1. Preparation and Characterization of Piroxicam
Microcrystals, for Better Dissolution Profile
Mohammed Dahmash

2. Main Points
• Discuss the dissolution problem of piroxicam and
how to solve it.
• Elaborate on how the 0.3% of Kolliphor® EL
surfactant produce micronized crystals.

3. Introduction
• The poor dissolution of hydrophobic drugs results in:
High drug precipitation, low drug absorption,
low drug bioavailability, GI injury and high cost(1).
1. Harvey, R A, Clark M A & Finkel R. Chapter 41: Anti-inflammatory Drugs. Lippincott's Illustrated Reviews:
Pharmacology. New York : Lippincott Williams & Wilkins, 2009, p. 508.

4. Aim and Objectives
 Enhance the dissolution of piroxicam by using in-situ
crystallization method with the aid of Kolliphor® EL.
Then, analyse the obtained crystals by various
techniques to investigate the micronization effects.

5. Materials and Methods
• Kolliphor® EL,
• In situ crystallization(2),
• Lyophilisation,
• Paddle-apparatus dissolution,
• Polarized microscopy,
• Zeta size analyser (ZSA), and
• Fourier-transform infrared spectroscopy (FTIR).
2. Rasenack, N, Steckel, H & Müller, B. Preparation of microcrystals by in situ micronization. Journal of
Powder Technology, Vols. 143-144, 2004, pp. 291-296.

6. Results and Discussion
• A significant increase in dissolution with both 0.1 and
0.3% of Kolliphor® EL (p-values≤0.05) and
significant decrease in the effective diameter with
0.3% of Kolliphor® EL (p=0.0375), result in:
Decreased particle size and surface tension, increased
surface area and wettability(3).
3. Elkordy AA, Jatto A & Essa E. In situ controlled crystallization as a tool to improve the dissolution of
Glibenclamide. International Journal of Pharmaceutics, Vol. 428, 2012, pp. 118-120.

7. The dissolution profile of piroxicam in different
formulations
0.3 % of
Kolliphor® EL
0.1% of
Kolliphor® EL
ControlRaw
drug

8. Piroxicam microcrystals of 0.3% Kolliphor® ELPiroxicam crystals of 0.1% Kolliphor® EL
Raw piroxicam Piroxicam crystals without Kolliphor® EL

9. Results and Discussion
(Continued)
• Enhanced “in process” stability with 0.1 and 0.3% of
Kolliphor® EL, mainly because the amide stretch of
piroxicam was conserved (4)
Piroxicam structure, highlighting its amide group
4. Watson, D G. Infrared Spectroscopy. Pharmaceutical Analysis: A Textbook for Pharmacy Students and
Pharmaceutical Chemists. Philadelphia, USA: Elsevier Churchill Livingstone, 2005, pp. 113-125.

10. 500100015002000250030003500
0.55
0.6
0.65
0.7
0.75
0.8
0.85
0.9
0.95
1
Transmittance
Wavenumbers [cm-1]
Amide stretch of piroxicam at 3336 cm-1
Raw piroxicam

11. 500100015002000250030003500
0.625
0.7
0.8
0.9
1
1.025
Wavenumbers [cm-1]
Primary amine that resulted
from amide hydrolysis
Transmittance
Piroxicam crystals without
Kolliphor® EL
EL

12. 500100015002000250030003500
0.4
0.5
0.6
0.7
0.8
0.9
1
1.1
Wavenumbers [cm-1]
Amide stretch of piroxicam
was conserved
Transmittance
Piroxicam crystals with
0.1 and 0.3% of Kolliphor® EL

13. Conclusion
• The microcrystallized formulation can be obtained
with 0.3% of Kolliphor® EL and used to enhance
piroxicam dissolution, to result in:
less GI side effects and high cost-effectiveness.
• Future work...
The Tunable Resistive Pulse Sensing (TRPS) device
would be recommended to be used for:
obtaining more accurate information based on particle
by particle sizing of piroxicam micro/nano-crystals.

14. Acknowledgements
• I thank with gratitude and sincerity:
Miss Zahra Batool,
Mrs Muna Al-lami,
Dr Amal Elkordy, and
Dr Cheng Chaw.

15. Thank you
Any questions ?