender essential oil (LO) is widely used affected the free radical scavenging activity. The
as a bioactive component in cosmetics. In this DPPH radical scavenging activity increased
study, the pseudo ternary phase diagrams of micro-
continuously with water content from 10% to 90%, dependent while increased again and peaked at
indicating that increasing free water may accelerate 70% water content in O/W regions. The micro-
the interaction between LO and DPPH radicals. emulsion techniques could be applied as potential
The ABTS radical scavenging activity of W/O and delivery systems to improve the application of
bi-continuous formulations was concentration- poorly water-soluble essential oils.
SIZE AND SHAPE:
RHEOLOGY:
CONDUCTIVITY:
The conductivity measurements help in ZETA POTENTIAL:
determining whether the micro-emulsion system Zeta potential results of the optimized
formed is oil-continuous or water-continuous. The micro-emulsion and its diluted form (100 times
solubilization of water phase in the selected oily diluted with 0.1N HCL) have been shown in Figure
mixture was monitored quantitatively by measuring 3, and were found to be -6.34 mV and -3.02 mV,
the electrical conductivity. The conductivity of the respectively. Aggregation is not expected to take
optimized micro-emulsion (B-9) as determined by place, due to the slightly negative charge of the
the conductivity meter was found to be 0.283 σ. droplets.
From electro conductivity study it can be
concluded that the system is of o/w type.
PH: the dispersion using a calibrated pH meter (Digital

The pH of 10% aqueous solution of the Potentiometer Model EQ-601 Equip-tonics).
base was measured For SA ME systems, it was
measured by direct immersion of the electrode of
the pH meter (Hanna-213, Portugal) in the system. DRUG RELEASE STUDIES:
PH values of the optimized formulation were The in vitro drug release studies were
measured by immersing the electrode directly into performed by using Franz diffusion cell with
cellophane paper. The water jacketed recipient
compartment had total capacity of 25 ml and it had PHYSICAL STABILITY STUDY:

2 arms, one for sampling and another for Selected formulations were centrifuged at
thermometer. The donor compartment had internal 3000 rpm for 30 min. The formulations having no
diameter of 2 cm. The donor compartment was phase separations were taken for the heating and
placed in such a way that it just touches the cooling cycle (freeze thaw cycle). Six cycles
diffusion medium in receptor compartment. The between the temperatures 4°C (refrigerator) and
receptor compartment contained phosphate buffer 45°C in a hot air oven with storage at each
saline (PBS) that was maintained at 37°C ± 1°C. temperature for not less than 48 h were done. The
The membrane was equilibrated before application formulations which were stable at these
of the micro-emulsion equivalent to 10 mg of drug temperatures were selected for further studies.
onto the donor side. Samples were periodically The optimized micro-emulsion
withdrawn from the receptor compartment, formulation was stored at 4°C, room temperature
replacing with the same amount of fresh PBS and 45°C for 3 months and samples were evaluated
solution, and assayed by using a spectrophotometer for physicochemical parameters like globule size
at 254 nm. and drug content at 1 month interval.
Application of micro-emulsion
Sr. Delivery Drug Category Application

No. System
1. Nasal Delivery Diazepam Anticonvulsant or Nasal route for

antiepileptic drug administration of
diazepam is useful
approach for the
rapid onset of action
during the
emergency treatment
of status epilepticus.
2. Ophthalmic Dexamethason Anti-allergic It showed better

Delivery e tolerability and
higher
bioavailability. The
formulation showed
greater penetration in
the eye which
allowed the
possibility of
decreasing the
number of
applications per day.
3. Parenteral vitamins E, A, D, Supplements It suitable for fat

Application and K soluble vitamins and
hydrophobic drugs
4. Oral Paclitaxel Anticancer Micro-emulsion

administration permitted its rapid
and efficient
absorption resulting
in improved oral
bioavailability.
5. Anti-ycotics Micro-emulsions
impart to them
increased drug
loading, enhanced
penetration through
the biological
miconazole, membrances, and
Topical ketoconazole, increased
administration itraconazole bioavailability,
6. Tumor Aclacino-mcycin Antitumor agent Folate-linked micro-

targeting emulsion is feasible
for tumour targeted
ACM delivery. The
study showed that
folate modification
with a sufficiently
long PEG chain on
emulsions is an
effective way of
targeting tumour
cells.
7. Brain targeting Clonazepam Anticonvulsant or Muco-adhesive

antiepileptic drug micro-emulsion
compared to iv. was
found to be 2-fold
higher indicating
larger extent of
distribution of the
drug in the brain.
8. Cosmetic - Moisturizing, soothing They are now being

agents, sunscreens, widely investigated
antiperspirants, body for preparing
cleansing agents. personal care
products with
superior features
such as having
improved product
efficiency, stability.
Current and Future Developments: The full potential of micro-emulsion

systems is yet to be realized. A lot of innovations
are expected to come in the field of micro-emulsion Pharmaceutical, Chemical and Biological
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International Journal of Pharmaceutical Research and Applications

Volume 7, Issue 6 Nov-Dec 2022, pp: 1644-1654 www.ijprajournal.com ISSN: 2456-4494

A Review on Formulation and Evaluation of Microemulsion

Advantages: • Ability to carry both hydrophilic and

1)-saturated fatty acid- lauric acid, carpic acid

Surfactant 1-polyoxyethylene/polysorbate/tween 20,40,60,80

Co-surfactant 1-ethanol, Propanol, butanol, isopropanol, Pentanol, hexanol

Preparation Method of Micro-Emulsion: are essentialaspects of the study. As quaternary

Phase Inversion Method: system crosses a point of zero

EVALUATION OF MICROEMULSION emulsions composed of oil phase (LO: short-chain

SIZE AND SHAPE:

PH: the dispersion using a calibrated pH meter (Digital

compartment had total capacity of 25 ml and it had PHYSICAL STABILITY STUDY:

Sr. Delivery Drug Category Application

1. Nasal Delivery Diazepam Anticonvulsant or Nasal route for

2. Ophthalmic Dexamethason Anti-allergic It showed better

3. Parenteral vitamins E, A, D, Supplements It suitable for fat

4. Oral Paclitaxel Anticancer Micro-emulsion

6. Tumor Aclacino-mcycin Antitumor agent Folate-linked micro-

7. Brain targeting Clonazepam Anticonvulsant or Muco-adhesive

8. Cosmetic - Moisturizing, soothing They are now being

Current and Future Developments: The full potential of micro-emulsion

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