title: Development of a novel starch with a three-dimensional ordered macroporous structure for improving the dissolution rate of felodipine.
abstract: In this study, silica nanospheres with different particle sizes were used as hard template for synthesis of a starch with a novel three-dimensional ordered macroporous structure (3DOMTS). As a pharmaceutical adjuvant, 3DOMTS was used to improve the dissolution rate and oral relative bioavailability of water-insoluble drugs. Felodipine (FDP) was chosen as a model drug and was loaded into the 3DOMTS by solvent evaporation. FDP loading into 3DOMTS with different pore sizes was characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), differential scanning calorimeter (DSC), powder X-ray diffractometer (PXRD) and Fourier-Transform Infrared (FTIR). The results obtained showed that FDP was present in the pores in an amorphic or microcrystalline state. The in vitro dissolution results showed that 3DOMTS could effectively improve the dissolution rate of FDP in comparison with commercial common tablets. Pharmacokinetic results indicated that the oral relative bioavailability of self-made FDP-3DOMTS tablets were 184%, showing that 3DOMTS produced a significantly increased oral absorption of FDP. In conclusion, 3DOMTS exhibits the dual potential of improving the dissolution rate of poorly water soluble drugs and the novel filler produced by direct compression technology confirming that 3DOMTS will be useful for many applications in the field of pharmaceutics.
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Yanna
authors.initials: Y
authors.lastname: Hao
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China. Electronic address: wuchao27@126.com.
authors.forename: Chao
authors.initials: C
authors.lastname: Wu
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Zongzhe
authors.initials: Z
authors.lastname: Zhao
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Xu
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Qiu
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Jiang
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Tong
authors.initials: T
authors.lastname: Yu
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Chunyu
authors.initials: C
authors.lastname: Ma
authors.affiliation: Pharmacy School, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
authors.forename: Buyun
authors.initials: B
authors.lastname: Zhou
mesh_terms: D000818:Animals; D002236:Carbohydrate Conformation; D015736:Felodipine / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D016062:Porosity; D011817:Rabbits; D012995:Solubility; D013213:Starch / Q000737:chemistry* / Q000648:ultrastructure*
chemical_list: D013213:Starch; D015736:Felodipine
keywords: Felodipine; Insoluble drug; Relative bioavailability; Starch; The dissolution rate; Three-dimensional ordered macroporous