A green route to beclomethasone dipropionate nanoparticles via solvent anti-solvent precipitation by using subcritical water as the solvent

Abstract

Oral beclomethasone dipropionate (BDP) has been extensively studied in the management of ulcerative colitis in clinical practice in recently years. However, the effective bioavailability and absorption of BDP are limited by its poor water solubility when administered orally. Herein, we report a green process for the synthesis of BDP nanoparticles via solvent anti-solvent precipitation, in which the subcritical water (SBCW) and cold water were used as the solvent and anti-solvent respectively. Polyethylene glycol (PEG), a non-ionic, hydrophilic polymer was introduced as stabilizers in the SBCW process to obtain sub-50nm BDP nanoparticles with improved dissolution rate. Scanning electronic microscopy (SEM), Fourier transform infrared (FTIR) spectrophotometry, powder X-ray diffraction (XRD) and dissolution tests were performed to investigate the corresponding particle morphology, structure and dissolution rate properties of the BDP nanoparticles. The obtained BDP nanoparticles are <50nm in diameters with uniform distribution, exhibiting similar chemical structures, lower crystallinity and much higher dissolution rate than the raw BDP drug. These results show that as-synthesized BDP nanoparticles are promising for oral administration of BDP towards the management of ulcerative colitis.