Development of micro-fibrous solid dispersions of poorly water-soluble drugs in sucrose using temperature-controlled centrifugal spinning

• DOI: 10.1016/j.ejpb.2016.03.021
• Publication Date: 2016-03-21T23:49:27Z
• Authors: Stefania Marano; Susan Anne Barker; Bahijja Tolulope ...; Shahrzad Missaghi; Ali Rajabi-Siahboomi; Duncan Q.M. Craig
• Keywords: Microfiber; Supersaturation

Solid dispersion technology represents a successful approach to addressing the bioavailability issues caused by low aqueous solubility of many Biopharmaceutics Classification System (BCS) Class II drugs. In this study, use high-yield manufacture fiber-based is explored as an alternative monolith production methods. A temperature-controlled solvent-free centrifugal spinning process was used produce sucrose-based microfibers containing poorly water-soluble drugs olanzapine and piroxicam (both BCS II); these were successfully incorporated into basic characteristics fiber diameter, glassy behavior, drug loading capacity drug–sucrose interaction assessment measured. Scanning electron microscopy revealed that bead-free drug-loaded with homogenous morphology diameter in range few micrometers prepared using our process. Differential scanning calorimetric X-ray diffraction analyses showed both carrier present amorphous state microfibers, although case piroxicam-loaded presence small amounts crystalline observed under polarized light Fourier transform infrared spectra. Drug dissolution performance evaluated sink non-sink conditions found be significantly enhanced compared corresponding physical mixtures pure drugs, evidence supersaturation behavior noted conditions. This study has demonstrated microfiber-based dispersions may manufactured possess are favorable for oral absorption