Chitosen microsphere prepared by spray drying

1. Title : Chitosan microspheres prepared by
spray drying
Department of Pharmaceutics
ISF College of Pharmacy,Moga,Punjab
Presented By:
OMPRAKASH SAHU
M.Pharm 1st year
INTERNATIONAL
JOURNAL OF
PHARMACEUTICS
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2. Flow of presentation
 Introduction
 Methods of preparation
 Characterisation of microsphere
 Result and discussion
 Conclusion
 References
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3. Introduction
 Chitosan is a hydrophilic, biocompatible and biodegradable
polysaccharide of low toxicity, which in recent years has been used
for development of drug delivery systems.
 Non-crosslinked and crosslinked microspheres were prepared by a
spray drying method.
 The microspheres so prepared had a good sphericity and a smooth.
 They were positively charged and particle size range from 2 to 10
µm.
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4. Methods of Preparation
As a comparison, a water insoluble polymer ethyl cellulose(EC) was used to prepare microsphere from 2-4 % polymer
solution in DCM
Yield was formed 200mg to 1g dependent upon the concentration of Chitosan
Spray drying was co-currently performed using a SD-04 Spray dryer(Lab plant, UK)
Dissolving the model drug (16.6 % w/w of cimetidine, famotidine or nizatidine) in the chitosan solution separately
1 % aqueous solution of formaldehyde & glutaraldehyde were added separately as a crosslinking agents
250 ml of a 0.1-0.5 % aqueous solution of chitosan hydrochloride salt containing acetic acid of chitosan free base
were prepared
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(Fig.1)
(Spray dryer)
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5. Characterisation of Microsphere
Droplet size
• Microsphere were sized
using a Malvern
MasterSizer(MS
1002),determines the
volume diameter(VMD) &
polydispersive index(PDI)
Zeta potential
• Zeta potential of the
microsphere was measured
by laser doppler(Malven
zetasizer 4)employing
0.005,0.0005 & 0.001 M
phosphate buffer at pH 7.0
& 0.001 M acetate buffer
at pH 4.0
DSC
• DSC study was performed
using a perkin elmer DSC-2
• Sample was purged with
atmosphere of
Nitrogen,heat flow rate
was recorded from 280 to
520 K,at a rate of 10 K/min.
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6. Physicochemical Characterization of non-
crosslinked chitosan and EC
Microsphere type Size (µm) Zeta potential (mV)
0.001 M pH 4 acetate buffer 0.0001 M pH 7 phosphate
Chitosan
hydrochloride salt
5.58 27.2 24.9
Chitosan free base
4.19 14.8 9.7
EC 5.1 −15.5 −5.2
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7. Graph between the particle size & amount of the
Glutaraldehyde in different concentration of chitosan
microspheres
(Fig.2)3/5/2020
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8. Characteristics of cimetidine loaded
chitosan microspheres
Added Found Efficiency(%) pH4 pH7
Glutaraldehyde (4%)
0.1 1 16.6 15.7 94.7 7.85 17.4 15.0
0.1 2 16.6 13.0 78.3 4.03 15.8 13.6
0.1 4 16.6 11.8 71.0 1.67 15.5 9.1
0.2 1 16.6 16.2 98 4.89 17.3 15.2
0.2 2 16.6 15.6 94 4.62 16.2 14.5
0.2 4 16.6 14.2 85.7 2.93 14.6 13.4
0.2 1 9 8.04 88.5 5.19 17.4 14.4
0.2 2 9 7.11 78.3 4.58 15.5 14.5
0.2 4 9 6.65 73.2 2.22 14.9 13.1
Formaldehyde (1%)
0.2 2 16.6 16.2 97.6 7.91 22.5 17.4
0.2 4 16.6 15.3 92.4 3.89 18.8 15.3
Concentration of chitosan Crosslinking agent (ml) Drug contents (%) Size (µm) Zeta potential (mV) (%)
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9. Determination of drug Content
 For the determination of drug content UV
spectrophotometer(UVIKON 860) were used ,For cimetidine UV
absorption spectra of the sample solution (2-20 µg/mL) were
recorded.
 The absorbance difference at 260 nm were calculated.
 For the determination of famotidine & nizatidine contents, the
absorbance of sample solution (4-20 µg/mL) were recorded at 284
nm & 313 nm respectively.
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10. In-vitro drug release
 The rate of release of the model drugs from the
microspheres in phosphate buffer saline(PSB) was
determined in a dissolution apparatus with the dissolution
paddle assembly(USP apparatus 2).
 30-50 mg of microsphere were suspended in 300 ml of
PBS, pH=7.4 at 37℃ & at 50 rpm agitation rate.
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11. Result and discussion
In vitro Drug release study:-
(Fig.3) (Fig.4) (Fig.5)
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12. Result and Discussion
SEM ANALYSIS:-
SEM of drug free chitosan microspheres prepared from 0.2% aqueous solutions for chitosan hydrochloride salt
(Mw 140 – 160 kDa) by a spray drying method, crosslinked by glutaraldehyde (a), and formaldehyde (b).
SEM of drug loaded (a) cimetidine; (b) famotidine; (c) nizatidine, chitosan microspheres prepared form
0.2% aqueous solutions of chitosan hydrochloride salt (Mw 140 – 160 kDa) by a spray drying method
(Fig.6)
(Fig.7)
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13. Result and discussion
DSC Analysis:-
DSC thermograms of chitosan (a) and model drug (cimetidine (A); famotidine (B)) materials (b),
chitosan– drug physical mixture (c) 10:2; drug free chitosan microspheres (d); and the drug
loaded chitosan microspheres, 10:2 (e).
DSC thermograms of cimetidine material (a) chitosan– cimetidine (b)
30:70; (c) 50:50; (d) 10:2, physical mixture and cimetidine loaded (e)
70%; (f) 50% chitosan microspheres
(Fig.8) (Fig.9) (Fig.10)
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14. Conclusion
 Non-crosslinked and crosslinked chitosan microspheres were prepared by a spray
drying method. The microspheres so prepared had a good sphericity and a
smooth but distorted surface morphology. They were positively charged. The
particle size ranged from 2 to 10 µm.
 The release of model drugs (cimetidine, famotidine and nizatidine) from these
microspheres was fast, and accompanied by a burst effect.
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15. References
 He, Ping, Stanley S. Davis, and Lisbeth Illum.
"Chitosan microspheres prepared by spray
drying." International journal of pharmaceutics 187.1
(1999): 53-65.
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16. THANKYOU
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