A stable hydrocortisone nanosuspension for improved dissolution: Preparation, characterization and in vitro evaluation

• Published in: Pakistan journal of pharmaceutical sciences Vol. 30; no. 5; pp. 1635 - 1643
• Main Authors: Ali, Hany Sm, Khan, Shahzeb, York, Peter, Shah, Syed Mukarram, Khan, Jahangir, Hussain, Zahid, Khan, Barkat Ali
• Format: Journal Article
• Language: English
• Published: Pakistan Pakistan Journal of Pharmaceutical Sciences 01-09-2017
• Subjects: Bioavailability; Dosage and administration; Drug delivery systems; Hydrocortisone; Properties; Suspensions (Chemistry); Testing
• ISSN: 1011-601X

Drug nanosuspensions have gained tremendous attraction as a platform in drug delivery. In the present work, a nanosuspension was prepared by a wet milling approach in order to increase saturation solubility and dissolution of the water insoluble drug, hydrocortisone. Size of the generated particeles was 290 nm ± 9 nm having a zeta potential of -1.9 mV ± 0.6 mV. Nanosized particles were found to have a rod shape with a narrow particle size distribution (PDI =0.17). Results of differential scanning calorimetry and X-ray diffraction analyses revealed minor modifications of crystallinity of hydrocortisone following the milling process. Solubility of hydrocortisone was enhanced by nanonization to 875µg/ml ±2.5, an almost 2.9-fold compared to the raw hydrocortisone. Moreover, the nanosuspension formulation substabtially enhanced the dissolution rate of hydrocortisone where >97% of the hydrocortisone was dissolved within 10 minutes opposed to 22.3% for the raw 50% for the raw hydrocortisone and the commercial tablet, respectively. The bioavailability study resulted in AUC 0-9h for HC nanosuspensions (31.50±2.50), which is significantly (p<0.05) higher compared to the AUC
(14.85±3.25) resulted for HC solution. The nanosuspension was physically stable at room temperature for 24 months.