WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

Volume x, Issue x, 1-6. ISSN 2278 – 4357

MICROSPHERE : A BOON IN
PHARMACEUTICALS

ABSTRACT
The present review article introduce about various types of microspheres, different methods of preparation, its
applications and also various parameters to evaluate their efficiency. Microspheres are various types like mag-
netic microspheres, floating microspheres, radioactive microspheres, bioadhesive microspheres, polymeric micro-
spheres, biodegradable polymeric microspheres, synthetic polymeric microspheres and are prepared by methods
like spray drying, solvent evaporation, single emulsion technique, double emulsion technique, phase separation
coacervation technique, spray drying and spray congealing, solvent extraction. Microspheres have wide range of
applications because of controlled and sustained release. Current aim of this review is to study various aspects of
the microsphere drug delivery system Including method of formulation, evaluation parameter and characterization.

About Author : Mr. Ravirajsinh Gohil

KEYWORDS: Microspheres, Types of microspheres, Method of preparation, Application 2

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INTRODUCTION

Microsphere is defined as the small spherical free flowing particles which is of size not more
than 200 micrometer. It can be injects by 18 or 20 number needle. Generally microsphere
composed of protein or synthetic polymers. A microsphere based drug delivery system can
overcome the problems linked with conventional dosage form and improve the therapeutic ac-
tion of drug given. Floating microspheres an example of gastro-retentive drug delivery systems
based on non effervescent approach. Magnetic microspheres Use for target to tumors, The
clearance kinetics, tissue distribution, metabolism i.e. Kinetics and cellular interaction of the
drug are strongly influenced by the behavior of the Carrier. The exploitation of these changes
in pharmacodynamics behavior may lead to enhanced therapeutic efficiency.1−2
Advantages of microsphere
1. Protect the drug from enzymatic and photolytic cleavage hence stable for long time.
2. Decrease dose and increase efficacy.
3. Drug release is constant hence prolonged therapeutic effect.
4. Increase solubility of the poorly soluble drug due to particle size reduction.
5. Provide constant drug concentration in blood there by less or no toxicity.
6. Provides prolonged therapeutic effect.
7. Improve the patient compliance by reducing the dosing frequency.
8. The spherical shape and smaller size makes them to be injected into the body.
9. The morphology of microspheres shows variability in controlled release of drug.
10. Conversion of oil and other liquids to solids for ease of handling.
Disadvantages of microsphere
1. The altered release from the formulations.
2. Thee release rate of the controlled release dosage form may vary from a variety of factors
like GI content and the rate of transit though gut.
3. Differences in the release rate from one dose to another due to manufacturing faults.
4. Microsphere contains large amount of drug dose so if any change in physical integrity of
microsphere that may shows potential toxicity.
5. Dose dumping: loss of physical integrity by various factors like manufacturing faults, crush-
ing and co administering with other drugs.
6. Drug Release reproducibility is difficult.

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TYPES OF MICROSPHERE
1. Bioadhesive microspheres
2. Magnetic microsphere
3. Floating microspheres
4. Mucoadhesive microspheres
5. Radioactive microspheres
6. Polymeric microspheres
A. Biodegradable polymeric microsphere
B. Synthetic polymeric microsphere
1. Bioadhesive microspheres
The word bioadhesive means any substance which binds to biological substance like mucosal
membrane. When bioadhesive drug delivery device attached to a biological membrane it pro-
vides prolonged contact at site of administration. Due to the prolonged contact at the site
of administration there will be greater absorption of particular drug and prolonged residence
time thus it reduce the dosing frequency and improve the patient compliance. Microsphere,
nanospheres, liposome, nanoparticle drug delivery system which modifies the absorption and
release pattern of the drug. Microsphere is one of the most important part of these particulate
drug delivery system.3
2. Magnetic microsphere
Magnetic microsphere is very much important which target the drugs to the particular disease
site. In magnetic microsphere the large amount of release circulating drug can be replaced with
small amount of magnetically target drug. After that microsphere is injected in the body. The
high strength magnetic field is applied externally over the target organ to gather microsphere
at the target site. Therapeutic magnetic microsphere delivers the chemotherapeutic agent to the
liver tumor.4
3. Floating microspheres
The bulk density of floating microspheres is less than the gastric fluid so it floats over the gastric
content in stomach without affecting gastric emptying rate. If the system is floating on gastric
content it produce release of drug at desirable rate & increases stomach residence time. The
drug ketoprofen is given in floating microsphere. Floating microspheres reduces the chances of
dose dumping and provide prolonged therapeutic effect.5

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4. Mucoadhesive Microspheres
Mucoadhesive microspheres are defined as the microsphere which are of size 1-1000 mm made
up of mucoadhesive polymers. Mucoadhesive microspheres has following additional advan-
tages like enhanced bioavailability & efficient absorption of drugs. Mucoadhesive microspheres
can adhere to the any mucosal tissue membrane of eye, nasal cavity, GIT & thus provides great
possibilities of systemic & controlled released of drugs.6
5. Radioactive microspheres
Radioactive microsphere is of size 10-30 nm. Generally radioactive microspheres are differ
from other drug delivery systems. The different types of radioactive microsphere are α Emit-
ters, β emitters, γ emitters. There is no radioactivity released from microsphere. Radioactive
microsphere are injected to the arteries that lead to tumor of interest. That produce high rate of
radiation at the target site without damaging surrounding tissues.
6. Polymeric microspheres
A. Biodegradable Polymeric microsphere
Biodegradable polymeric microsphere are made up of biodegradable, biocompatible & bioad-
hesive polymer like starch. When this biodegradable polymer comes in contact with aqueous
medium it swells & produce gel like structure. Due to this property biodegradable polymer
prolongs the residence time. The release of drug from biodegradable polymeric microsphere is
controlled by concentration of polymer & release pattern in a sustained manner.7
B. Synthetic polymeric microsphere
Synthetic polymeric microsphere are widely used in field of clinical application, moreover that
also used as bulking agent, fillers, embolic particles, drug delivery vehicles. But here the main
disadvantage is that when synthetic polymeric microsphere is injected to body that might tend
to be migrate from the injection site to surrounding tissue organ that may lead to potential at
risk and toxicity.8
METHOD OF PREPARATION
The choice of method for the preparation of microsphere depends upon the nature of drugs
and polymer used and it also depends on the duration of therapy. There are several important
chemical factor that may be controlled in microsphere manufacture are
• Molecular weight of polymer
• Release of active reagent with a good control over a wide time controlled particle Size and

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dispensability in aqueous vehicles for injection

• Reproducibility
• Total mass of drug and polymer
• Final product should be non-toxic.
1. Single emulsion technique
In single emulsion technique first the natural polymers are dissolved in aqueous media followed
by dispersion of heated oil. i.e. non aqueous medium that lead to the

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ACKNOWLEDGMENTS

I am very thankful to my guide Ms. Grishma Dalal, the person who makes me to follow the
right step during the review project. I expressed my deep sense of gratitude to Ms. Payal Vaja
for his guidance, suggestion and expertise at every stage. A part from that his valuable and
expertise, suggestion during documentation of my report indeed help me a lot. I would heartily
thankful to head of department Dr. C. J. Tank to give me an opportunity to work over this

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project and for their endless and great support.

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