Comparison of Spray Freeze Drying and the Solvent Evaporation Method for Preparing Solid Dispersions of Baicalein with Pluronic F68 to Improve Dissolution and Oral Bioavailability |
| |
Authors: | Xiuqiong He Lixia Pei Henry H Y Tong Ying Zheng |
| |
Institution: | (1) Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China;(2) School of Health Sciences, Macao Polytechnic Institute, Macao SAR, China; |
| |
Abstract: | The objective of this study was to prepare solid dispersions consisting of baicalein and a carrier with a low glass transition/melting
point (Pluronic F68) by spray freeze drying (SFD). We compared these powders to those produced from the conventional solvent
evaporation method. In the SFD process, a feeding solution was atomized above the surface of liquid nitrogen following lyophilization,
which resulted in instantaneously frozen microparticles. However, solid dispersions prepared by the solvent evaporation method
formed a sticky layer on the glass flask with crystalline baicalein separated out from the carrier. The powder samples were
characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), surface area measurement, differential
scanning calorimetry, and Fourier transform infrared spectrometry. SEM and PXRD results suggested that the majority of baicalein
in the SFD-processed solid dispersion was in the amorphous state, which has a higher specific surface area than pure baicalein.
However, the majority of baicalein was recrystallized in the solid dispersion at the same composition prepared by the solvent
evaporation method, which showed a similar dissolution rate to the physical mixture. SFD product was physically and chemically
stable after being stored at 40°C with low humidity for 6 months. After enzyme hydrolysis, baicalein in the SFD product displayed
a significantly shorter T
max and higher C
max than pure baicalein after oral dosing. The relative bioavailability of the SFD product versus pure baicalein determined by comparing the AUC0–12 was 233%, which demonstrated the significantly improved oral bioavailability of baicalein produced by the SFD technique. |
| |
Keywords: | |
本文献已被 SpringerLink 等数据库收录! |
|