Article open access publication

Polymeric microcontainers improve oral bioavailability of furosemide

International Journal of Pharmaceutics, Elsevier, ISSN 0378-5173

Volume 504, 1-2, 2016

DOI:10.1016/j.ijpharm.2016.03.050, Dimensions: pub.1036982321, PMID: 27033999,

Affiliations

Organisations

  1. (1) Technical University of Denmark, grid.5170.3, DTU
  2. (2) University of Valencia, grid.5338.d
  3. (3) University of Copenhagen, grid.5254.6, KU

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Spain

Denmark

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Europe

Description

Microcontainers with an inner diameter of 223 μm 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.

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NORA University Profiles

Technical University of Denmark

University of Copenhagen

Danish Open Access Indicator

2016: Realized

Research area: Science & Technology

Danish Bibliometrics Indicator

2016: Level 1

Research area: Science & Technology

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Times Cited: 29

Field Citation Ratio (FCR): 8.81

Relative Citation ratio (RCR): 2.07

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Green, Submitted