Background: Organic porous material is a promising carrier for enhancing the dissolution of poorly water soluble drug. The aim of the present study was to enhance dissolution and oral bioavailability of lovastatin (LV) by preparing a porous starch microsphere foam (PSM) using a novel method, meanwhile, looking into the mechanism of improving dissolution of LV.
Methods: PSM was prepared by the W/O emulsion – freeze thawing method. The porous structure of PSM was characterized by scanning electron microscopy (SEM) and nitrogen adsorption/desorption analysis. The adsorption role of nanopores on the drug dissolution and physical state of LV was systematically studied by instrumental analysis, and in vitro and in vivo drug dissolution studies. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to evaluate carrier cytotoxicity.
Results: The SEM images of PSM showed nanometer-sized pores. Physical state characterization indicated that porous structure effectively limited the degree of crystallinity of LV. The results of in vitro and in vivo tests testified that PSM accelerated the release of LV and enhanced its oral bioavailability in comparison with crude LV and commercial capsules. The loaded PSM powder indicated a good physical stability under storage for 12 months. MTT assay shows PSM has no toxicity for Caco-2 cell.
Conclusion: The preparation was a promising method to produce small and uniform PSM with markedly enhanced dissolution rate and oral bioavailability due to the spatial confinement effect of porous structure. The present work demonstrates the significant potential for the use of PSM as a novel delivery system for poorly water soluble drugs. 相似文献
By optical microscopy, transmission electron microscopy and energy dispersive spectroscopy, the changes with aging time in size, composition and distribution of nanometer-sized (Ti, Mo)C precipitated in Ti-Mo low-alloy ferritc steel have been studied in comparison with that of nanometer-sized TiC precipitated in Ti low-alloy ferritc steel. It was found that the growth rate of (Ti,Mo)C in Ti-Mo steel was less than that of TiC in Ti steel. Nanometer- sized carbides formed at 650 ~C (or 550 ~C) for 55 h were at transitional stage from growth to coarsening. When aging time reaches 55 h, the coarsening rates of nanometer-sized carbides in Ti and Ti-Mo steel tend to be the same and in- variable. The influence of Mo on growth and coarsening of nanometer-sized carbides tends to decrease with increasing aging time, and Mo contents in nanometer-sized carbides with the same size at different aging time were different. 相似文献