Enhancement of abiraterone acetate oral bioavailability by supersaturated-silica lipid hybrids.

Title Enhancement of abiraterone acetate oral bioavailability by supersaturated-silica lipid hybrids.
Authors H.B. Schultz; A.D. Wignall; N. Thomas; C.A. Prestidge
Journal Int J Pharm
DOI 10.1016/j.ijpharm.2020.119264
Abstract

Abiraterone acetate (AbA) has an oral bioavailability of <10% due to its poor water solubility. Here we investigate the performance of silica-lipid hybrids (SLH) and supersaturated SLH (super-SLH) in improving oral bioavailability of AbA. Specifically, we investigate the influence of lipid type and AbA saturation level of the equilibrium solubility in the lipid (S), and explore in vitro-in vivo correlation (IVIVC). An oral pharmacokinetic study was conducted in fasted Sprague-Dawley rats. Suspensions of the formulations were administered via oral gavage at an AbA dose of 25 mg/kg. Plasma samples were collected and analyzed for drug content. SLH with a saturation level of 90% S enhanced the oral bioavailability of unformulated AbA by 31-fold, and super-SLH with saturation levels of 150, 200 and 250% S, enhanced the bioavailability by 11, 10 and 7-fold, respectively. In comparison with the commercial product Zytiga, SLH (90% S) increased the oral bioavailability 1.43-fold whereas super-SLH showed no improvement. A reasonable IVIVC existed between the performance of unformulated AbA, SLH and super-SLH, in the in vitro lipolysis and in vivo oral pharmacokinetic studies. SLH and super-SLH significantly enhanced the oral bioavailability of AbA. Additionally, supersaturation of SLH improved drug loading but did not correlate with enhanced AbA bioavailability.

Citation H.B. Schultz; A.D. Wignall; N. Thomas; C.A. Prestidge.Enhancement of abiraterone acetate oral bioavailability by supersaturated-silica lipid hybrids.. Int J Pharm. 2020;582:119264. doi:10.1016/j.ijpharm.2020.119264

Related Elements

Silicon

14 Si 28.085500000 Silicon

See more Silicon products. Silicon (atomic symbol: Si, atomic number: 14) is a Block P, Group 14, Period 3 element with an atomic weight of 28.085. Silicon Bohr MoleculeThe number of electrons in each of Silicon's shells is 2, 8, 4 and its electron configuration is [Ne] 3s2 3p2. The silicon atom has a radius of 111 pm and a Van der Waals radius of 210 pm. Silicon was discovered and first isolated by Jöns Jacob Berzelius in 1823. Silicon makes up 25.7% of the earth's crust, by weight, and is the second most abundant element, exceeded only by oxygen. The metalloid is rarely found in pure crystal form and is usually produced from the iron-silicon alloy ferrosilicon. Elemental SiliconSilica (or silicon dioxide), as sand, is a principal ingredient of glass, one of the most inexpensive of materials with excellent mechanical, optical, thermal, and electrical properties. Ultra high purity silicon can be doped with boron, gallium, phosphorus, or arsenic to produce silicon for use in transistors, solar cells, rectifiers, and other solid-state devices which are used extensively in the electronics industry.The name Silicon originates from the Latin word silex which means flint or hard stone.

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