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Indian Journal of Science
Analysis
The International Journal for Science
ISSN 2319 – 7730
EISSN 2319 – 7749
© 2016 Discovery Publication. All Rights Reserved
Formulation and evaluation of Aspirin Nanoemulsion
Publication History
Received: 20 January 2016
Accepted: 13 February 2016
Published: 1 March 2016
Page
245
Citation
Selvi PP, Faustina S, Sowmiya A. Formulation and evaluation of Aspirin Nanoemulsion. Indian Journal of Science, 2016,
23(79), 245-252
FORMULATION AND EVALUATION OF ASPIRIN NANOEMULSION
Mrs.P.P.Selvi, Faustina.S, Sowmiya.A
Department of Chemical Engineering
Kongu Engineering College (Autonomous), Perundurai
Email-ID:[email protected]
Keywords – Nanoemulsion, Solubility,
Drug release, Aspirin
INTRODUCTION
Nanoemulsion can be defined as
the oil in water emulsion with mean
droplet diameters ranging from 50 to
1000nm.Usually, the average droplet size
is between 100 and 500nm. The particles
can exist as water in oil, respectively. The
REASONS FOR SELECTION OF
DRUG
The efficacy of many drugs is often
limited by their potential to reach the site
of therapeutic action due to various
problems such as - poor bioavailability, in
vivo stability, solubility, intestinal
absorption, sustained and targeted delivery
to site of action, therapeutic effectiveness.
In most cases only a small amount of
administered dose reaches the target site,
while the majority of the drug distributes
throughout the rest of the body in
accordance with its physicochemical and
biological properties. It is estimated that at
present 40% of New Chemical Entities
under development and60% of synthesized
drugs are poorly water soluble compounds.
Even more 70% of drugs are discarded due
to poor solubility. The dosage form of an
active ingredient can have a great effect on
its solubility and permeability, thereby
affecting bioavailability. Nanonization
forms have better approach for increased
solubility of Drug and leads to an increase
in Bioavailability of the Drug. The BioPharmaceutics
Classification
System
classifies drugs into four groups:
246
Nanoemulsion can be defined as
the emulsions with mean droplet
diameter ranging from 20-500nm used
as targeted drug delivery carrier in
pharmaceutical products. The present
objective is to formulate and evaluate
the nanoemulsion of Aspirin. The first
part of the work is considered to
formulate Aspirin Nanoemulsion to
overcome poor solubility. It is composed
of Aspirin drug, Acetone as solvent,
Arachis oil as oil phase, Tween 80 as
surfactant, Polyethylene Glycol 400 as
Co-Surfactant and Water. Various
formulations
of
Oil
in
Water
Nanoemulsions were prepared by
varying the Smix ratios and formulating
at constant temperature. Nanoemulsions
were evaluated for various parameters
and its compatibility studies were made.
The obtained nanoemulsion has a
particle size of about 111nm. FTIR data
indicate the compatibility nature of
drug in the formulation. The drug
release was up to 77.35% at the end of
3rd hour.
terms Sub-Micron Emulsion (SME) and
Mini emulsion are used as synonyms.
Usually, SME’s contain 10 to 20 percent
oil stabilized with 0.5 to 2 percent egg or
soya bean lecithin. Nanoemulsion are a
group of dispersed particles used for
pharmaceutical and biomedical aids and
vehicles that show a great promise for the
future of Cosmetics, Diagnostics, Drug
Therapies and Biotechnologies.
Page
ABSTRACT
Class 1:
Solubility
High
Permeability,
High
Class 2:
Solubility
High
Permeability,
Low
Class 3:
Solubility
Low
Permeability,
High
Permeability,
Low
As the Drug Aspirin belongs to
Class 4 system of classification it has Less
Solubility
which
leads
to
Low
Bioavailability. To overcome these
problems, Aspirin must be formulated as a
Nanoemulsion in size rage of 20-500nm.
PROPOSED WORK
The ultimate aim of the present work is
to Formulate and Evaluate the Aspirin
Nanoemulsion to increase the solubility of
the Drug.
 To develop an ideal formulation of
Aspirin Nano emulsion.
 To optimize the process parameters
to produce a formulation with
acceptable properties.
 To enhance the Solubility and the
Bioavailability of the Aspirin.
 To evaluate different properties of
prepared
Nanoemulsion
like
Particle size, Density Viscosity,
etc.
 To study the pattern of Drug
Release Kinetics for the prepared
Nano emulsion.
FORMULATION OF
NANOEMULSION
The drug loaded Nanoemulsion
was formulated by dissolving 5mg of the
drug in acetone and adding varying
concentration of oil to the acetonolic drug
EVALUATION OF NANOEMULSION
1. CALIBRATION CURVE FOR
DRUG
10mg of Aspirin was accurately
weighed and dissolved in 100ml of
phosphate buffer solution 7.4. Take 1ml
and make up to 10ml in a standard flask to
produce the concentration of 10µg/ml.
Label this solution as primary stock
solution. Then withdraw 1ml of primary
stock solution and diluted to 10ml in a
standard flask to produce the concentration
of 10µg/ml. This solution is considered as
secondary stock solution. From the
secondary stock solution withdraw 2ml,
4ml, 6ml, 8ml and10ml and make up the
volume to 10ml with phosphate buffer of
pH7.4, in order to produce the
concentration ranging from 2µg/ml,
4µg/ml, 6µg/ml, 8µg/ml and 10µg/ml.
2. PHYSICAL APPEARANCE
The physical appearance of Drug,
Excipients and Formulation were analysed
visually. The Drug Aspirin, Arachis Oil as
Oil Phase, Tween80 as Surfactant, and
Polyethylene Glycol as Co-Surfactant are
observed visually for the Physical
Appearance.
3. PHASE DILUTION TEST
Phase Dilution Test was performed
in order to determine the type of emulsion.
Here few ml of Nanoemulsion is diluted
247
Low
Page
Class 4:
Solubility
solution. The aqueous phase was prepared
by adding Tween 80 and PEG-400 to
distilled water. The oil phase was added to
the aqueous phase drop by drop which is
placed in a magnetic stirrer. It is then
sonicated
for
about
45
mins.
Nanoemulsions are formed. The procedure
was repeated for varying concentration of
oil, surfactant and co-surfactant.
with water and it was visually observed
and confirmed if there was any change in
homogeneous phase.
4. PARTICLE SIZE ANALYSIS
The most important physical
property of particulate samples is particle
size. Particle size analysis, particle
size measurement,
or
simply particle
sizing is the collective name of the
technical procedures, or laboratory
techniques
which
determines
the size range, and/or the average, or
mean size of the particles in a powder or
liquid sample. The Particle Size was
measured by Particle Size Analyzer. It is
important to measure the Particle Size and
necessary to understand how they affect
the products.
5. ZETA POTENTIAL
Zeta Potential is scientific term for
electro kinetic potential. Zeta Potential is
the potential difference existing between
the surfaces of a solid particle immersed in
a conducting liquid. It is determined to
calculate the surface charge of the
formulation. The Zeta Potential is a key
indicator of the stability of colloidal
dispersions.
7. IN-VITRO STUDIES
In-vitro drug release study of
Aspirin Nanoemulsion was performed in
the Magnetic Stirrer with a hot plate with
an agitation speed of 100rpm. One ml of
Aspirin Nanoemulsion was placed in
dialysis bag, sealed at the both ends placed
in a glass beaker. The dissolution medium
used was phosphate buffer saline pH 7.4.
At designed intervals for 3 hours, the
Absorbance was measured by UV-Vis
spectrophotometer
at
265nm.
The
concentration of Aspirin Nanoemulsion
was determined from the calibration graph
and the percentage of drug release was
calculated by respective concentration of
standard calibration curve with suitable
dilution factor.
RESULTS
1. PHYSICAL APPEARANCE
The active substance Aspirin was
in the form of white crystalline powder.
The Tween 80 was amber coloured liquid
and viscous in nature. The Arachis oil was
pale yellow in colour and viscous in
nature. The PEG 400 was a transparent
liquid. The Nanoemulsion was Bluish
translucent dispersion.
Page
The presence of peak at a specific
wave number indicates the presence of a
specific chemical bond. If specific
interaction took place between the
materials, the most obvious and significant
difference would be the appearance of new
peaks or a shift of existing peaks. FT-IR is
used to study the interactions occurring
between drug and excipient by matching
the peaks of spectra.
248
6. FOURIER-TRANSFORM INFRARED SPECTROSCOPY
2. PHASE DILUTION TEST
This test clearly indicates the type
of emulsion to which it belongs. If water
distributes uniformly then it is O/W
Emulsion. If water separates out as a layer
then it is W/O Emulsion. The Formulated
Nanoemulsions belongs to O/W TYPE
since when it is diluted with water, it
distributes uniformly throughout the
solution.
3. PARTICLE SIZE ANALYSIS
NANOEMULSION 3 (1:3) – 111.3nm
5. FOURIER-TRANSFORM INFRARED SPECTROSCOPY
ARACHIS OIL (OIL)
4. ZETA POTENTIAL
TWEEN 80 (SURFACTANT)
Page
249
NANOEMULSION 3 (1:3)
RESULTS
7. IN-VITRO STUDIES
PLOT HIGUCHI
EQUATION
The straight line of linear
regression analysis indicates zero order of
the data yields the equation of best line
with value = 0.8703 and the slope of line
corresponds to the Zero Order Rate
constant was 2.138. The best linearity was
found in Higuchi’s Equation plot =
0.8703 indicating the release of drug from
matrix as a square root of time dependent
process based on Fickian diffusion. The
dissolution data was also plotted in
accordance with Hixson Crowell cube
root law. Applicability of data
= 0.9295 indicates a change in surface area
CONCLUSION
The Major objective of the study
was to develop Aspirin Nanoemulsion for
increasing the solubility thus increasing
the bio availability. The compatibility of
the drugs and the excipients were
performed in pre formulation studies. The
formulations were made by varying the oil
and
surfactant
concentration.
The
formulations were characterized by the UV
spectroscopy, Particle size and Zeta
potential. The impacts of different
surfactant concentrations on drug loading
250
PLOT HIXON CROWELL
EQUATION
and diameter of Nanoemulsion with the
progressive dissolution of matrix as a
function
of
time.
According
to
Korsmeyer-Peppas where n is the release
exponent, indicative of mechanism of drug
release 0.9926. Fickian diffusional release
and a case-II relaxation release are the
limits of this phenomenon. Fickian
diffusional release occurs by the usual
molecular diffusion of the drug due to a
chemical potential gradient. Case-II
relaxation release is the drug transport
mechanism associated with stresses.
Page
PLOT KORSMEYER-PEPPAS
EQUATION
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