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FORMULATION AND EVALUATION OF
DASATINIB LOADED SOLID LIPID
NANOPARTICLES
Prepared by: Roshan Kailas Ahire
Roll no.32
Guided by: Dr. K. V. Bhambar
Department of Pharmaceutical Quality Assurance
Mahatma Gandhi Vidyamandir’s Pharmacy College ,Panchavati, Nashik
Vision
“To be Centre of professional excellence by contributing
honestly to the pharmacist moulding process”
Mission
Impact high quality education to graduates contribute to all
spheres of professional activities uphold human values and
ethics nurture them into globally competent professionals
Journal Name :- International Journal of
Pharmacy and Pharmaceutical Sciences
Article Name :- FORMULATION AND
EVALUATION OF DASATINIB LOADED SOLID
LIPID NANOPARTICLES
Auther :- M. YASMIN BEGUM1, PRATHYUSHA
REDDY GUDIPATI
Article received :- 27 May 2018
Article revised:- 27 Oct 2018
Article accepted:- 27 Oct 2018
Impact factor:-6.2
Cite score:-14.5 3
Content
• Introduction
• Abstract
• Materials and methods
• Results
• Discussion
• Conclusion
• References
4
Introduction
Although a large number of new drug
molecules with varied therapeutic
potentials have been discovered in the
recent decade, yet most of them are still
in the developmental process.
5
6
To treat Philadelphia
chromosome positive
chronic myeloid
leukemia (Ph+ CML) in
adults and children.
Materials Sources
Dasatinib Aizant laboratories,
Hyderabad.
Stearic acid, ethanol,
chloroform, DMSO
SD Fine Chemicals
Pvt Ltd, Mumbai.
Lecithin and
poloxomer 188
Dr, Reddy’s
Laboratories,
Hyderabad
7
Materials and methods
Analytical analysis
Accurately weighed quantity of DST was
dissolved in little of DMSO followed by pH
4 Acetate buffer and further dilutions were
done using pH 4 Acetate buffer to get the
standard working solutions of 2 to 9 µg/ml.
8
DST Loaded SLNs was prepared by
making an organic phase containing the
drug, stearic acid, and lecithin at varying
ratios into ethyl alcohol (10 ml, 93%
V/V). The aqueous phase was prepared by
dissolving variable amounts of poloxamer
188 in water (50 ml).
9
Preparation of DST loaded SLNs (homogenization)
The organic phase was dropped into the
aqueous phase at a constant rate under
homogenization at 800rpm for 15 min
using a high sheer homogenizer. The
resulting suspension was immediately
transferred to cold distilled water (50 ml).
10
Then the suspension was centrifuged at
5000rpm for 1h. The precipitate was
washed twice with double-distilled water
and suspended in mannitol solution (10 %
w/v). The suspension was lyophilized and
kept at a constant temperature of 4 °C for
further use.
11
12
• Formulation
• Evaluation of DST loaded SLNs
FTIR compatibility studies
FTIR spectrum was recorded over the
region of 400 to 4000 cm-1 for pure drug
alone and along with excipients in
BRUKER FTIR Instrument using KBr
pellet technique.
13
14
Determination of zeta potential
The Zeta Master apparatus (Malvern Instruments,
Malvern.) was used to calculate zeta potential by
determining the electrophoretic mobility of the
optimized formulation. It was obtained by
performing an electrophoresis experiment on the
sample and measuring the velocity of particles.
The Zeta Master apparatus (Malvern
Instruments, Malvern.) was used to calculate
zeta potential by determining the
electrophoretic mobility of the optimized
formulation. It was obtained by performing an
electrophoresis experiment on the sample and
measuring the velocity of particles.
15
• Particle size and morphology
Scanning electron microscopy was used to verify
the uniformity of particle shape and size [9]. The
lyophilized nanoparticles were dropped onto
double-sided carbon tape. They were then vacuum
coated for 45 seconds with a platinum mixture and
examined for morphology with a FE-SEM (JEOL
JSM7500, Thermo Scientific) at 5 kV.
16
Drug entrapment efficiency
The percentage of drug entrapped was
determined by centrifugation method. 10
ml of aqueous suspension was centrifuged
at 10,000 rpm for 20 min. The amount of
drug was detected in the supernatant and in
the pellet.
17
Stability studies
Stability study was conducted for the
formulation F5 having high entrapment
efficiency by storing the formulation at two
different temperatures, 4 °C and 25±2 °C
and the drug content was estimated every
15 d, to find out any change in the
entrapment efficiency of the SLNs
18
RESULTS AND DISCUSSION
Solubility studies
The solubility of DST was found to be 200
mg/ml in DMSO. It was found to be poorly
soluble in water and ethanol. So DMSO
was selected as co-solvent to dissolve DST
during construction of calibration curve.
19
FTIR compatibility studies
20
FTIR compatibility studies
21
22
Zeta potential
23
Scanning electron microscopy
24
CONCLUSION
SLNs have emerged as a promising drug
delivery system in recent years as its
potential is gradually and eventually
being realized. Many drugs having
therapeutic activity are highly lipophilic
in nature. Incorporation and delivery of
such lipophilic active ingredients at the
drug delivery site/target site has always
been a concern.
25
Reference
• Rakesh P, Nitish T. Studies in development of dasatinib nanoformulations. Eur J Pharm
Med Res 2016;3:423-32.
• Saikat R, Rosalynn Q, Adam JM. Structural and physicochemical aspects of dasatinib
hydrate and anhydrate phases. Cryst Growth Des 2012;12:2122-6.
• Siu FW. New dosing schedules of dasatinib for CML and adverse event management. J
Hematol Oncol 2009;2:10-6.
• Sandeep K, Vijaykumar N. A review on improved delivery of poorly soluble compounds
using nanoparticle technology. Drug Delivery Transl Res 2016;6:319-32.
• Lee J. Nanoparticle formulation increases oral bioavailability of poorly soluble drugs:
approaches experimental evidences and theory. Curr Nanosci 2005;1:237–43.
26

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Journal Club Sample M.pharmacy Second year.pptx

  • 1. FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES Prepared by: Roshan Kailas Ahire Roll no.32 Guided by: Dr. K. V. Bhambar Department of Pharmaceutical Quality Assurance Mahatma Gandhi Vidyamandir’s Pharmacy College ,Panchavati, Nashik
  • 2. Vision “To be Centre of professional excellence by contributing honestly to the pharmacist moulding process” Mission Impact high quality education to graduates contribute to all spheres of professional activities uphold human values and ethics nurture them into globally competent professionals
  • 3. Journal Name :- International Journal of Pharmacy and Pharmaceutical Sciences Article Name :- FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES Auther :- M. YASMIN BEGUM1, PRATHYUSHA REDDY GUDIPATI Article received :- 27 May 2018 Article revised:- 27 Oct 2018 Article accepted:- 27 Oct 2018 Impact factor:-6.2 Cite score:-14.5 3
  • 4. Content • Introduction • Abstract • Materials and methods • Results • Discussion • Conclusion • References 4
  • 5. Introduction Although a large number of new drug molecules with varied therapeutic potentials have been discovered in the recent decade, yet most of them are still in the developmental process. 5
  • 6. 6 To treat Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in adults and children.
  • 7. Materials Sources Dasatinib Aizant laboratories, Hyderabad. Stearic acid, ethanol, chloroform, DMSO SD Fine Chemicals Pvt Ltd, Mumbai. Lecithin and poloxomer 188 Dr, Reddy’s Laboratories, Hyderabad 7 Materials and methods
  • 8. Analytical analysis Accurately weighed quantity of DST was dissolved in little of DMSO followed by pH 4 Acetate buffer and further dilutions were done using pH 4 Acetate buffer to get the standard working solutions of 2 to 9 µg/ml. 8
  • 9. DST Loaded SLNs was prepared by making an organic phase containing the drug, stearic acid, and lecithin at varying ratios into ethyl alcohol (10 ml, 93% V/V). The aqueous phase was prepared by dissolving variable amounts of poloxamer 188 in water (50 ml). 9 Preparation of DST loaded SLNs (homogenization)
  • 10. The organic phase was dropped into the aqueous phase at a constant rate under homogenization at 800rpm for 15 min using a high sheer homogenizer. The resulting suspension was immediately transferred to cold distilled water (50 ml). 10
  • 11. Then the suspension was centrifuged at 5000rpm for 1h. The precipitate was washed twice with double-distilled water and suspended in mannitol solution (10 % w/v). The suspension was lyophilized and kept at a constant temperature of 4 °C for further use. 11
  • 13. • Evaluation of DST loaded SLNs FTIR compatibility studies FTIR spectrum was recorded over the region of 400 to 4000 cm-1 for pure drug alone and along with excipients in BRUKER FTIR Instrument using KBr pellet technique. 13
  • 14. 14 Determination of zeta potential The Zeta Master apparatus (Malvern Instruments, Malvern.) was used to calculate zeta potential by determining the electrophoretic mobility of the optimized formulation. It was obtained by performing an electrophoresis experiment on the sample and measuring the velocity of particles.
  • 15. The Zeta Master apparatus (Malvern Instruments, Malvern.) was used to calculate zeta potential by determining the electrophoretic mobility of the optimized formulation. It was obtained by performing an electrophoresis experiment on the sample and measuring the velocity of particles. 15
  • 16. • Particle size and morphology Scanning electron microscopy was used to verify the uniformity of particle shape and size [9]. The lyophilized nanoparticles were dropped onto double-sided carbon tape. They were then vacuum coated for 45 seconds with a platinum mixture and examined for morphology with a FE-SEM (JEOL JSM7500, Thermo Scientific) at 5 kV. 16
  • 17. Drug entrapment efficiency The percentage of drug entrapped was determined by centrifugation method. 10 ml of aqueous suspension was centrifuged at 10,000 rpm for 20 min. The amount of drug was detected in the supernatant and in the pellet. 17
  • 18. Stability studies Stability study was conducted for the formulation F5 having high entrapment efficiency by storing the formulation at two different temperatures, 4 °C and 25±2 °C and the drug content was estimated every 15 d, to find out any change in the entrapment efficiency of the SLNs 18
  • 19. RESULTS AND DISCUSSION Solubility studies The solubility of DST was found to be 200 mg/ml in DMSO. It was found to be poorly soluble in water and ethanol. So DMSO was selected as co-solvent to dissolve DST during construction of calibration curve. 19
  • 24. 24 CONCLUSION SLNs have emerged as a promising drug delivery system in recent years as its potential is gradually and eventually being realized. Many drugs having therapeutic activity are highly lipophilic in nature. Incorporation and delivery of such lipophilic active ingredients at the drug delivery site/target site has always been a concern.
  • 25. 25
  • 26. Reference • Rakesh P, Nitish T. Studies in development of dasatinib nanoformulations. Eur J Pharm Med Res 2016;3:423-32. • Saikat R, Rosalynn Q, Adam JM. Structural and physicochemical aspects of dasatinib hydrate and anhydrate phases. Cryst Growth Des 2012;12:2122-6. • Siu FW. New dosing schedules of dasatinib for CML and adverse event management. J Hematol Oncol 2009;2:10-6. • Sandeep K, Vijaykumar N. A review on improved delivery of poorly soluble compounds using nanoparticle technology. Drug Delivery Transl Res 2016;6:319-32. • Lee J. Nanoparticle formulation increases oral bioavailability of poorly soluble drugs: approaches experimental evidences and theory. Curr Nanosci 2005;1:237–43. 26