Aceclofenac is an analgesic and anti-inflammatory drug that reduces fever, pain, and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. Aceclofenac has higher anti-inflammatory action than conventional NSAIDs. Development of microspheres is a promising technology for controlled release and drug targeting. Various types of microspheres such as bio-adhesive, magnetic, floating, radioactive and polymeric microspheres are developed for various purposes. Microspheres occupied a central place in novel drug delivery, it can targeted and localized drug delivery system. This Aceclofenac Microsphere is Prepared by using Spray drying Technique in which release rate of drug is mainly depends on formulation composition (Eudragit RS 30 D and Ethyl Cellulose (1:2 ratio)). Formulated microspheres were characterized for particle size, encapsulation efficiency and In vitro studies. The optimum drug-to-polymer ratio and feed flow rate is responsible for higher percent yield, smaller particle size and maximum encapsulation efficiency.

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FORMULATION AND EVALUATION OF MICROSPHERES WITH ACECLOFENAC
Sagar Kishor Savale1*
*1
Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur 425405, Dist.
Dhule Maharashtra State, India.
Article Received on 04/06/2016 Article Revised on 25/06/2016 Article Accepted on 15/07/2016
INTRODUCTION[1, 2, 3, 4, 5, 6, 7, 8]
Microspheres have played a vital role in the development
of controlled/sustained release drug delivery systems.
Microspheres have been of particular interest from the
pharmaceutical point of view providing the possibility to
achieve sustained and controlled drug release.
Microspheres are matrix systems that contains drug
throughout their structure and are potential candidates for
oral controlled release. Microsphere can be defined as
solid spherical particles ranging from one to 1000 μm in
size. The microspheres are free flowing powders
consisting of proteins or synthetic polymers, which are
biodegradable in nature. Microsphere is prepared by
various techniques in which Aceclofenac Microsphere is
prepared by using Spray drying technique. Spray drying
is defined has the solidification is done by rapid
evaporation coatings solution contain in coating
polymeric material. Aceclofenac is a Non-Steroidal Anti-
inflammatory drug (NSAIDS). Aceclofenac is important
to show the Analgesic as well as anti-inflammatory
activity for the prevention of Inflammation. The Basic
mechanism action of drug to inhibit the COX I, COX II,
(Cyclooxygenase I and Cyclooxygenase II) is
Responsible for the Inflammation. The chemically
Aceclofenac is known as 2-[[2-[2-[(2, 6-dichlorophenyl)
amino] phenyl] acetyl] oxy] acetic acid. It is important to
give symptomatic treatment of rheumatoid arthritis,
osteoarthritis and ankylosingspondylitis. Aceclofenac is
a drug is important to prevent the problem associated in
gastric irritation and maintain the stability of GI
environment. Aceclofenac is a drug is mainly used for
the treatment of mild, moderate, postoperative pain and it
is effective against menstrual pain and endometriosis.
MATERIAL AND METHOD
Material
Aceclofenac and all Formulation Excipient (Eudragit RS
30 D, Ethyl cellulose, Iso Propyl Alcohol) was obtained
from Pharmaceutics Laboratory of R. C. Patel Institute of
Pharmaceutical Education and Research, Shirpur
425405, Maharashtra State, one of the NBA and NAAC
accredited and AICTE Approved institutes in India.
Method
The parameters of Authentication and Preformulation is
carried out by pure drug Aceclofenac for Maintaining
their Quality, Purity and Standard.
AUTHENTICATION PARAMETERS[9,10,11,12,13,14,15]
Melting Point Method
Melting Point determination is one of the preformulation
property in which the temperature at which it changes
state from solid to liquid at atmospheric pressure. At the
melting process the solid and liquid can exist
equilibrium. The Melting point of Aceclofenac pure
wjpmr, 2016,2(4), 181-187 SJIF Impact Factor: 3.535
Research Article
ISSN 2455-3301
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WORLD JOURNAL OF PHARMACEUTICAL
AND MEDICAL RESEARCH
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*Corresponding Author: Sagar Kishor Savale
Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur 425405, Dist. Dhule Maharashtra State,
India.
ABSTRACT
Aceclofenac is an analgesic and anti-inflammatory drug that reduces fever, pain, and inflammation in rheumatoid
arthritis, osteoarthritis and ankylosing spondylitis. Aceclofenac has higher anti-inflammatory action than
conventional NSAIDs. Development of microspheres is a promising technology for controlled release and drug
targeting. Various types of microspheres such as bio-adhesive, magnetic, floating, radioactive and polymeric
microspheres are developed for various purposes. Microspheres occupied a central place in novel drug delivery, it
can targeted and localized drug delivery system. This Aceclofenac Microsphere is Prepared by using Spray drying
Technique in which release rate of drug is mainly depends on formulation composition (Eudragit RS 30 D and
Ethyl Cellulose (1:2 ratio)). Formulated microspheres were characterized for particle size, encapsulation efficiency
and In vitro studies. The optimum drug-to-polymer ratio and feed flow rate is responsible for higher percent yield,
smaller particle size and maximum encapsulation efficiency.
KEY WORDS: Microspheres, Spray drying, Aceclofenac, Particle size, Encapsulation Efficiency.

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drug is determine by using two types of method one is
Conventional method and another is Digital method.
Log P Value
Log p value is determined by using Partition Coefficient
Phenomenon. In which The 1 gm of drug is added in
separating funnel containing equal portion of 25 ml of
Octanol and 25 ml of Water. The separating funnel is
shake 20 – 25 min. and stabilized the mixture. After
stabilizing the mixture to remove water phase from
separating funnel and filter it. Take Absorbance of
Filtrate and calculate the log p value.
Solubility Studies
The Term Solubility is defined as maximum amount of
solute that can be dissolved in a given amount of solvent
to form a homogenous system at specified temperature
and Specific Pressure to from Saturated Solution.
Procedure
 To Prepare a different solutions Water, PH 1.2
Acidic Buffer, PH 6.8 Phosphate Buffer, PH 7.4
Phosphate Buffer.
 The drug material is added in to above solutions till
Supersaturated Solution is from.
 The Mixture can Placed in Orbital Shaker for 24 hrs.
After 24 hrs. Filter the mixture Take Filtrate and
Give Absorbance.
 To detect the Concentration of Drug is Soluble in
Different Solutions.
Calibration Curve of Aceclofenac
Calibration Curve is determined by using UV
Spectrophotometric methods. In which 10 mg drug is
added in 100 ml of water (100 μg/ml Solution). To
Prepared different Dilutions (0, 2, 4, 6, 8, 10, 12) of
above solution (100 μg/ml Solution). Take Absorbance
in respective λmax 276 nm.
PREFORMULATION STUDIES[16, 17, 18, 19]
Drug-Excipient Compatibility Studies
Drug is an active part of dosages form and it is mainly
responsible for therapeutic value and Excipient
substances which are included along with drugs being
formulated in a dosage form so as to impart specific
qualities to them. It’s also used for development of new
drug delivery system as well as investigation of new drug
Product.
Procedure
The Equal portion of Drug and Excipient (1:1 ratio) is
added in Ampules and the Ampules are placed in
Stability Chamber for one Weak, After One Weak the
Drug Excipient Compatibility Study is Determine by
using TLC (Thin Layer Chromatography), (n-hexane:
Ethyl acetate: acetic acid (7: 0.5: 2.5)), IR (Infrared
Spectroscopy) and DSC (Differential Scanning
Colariometry).
Method of Formulation
Aceclofenac Microspheres is prepared by spray-drying
Technique. In 1 gm of drug and 1 gm Eudragit RS 30 D,
1 gm Ethyl cellulose (Drug-to-polymer ratio 1:2, 1:3,
1:4, 1:5) is added in 100 ml Iso propyl alcohol (100 ml
beaker)., Beaker (100 ml solution) was placed in
mechanical stirrer at 5000 rpm, by using spray-dryer
apparatus, the solution was fed to the nozzle with a
peristaltic pump, atomized by the force of compressed air
and blown together with heated air to the chamber where
the solvent in the droplets was evaporated. The dried
microparticles were harvested from the apparatus
collector. All Formulation Ingredients was reported in
Table 1 and Parameters for the preparation of
microspheres is reported in Table 2.
EVALUTION PARAMETERS[20, 21, 22, 23, 24, 25, 26, 27, 28]
Particle size analysis
Particle size analysis was performed by Motic
microscopy method with imaging facility by using
advanced Motic digital microscope. Total 200 particles
were measured for each formulation and the average
particle size was calculated.
Encapsulation efficiency
Microparticles of sample was weighed and then
completely dispersed in distilled water (100 ml (100 ppm
solution)), the solution was placed in orbital shaker for
24 hrs. , for complete solubilization of Aceclofenac.
After 24 hrs. Sample was filter and take absorbance by
using suitable analytical technique (UV spectroscopy) at
λmax of 276 nm. And determine Concentration of active
constituent in solution. Following formula was used for
calculation of encapsulation efficiency.
Encapsulation Efficiency % = Practical drug content
/ Theoretical drug content × 100
In-vitro dissolution testing
In vitro study of Aceclofenac microspheres or
Microparticles is conducted in pH 6.8 Phosphate buffer
was used as a dissolution medium. Microparticles
equivalent to 50 mg of Aceclofenac were weighed
accurately, and then dispersed into the dialysis
membrane. Then the membrane was placed into the
basket and rotated at 100rpm. Samples were withdrawn
at the time interval of 30, 60, 90, 120, 150 and 180. The
volume equivalent to sample withdrawn was replaced by
dissolution medium to maintain the sink condition.
RESULTS AND DISSCUSION
Authentication Parameters
Melting Point Method
The Melting Point of Aceclofenac is determined by
Conventional and Digital Method and Melting Point of
Aceclofenac is reported in Table 3.

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Log P Value
Log P Value is determined by Partition Coefficient
Phenomenon and Log P Value of Aceclofenac is
reported in Table 3.
Solubility Studies
The Solubility of Aceclofenac in Given Solution. (Water,
PH 1.2 Acidic Buffer, PH 6.8 Phosphate Buffer, PH 7.4
Phosphate Buffer) is Reported in Table 4 and Solubility
of Pure drug Aceclofenac in Different solvent is shown
in Figure 1.
Calibration Curve of Aceclofenac in water
The Calibration Curve of Aceclofenac is determined by
using U.V. Spectroscopic Method. In which the
Absorbance of Aceclofenac in Different Concentration
(0, 2, 4, 6, 8, 10, and 12) is reported in Table 5. And The
Calibration Curve is shown in Figure 2.
PREFORMULATION STUDIES
The Drug and Excipient Compatibility studies
determined by TLC (Thin Layer Chromatography) and
IR (Infrared Spectroscopy) Method In which The TLC of
Drug, Drug and Excipient before Stability Chamber and
After Stability Chamber is reported in Table 6 and TLC
(For drug excipient Compatibility) Shown in Figure
3.The IR of Drug taken. The IR Spectra of Pure drug
Aceclofenac is shown in Figure 4. The DSC of pure drug
Aceclofenac is reported in Figure 5.
EVALUTION PARAMETERS
Particle size analysis
Average particle size was calculated and reported in
Table 7. The Particle size is determined by using Motic
Microscopy, Digital image of Microsphere was shown in
Figure 6.
Encapsulation efficiency
Encapsulation Efficiency is calculated and reported in
Table 7.
In-vitro dissolution testing
In-vitro dissolution testing of Aceclofenac Microsphere
is conducted and reported in Table 7.
Table 1: Formulation Ingredients for Preparation of Microsphere.
Formulation ingredient F1 F2 Fop
Aceclofenac (gm) 0.5 (gm) 0.8 (gm) 1 (gm)
Eudragit RS 30 D (gm) 0.5 (gm) 0.8 (gm) 1 (gm)
Ethyl cellulose (gm) 0.5 (gm) 0.8 (gm) 1 (gm)
Iso Propyl Alcohol (ml) 100 (ml) 100 (ml) 100 (ml)
Table 2: Parameters for the preparation of microspheres (Spray dryer Instrument).
Parameters Conditions
Outlet Temperature 50˚c
Inlet temperature 80˚c
Plate Temperature 0
Tube Temperature 0
Cool Temperature 80
Drug-to-polymer ratio 1:2, 1:3, 1:4
Feed flow rate 20,30,40, 60, 80 (ml/min)
Inlet high 220
Outlet high 160
Aspirator Speed 45-80
Feed Pump 10
Plate Speed 0
D. block on 1
D block off 90
Cycle Time 225
Log Interval 1
Table 3. Melting Point of Aceclofenac
Sr.No. Parameters Experimental Result Std.
1 Melting Point (˚c) 151 – 159˚c 152 -153˚c
2 Log p Value 2.16 2.17

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Table 4: Solubility of Aceclofenac in different solvents.
Sr. No. Medium
Concentration of drug Soluble
(mg /ml)
1 Water 2.01 (mg /ml)
2 PH 1.2 Acidic Buffer 2.80 (mg /ml)
3 PH 6.8 Phosphate Buffer 4.0 (mg /ml)
4 PH 7.4 Phosphate Buffer 4.82 (mg /ml)
Result Class of drug BCS Class II
Table 5: Calibration of Aceclofenac in Water.
Conc(µg/ml) Absorbance
0 0
3 0.148
5 0.246
8 0.434
10 0.535
12 0.632
15 0.808
Table 6: TLC of Drug and Drug: Excipient.
Table 7: Evalution of Aceclofenac Microsphere.
Experimental parameters F1 F2 FOP
Average Particle size (mm) 35.21 25.35 23.9
Encapsulation efficiency (%) 90.56 95.25 98.76
In Vitro Drug Release (%) 92.12 96.52 97.27
Figure 1: Solubility studies in different solvents
Sr.
No.
Samples
(Pure From of Drug material)
(Drug + Excipient Mixture)
Retention factor of drug
Before the Stability
Chamber
Retention factor of
drug After the Stability
Chamber
1 Pure Drug Aceclofenac 0.76 0.79
2 Aceclofenac + Eudragit RS 30D 0.80 0.81
3 Aceclofenac+ Ethyl cellulose 0.74 0.76
4 Aceclofenac+ Iso Propyl Alcohol 0.70 0.72

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Figure 2. Calibration curve of Aceclofenac in Water
Figure 3: TLC Studies (For Drug: Excipient Compatibility)
Figure 4: IR of Pure drug Aceclofenac

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Figure 5: DSC of Pure drug Aceclofenac.
Figure 6: Average Particle size by using Motic Microscopy.
Figure 7. In vitro drug release of Aceclofenac in pH 6.8 phosphate buffer (Fop).
CONCLUSION
Aceclofenac Microsphere is prepared by Spray drying
Technique by employing a Eudragit RS 30 D and Ethyl
cellulose is responsible for slow release of drug and
shows sustained release activity. Particle size and
encapsulation Efficiency of the Aceclofenac loaded
Eudragit RS 30 D and Ethyl Cellulose microspheres was
found to be highly dependent on the Drug-to-polymer
ratio and feed flow rate of spray Dryer. The release
Microsphere is mainly depended on the composition of
Microsphere Formulation Material. The result associated
in Optimized batch is good to Satisfactory.

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ACKNOWLEDGEMENT
The authors are grateful to Hon. Principal, SES’s, R. C.
Patel Institute of Pharmaceutical Education and
Research, Dr. S. J. Surana sir. A special gratitude to Dr.
H.S. Mahajan sir Head, Dept. of Pharmaceutics and
Quality assurance. Without whom and their constant
caring and loving support we would be unable to achieve
this advancement and precious stage of our life.
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