Influence of Process Parameters on Compressibility, Solubility and Release Characteristics of Melt Sonocrystallized Fenofibrate

Aims: The aim of the present study was to investigate the suitability of the melt sonocrystallization (MSC) technique to modify the processability properties along with solubility and drug release of anti-hyperlipidemic drug fenofibrate (FNO) as a BCS Class II drug candidate.

Study Design: By 32 factorial design.

Place and Duration of Study: The study was performed in Department of Pharmaceutics, Ashokrao Mane College of Pharmacy, Peth-Vadagoan, Tal. Hatkanangale, Dist. Kolhapur, Maharashtra, India-416112 and the duration was two years.

Methodology: Melt sonocrystallized fenofibrate agglomerates (MSC-FNO) were prepared by probe ultrasonicator at varying sonication time (1, 2 and 3 min) and level of amplitude (60, 70 and 80%) by 32factorial design. Prepared MSC-FNO agglomerates were further evaluated for various parameters.

Results: Stable MSC-FNO agglomerates were prepared successfully with adequate percentage yield and drug content having porous surface and different crystal habits such as needles, plates, and some hollow tubes. MSC-FNO has shown improved micrometric properties consequently compressibility and flowability than FNO. Also MSC-FNO has shown increase in solubility and drug release may be due to formation of porous agglomerates witnessed in Scanning Electron Microscopic photographs. These results were well supported by Differential Scanning Calorimetry and X-ray Powder Diffraction which has indicated decrease in crystallinity of drug. As sonication time and amplitude increased properties of MSC-FNO were proportionally improved. Study of Fourier Transform Infrared Spectroscopy revealed that no chemical transition of FNO has occurred during MSC.

Conclusion: Thus MSC is a promising cost-effective technique that may give powder with improved required processability properties with better improvement in solubility and drug release, much needed for BCS class II drugs.