title: Preparation of novel porous starch microsphere foam for loading and release of poorly water soluble drug.
abstract: 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.
  
  
  CONCLUSIONS
  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.
authors: Department of Pharmaceutics, Shenyang Pharmaceutical University , Shenyang, Liaoning Province , China .
authors: Tongying
authors: T
authors: Jiang
authors: Chao
authors: C
authors: Wu
authors: Yikun
authors: Y
authors: Gao
authors: Wenquan
authors: W
authors: Zhu
authors: Long
authors: L
authors: Wan
authors: Zhanyou
authors: Z
authors: Wang
authors: Siling
authors: S
authors: Wang
mesh_terms: D000818:Animals; D018938:Caco-2 Cells; D004285:Dogs; D005260:Female; D006801:Humans; D008297:Male; D008863:Microspheres; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism; D016062:Porosity; D012995:Solubility; D013213:Starch / Q000737:chemistry* / Q000378:metabolism; D014867:Water / Q000737:chemistry* / Q000378:metabolism; D014961:X-Ray Diffraction
chemical_list: D004364:Pharmaceutical Preparations; D014867:Water; D013213:Starch