Transcript Slide 1

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MICROENCAPSULATION OF DRUG INTO
BIODEGRADABLE POLYMER AS A NOVEL DRUG
DELIVERY SYSTEM
Farahidah Mohamed , Ahmad Fahmi Harun Ismail and Abd Almonem Doolaanea
Department of Pharmaceutical Technology, Faculty of Pharmacy, International Islamic University of Malaysia, 25200 Kuantan Campus,
Malaysia.
Phone: 09-571-6400 Fax: 09-571-6775 E-mail: [email protected]
Abstract Summary
This study was done to observe the effects on the development of Gentamicinloaded PLGA microspheres based on several parameters named as PVA
concentration (1%, 2%, 3%, 4% and 5%), types of surfactant which were Span
80, Span 85, Tween 20, Tween 80, Triton X100 as well as the combination
between Span and Tween. The molecular weight of PLGA was also one of the
parameters used which were 0.2, 0.4 and 1.0 dL/g. The values for HLB according
to the surfactants used were manipulated to get certain level (4, 10, 13.5 and 16)
to observed the effects on the particle size of microspheres that were
fabricated. The microspheres were fabricated using double-emulsion solvent
evaporation method and the above said parameters were used as the
independent variables where they were applied. The particle size of fabricated
micropsheres for every batch was measured using the laser diffraction and the
size less than 10 µm was preferable. The images of micropsheres were taken
using the SEM at different resolutions to observe the external morphology as
well as the shape.
Result & Discussion
* Microspheres of 1% PVA
(scale bar= 2 µm)
* Microspheres of HLB 10
(scale bar= 10 µm)
* Microspheres of Triton
X100 (scale bar= 2 µm)
* Microspheres of 5% PVA
(scale bar= 2 µm)
* Microspheres of 3% PVA
(scale bar= 10 µm)
Objectives
1.
2.
3.
To fabricate microspheres loaded with Gentamicin using double-emulsion
solvent evaporation method by using PLGA 50:50.
To investigate the effects on particle size of microspheres against different
parameters i.e different MW of PLGA, the type of surfactants used, the HLB
values and also the different concentrations of PVA.
To study the external morphology
micropsheres using SEM.
as well as the shape of fabricated
Introduction
Mycoplasma pulmonis is one of the major causes for arthritis which can be
treated with Gentamicin. The conventional way of
administrating
Gentamicin is by giving in a repeated doses for certain period of time to
maintain the bioavailibility of the active ingredient to treat the illness. By
using microspheres loaded with Gentamicin, it is believed that the delivery
the drug i.e Gentamicin can be maintained in a certain period of time without
having to administer multiple doses of drug. The size of less than 10 µm of
the fabricated microspheres containing Gentamicin is the most preferable.
The external morphology as well as the shape of the micropsheres are
observed here as a more efficient method of delivering Gentamicin as well
as to carry the drug to the target area effectively.
Research Methodology
This is the schematic diagram of the procedure to fabricate Gentamicinloaded PLGA microspheres
•Microspheres of
Span 80 + Span 85
(scale bar= 2 µm)
These are some of the SEM images showing clearly the external morphologies of
the micropsheres according to the parameters used i.e the PVA concentration.
The images also show the spherical shape of the micropsheres fabricated with
Gentamicin. The images were taken at different resolutions and depth. Please
refer to the scale bar to get better perspective on the particle size of respective
microspheres.
PVA Conc. (%)
1
2
3
4
5
Particle size (µm)
(mean ± S.D); n=3
11.7
±
0.62
9.26
±
0.03
5.56
±
0.05
3.78
±
0.01
3.36
±
0.01
For PVA concentration, it shows clear reduction pattern
of the diameter size of microspheres as the PVA
concentration is increases. The PVA concentration used
gives inverse proportion to the particle size.
Surfactant
Span
80+85
Tween
20+80
Triton
X100
Span 80 +
Tween 80
Particle
size (µm)
(mean ± S.D);
n=3
15.97
±
0.21
10.53
±
0.15
12.07
±
0.12
9.55
±
0.07
HLB
value
#
Homogenized at
14,500 rpm for 1
min
€
Directly injected
into Aqueous 2
Ω
Particle size
(µm)
(mean ±
S.D); n=3
MW of
PLGA (dl/g)
Particle
size (µm)
(mean ±
S.D); n=3
∆
Homogenized
at 14,500 rpm
for 3 min
4
10
13.5
16
7.16 ±
0.03
5.12 ±
0.03
4.16 ±
0.02
3.96 ±
0.23
0.2
0.4
1.0
9.55 ±
0.07
11.02 ±
0.03
12.20 ±
0.01
* Microspheres of HLB 4
(scale bar= 2 µm)
* Microspheres of HLB 13.5
(scale bar= 2 µm)
In the case of HLB value, as
the value is increasing, the
hydrophilicity of the surfactant
increases. The microspheres tend to form
smaller particles due to the result known as
reverse miscelle.
As the molecular weight increases, the
particle size is also increases. The higher
molecular weight of PLGA means more
viscous the oil phase will be. So the particle
size is increases. Other than that, the water solubility will decrease as the molecular
weight is increases. Hence, the particle size will also increase.
Conclusion
Hardened
microspheres were
washed, collected
and lyophilized.
Continuously
stirred
Hardening
tank
Directly
poured
# Oil Phase which composed of PLGA, DCM and Surfactants
€ Aqueous 1 containing Gentamicin
Ω Primary emulsion (w/o)
∆ Aqueous 2 (secondary emulsion) which composed of different concentration of PVA
The particle size of Gentamicin-loaded PLGA microspheres is very much affected by
all the parameters studied. The combination of the parameters i.e higher
concentration of PVA with lower MW of PLGA used is believed to give smaller
particle size. Fabrication of microspheres using the combination of these
parameters is a promising way to obtain particle size less than 10 µm.
Acknowledgement
A great gratitude goes to Allah for His will, to Kulliyyah of Pharmacy of IIUM for
providing the place to conduct the research. To RMC of IIUM for the research grant
(EDW-B10100-0439) and to those directly or indirectly involved with the research.
IIUM Research, Invention and Innovation Exhibition 2011
‘Enhancing Quality Research and Innovation for Societal Development’