title: In Vitro Release and Bioavailability of Silybin from Micelle-Templated Porous Calcium Phosphate Microparticles.
abstract: Developing a promising carrier for the delivery of poorly water-soluble drugs, such as silybin, to improve oral absorption has become a very worthy of consideration. The goal of this study was to prepare a novel porous calcium phosphate microparticle using povidone-mixed micelles as template while evaluating its in vitro and in vivo properties with silybin as a model drug. The particle characterization, in vitro drug release behavior, and pharmacokinetic parameters of the prepared silybin-loaded calcium phosphate microparticle were investigated. The mean particle size was found to be 3.54 ± 0.32 μm with a rough surface porous structure. Additionally, the silybin-loaded calcium phosphate microparticle compared with the free silybin showed a prolonged 72-h release in vitro and a higher C max (418.5 ± 23.7 ng mL(-1)) with 167.5% oral relative bioavailability. A level A in vitro-in vivo correlation (IVIVC), established for the first time, demonstrated an excellent IVIVC of the formulated silybin in oral administration. In conclusion, this povidone-mixed micelle-based microparticle was successfully prepared to enhance the oral bioavailability of silybin. Therefore, application of this novel porous calcium phosphate microparticle holds a significant potential for the development of poorly water-soluble drugs.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhu
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China.
authors.forename: Miaomiao
authors.initials: M
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China.
authors.forename: Ya
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China.
authors.forename: Jin
authors.initials: J
authors.lastname: Zeng
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China.
authors.forename: E
authors.initials: E
authors.lastname: Omari-Siaw
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China.
authors.forename: Jiangnan
authors.initials: J
authors.lastname: Yu
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212001, People's Republic of China. xmxu@ujs.edu.cn.|Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China. xmxu@ujs.edu.cn.
authors.forename: Ximing
authors.initials: X
authors.lastname: Xu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002130:Calcium Phosphates / Q000737:chemistry* / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004285:Dogs; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D008297:Male; D008823:Micelles; D010316:Particle Size; D016062:Porosity; D011205:Povidone / Q000737:chemistry / Q000378:metabolism; D000077385:Silybin; D012838:Silymarin / Q000737:chemistry* / Q000378:metabolism*; D012995:Solubility; D014867:Water / Q000737:chemistry
chemical_list: D002130:Calcium Phosphates; D004337:Drug Carriers; D008823:Micelles; D012838:Silymarin; D014867:Water; D000077385:Silybin; C020243:calcium phosphate; D011205:Povidone
keywords: bioavailability; calcium phosphate; porous microparticles; povidone-mixed micelle; silybin