PREPARATION AND EVALUATION OF MICROSPHERE OF

ANTIDIABETIC DRUG BY EMULSION SOLVENT

EVAPORATION METHOD

NAME: KOUSHIK NARAYAN SARMA

UNDER THE GUIDANCE OF
M.PHARM, 4TH SEMESTER
MR. SUJIT DAS
ROLL NUMBER: 18HMPS05 DEPARTMENT OF PHARMACEUTICS
DEPARTMENT OF PHARMACEUTICS
 INTRODUCTION

• The conventional method of treatment has numerous disadvantages like the lack of safety and efficacy.
Therefore, targeted drug delivery system has gained so much response in recent era. They are called as
smart delivery system where drug can be directly administered into pre-selected target cell or tissue in a
specific manner without causing adverse reaction.
• So, there is numerous delivery systems that has been introduced to achieving controlled and targeted
treatment therapy via various routes of administration. In current years, Microsphere drug delivery system
has received glorious attentiveness in all over the world. Microspheres, also known as Micro particles are
small particles with the particle size range 1-200 micrometer.
• Microsphere has been recognized as a promising carrier of drugs in targeted delivery system as well as
various therapeutically active agent containing natural or/synthetic biodegrable polymers. Microspheres are
free flowing particle and can be homogeneously dispersed throughout the dispersion medium (solvent).
• Microsphere for oral route has a great advantage of sustain release of the drug. Microsphere spread out
more consistently and thus lowering specific side effects that has been produced in GI tract with compared
to other dosage form. Hence, to modify or delay the drug release, microspheres are considered as
significant choice.

• Diabetes mellitus is a complex phenomenon resulting in a big number of setbacks throughout the
world. It is estimated as one of the five major causes of death globally. Almost 150 million people are
affected by Diabetes internationally.

• Metformin (the proposed antidiabetic drug) is a white crystalline, hygroscopic powder of a 1, 1-

dimethyl biguanide analog used as an antidiabetic drug.

• Metformin is a drug of choice for newly diagnosed type-2 diabetes and perhaps the best oral
hypoglycemic agent proven to decrease cardiovascular mortality.
• The drug generally works by suppressing hepatic gluconeogenesis and decreasing glucose output in
the liver. It also increases insulin-mediated glucose disposal in muscle and fat.

• In diabetic patients, the blood sugar level should be maintained at a certain level for a long period. So, a
sustained or controlled release dosage formulation will be beneficial for proper controlling of diabetes
mellitus.

• Microsphere formulations provide longer duration of drug action with minimal gastric irritation. So, the
microspheres of metformin will be very helpful to fight against hyperglycemia for a longer duration
period.
 AIM & OBJECTIVE

1. To prepare microsphere of Anti Diabetic drug by emulsion solvent evaporation method.

2. Evaluation of the prepared microsphere.
 MTERIAL REQUIRED

SL NO NAME OF THE INGREDIENT QUANTITITY

1 DRUG (Metformin HCl) 20gm
2 CHLOROFORM 750 ml
3 ETHYL CELLULOSE 250gm
4 SODIUM CARBOXYMETHYL
100gm
CELLULOSE
5 N- HEXANE 500 ml
6 K2HPO4 50gm
7 KCL 50gm
8 KH2PO4 50gm
9 NA2HPO4 50gm
10 NACL 100gm
 METHODOLOGY

• Microsphere can be prepared by various method. One of the popular methods is emulsion solvent
evaporation method.
FORMULATION CHART

Formulation Drug Polymer Na CMC %

FS1 1 0.5 0.5

FS2 1 1 0.5

FS3 1 1.5 0.5

FS4 1 2 0.5

FS5 1 0.5 1

FS6 1 1 1

FS7 1 1.5 1

FS8 1 2 1
 EVALUATION TEST

• Pre formulation studies

a) Preparation of standard curve of Metformin hydrochloride
b) FTIR studies
c) Solubility test
• Micromeritics properties
a) Bulk density
b) Tapped density
c) Carr’s compressibility index
d) Hausner’s ratio
e) Angle of repose

• Particle size analysis

• Invitro drug release
 RESULT & DISCUSSIONS

PREFORMULATION STUDIES
a) Preparation of standard curve
b) Solubility studies
 Freely soluble in water.
 Slightly soluble in ethanol, methanol.
 Insoluble in acetone, ether.
c) FTIR STUDIES

Fig : IR spectra of Metformin Hcl

Fig: IR spectra of drug and polymer
DETERMINATION OF PARTICLE SIZE

S.No Formulations Particle size

(µm)
1 FS 1 359.9

2 FS 2 482.6

3 FS 3 635.1

4 FS 4 678.2

5 FS 5 368.7

6 FS 6 512.3

7 FS 7 664.1

8 FS 8 713.2
DETERMINATION OF MICROMERITIC PROPERTY

SL NO FORMULATI BULK TRUE HAUSNER’

ON DENSITY DENSITY S RATIO
1 FS 1 0.69 0.86 1.246

2 FS 2 0.67 0.87 1.299

3 FS 3 0.72 0.81 1.125

4 FS 4 0.60 0.79 1.324

5 FS 5 0.75 0.88 1.732

6 FS 6 0.80 0.96 1.203

7 FS 7 0.82 0.99 1.211

8 FS 8 0.76 0.85 1.112

S. No Formulation Angle of repose Consolidation index
%

1 FS1 14.5 13.0

2 FS2 14.7 10.4
3 FS3 15.9 9.7
4 FS4 16.5 8.3
5 FS5 14.3 6.7
6 FS6 17.8 12.5
7 FS7 15.5 8.5
8 FS8 18.7 7.9
INVITRO DRUG RELEASE

• The microspheres prepared with the core: coat ratio of 1:0.5 releases 53% of metformin hydrochloride at 8h.
• 1:1, 1:1.5 and 1:2 ethyl cellulose microspheres releases the drug metformin hydrochloride 51, 47 and 46 %
at 8h, respectively.
• The increase in concentration of ethyl cellulose causes the decreasing rate of drug release. The increasing
concentration of NACMC was slightly retarding the release rate. I.E. The same formulations with 1% CMC
were released 53, 52, 49 and 50 %.
INVITRO RELEASE PROFILE OF MICROSPHERE OF ALL PREPARED FORMULATIONS OF
METFORMIN HYDROCHLORIDE
 CONCLUSION

• Spherical microspheres of ethyl cellulose containing Metformin hydrochloride could be formulated by

emulsion-solvent evaporation technique employing chloroform as the solvent and is industrially feasible
method.
• The particle size was determined by using optical microscope. The uniformity, micromeritic properties and
flow properties were also determined.
• The release of Metformin hydrochloride from the microspheres was slow. The release rate was depended on
the core: coat ratio and size of the microspheres. The release rate was increased as the size of microspheres
was decreased. From the data collected through invitro release profile, we can say that formulation no. 4
(FS4, 1:2) is the best one as it has slower release rate than those other formulation.
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