Polymeric microcontainers improve oral bioavailability of furosemide

Line Hagner Nielsen, Ana Melero, Stephan Sylvest Keller, Jette Jacobsen, Teresa Garrigues, Thomas Rades, Anette Müllertz, Anja Boisen

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Abstract

Microcontainers with an inner diameter of 223μm are fabricated using the polymer SU-8, and evaluated in vitro, in situ and in vivo for their application as an advanced oral drug delivery system for the poorly water soluble drug furosemide. An amorphous sodium salt of furosemide (ASSF) is filled into the microcontainers followed by applying a lid using Eudragit L100. It is possible to control the drug release in vitro, and in vitro absorption studies show that the microcontainers are not a hindrance for absorption of ASSF. In situ perfusion studies in rats are performed with ASSF-filled microcontainers coated with Eudragit and compared to a furosemide solution. The absorption rate constant of ASSF confined in microcontainers is found to be significantly different from the solution, and by light microscopy, it is observed that the microcontainers are engulfed by the intestinal mucus. An oral bioavailability study in rats is performed with ASSF confined in microcontainers coated with Eudragit and a control group with ASSF in Eudragit-coated capsules. A relative bioavailability of 220% for the ASSF in microcontainers compared to ASSF in capsules is found. These studies indicate that the microcontainers could serve as a promising oral drug delivery system.
Original languageEnglish
JournalInternational Journal of Pharmaceutics
Volume504
Issue number1-2
Pages (from-to)98-109
Number of pages12
ISSN0378-5173
DOIs
Publication statusPublished - 2016

Keywords

  • Micro devices
  • Furosemide
  • Oral delivery
  • Delivery systems
  • Oral bioavailability
  • Intestinal perfusion

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