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M. Pharm, PhD.
Department of Pharmaceutics KLE Universitys College of Pharmacy Belgaum-590010 E-mail: bknanjwade@yahoo.co.in Cell No: 00919742431000
Nanocrystal
Definition: Drug nanocrystals are nanoparticles being composed of 100% drug without any matrix material. Methods of production: - Bottom up technology: Precipitation - Top down technology: High pressure homogenization
NIPER, Chandigarh 2
08/02/2010
Objectives of the study: To increase the drug solubility & dissolution. To increase the drug bioavailability.
Materials: Drug: Lovastatin (Krebs biochemicals Pvt. Ltd., Hyderabad) Solvents: Acetone, Methanol, Acetonitrile
08/02/2010
NIPER, Chandigarh
08/02/2010
NIPER, Chandigarh
Sr. no.
Code
Organic solvent
LVS Concentration in Volume of solvent LVS solution (mM) (ml) 3 mM 4 mM 3 mM 12.3 ml 10.8 ml 12.3 ml 10.8 ml 12.3 ml 10.8 ml
Dilution of LVS solution to water Volume of water (ml) 615 ml 540 ml 615 ml 540 ml 615 ml 540 ml
5
1. 2. 3. 4. 5. 6.
Acetone
Methanol
4 mM 3 mM 4 mM
Acetonitrile
NIPER, Chandigarh
a) Particle morphology
b) Particle size analysis c) Crystalline state evaluation - Powder X-ray diffraction (PXRD) - Differential scanning calorimetry (DSC) d) Solubility determination e) In vitro release study f) In vivo evaluation
g) Stability study
08/02/2010 NIPER, Chandigarh 6
F1 A Pure LVS
F2 A
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1000 803.71 Avg. particle size (nm) 800 579.33 600 400 200 0 620 584.58 711.85
848.06
F1A
F1B
F2A
F2B
F3A
F3B
08/02/2010
NIPER, Chandigarh
08/02/2010
NIPER, Chandigarh
08/02/2010
NIPER, Chandigarh
10
Sr. No
Media used
F1A
F1B
F2A
F2B
F3A
F3B
2.
3.
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NIPER, Chandigarh
11
F1B
F2A
F2B
F3A
F3B
Pure LVS
12
NIPER, Chandigarh
F1A
F2A
08/02/2010
NIPER, Chandigarh
13
Code
------0.826 0.821
------1.015 1.010
2 5* 2 2
Drug content after 30 days storage of F1A Code Percent drug content at 40C Percent drug content at 300C20C / 65% 5% RH Percent drug content at 400C20C/ 65% 5% RH
F1A
66.46%
66.32%
60.54%
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NIPER, Chandigarh
15
Continued.. Release study of F1A stored at 40C, at 300C20C / 65% 5% RH and 0 % Cumulative LVS % Cumulative LVS at 400C2 C/ 65% % Cumulative LVS5% RH
Time (Min.) release stored at 40C release stored at 30 C20C / 65% 5% RH
0
From the particle morphology by SEM, it was observed that LVS nanocrystals remain crystalline. Less particle size was observed in case of F1A & F2A as compared to all other. From PXRD and DSC data, it was observed that F1A , F2A & F3A showed no significant change in crystalline as compared to pure LVS. Solubility was enhanced due to less particle size & solvent used (acetone & methanol).
NIPER, Chandigarh 17
08/02/2010
In-vitro release rate studies showed that the maximum drug release was found in the F1A & F2A in the required period of time. In-vivo relative bioavailability of F1A & F2A was slightly increased as compared to absolute bioavailability. From stability study data it was revealed that nanocrystals of lovastatin remained more stable at 4C. The maximum instability of nanocrystals was observed at 402C.
NIPER, Chandigarh 18
08/02/2010
THANK YOU.
08/02/2010 NIPER, Chandigarh
E-mail: bknanjwade@yahoo.co.in 19