Polymeric microcontainers improve oral bioavailability of furosemide

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Polymeric microcontainers improve oral bioavailability of furosemide. / Nielsen, Line Hagner; Melero, Ana; Keller, Stephan Sylvest; Jacobsen, Jette; Garrigues, Teresa; Rades, Thomas; Müllertz, Anette; Boisen, Anja.

In: International Journal of Pharmaceutics, Vol. 504, No. 1-2, 17.05.2016, p. 98-109.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Nielsen, LH, Melero, A, Keller, SS, Jacobsen, J, Garrigues, T, Rades, T, Müllertz, A & Boisen, A 2016, 'Polymeric microcontainers improve oral bioavailability of furosemide', International Journal of Pharmaceutics, vol. 504, no. 1-2, pp. 98-109. https://doi.org/10.1016/j.ijpharm.2016.03.050

APA

Nielsen, L. H., Melero, A., Keller, S. S., Jacobsen, J., Garrigues, T., Rades, T., ... Boisen, A. (2016). Polymeric microcontainers improve oral bioavailability of furosemide. International Journal of Pharmaceutics, 504(1-2), 98-109. https://doi.org/10.1016/j.ijpharm.2016.03.050

Vancouver

Nielsen LH, Melero A, Keller SS, Jacobsen J, Garrigues T, Rades T et al. Polymeric microcontainers improve oral bioavailability of furosemide. International Journal of Pharmaceutics. 2016 May 17;504(1-2):98-109. https://doi.org/10.1016/j.ijpharm.2016.03.050

Author

Nielsen, Line Hagner ; Melero, Ana ; Keller, Stephan Sylvest ; Jacobsen, Jette ; Garrigues, Teresa ; Rades, Thomas ; Müllertz, Anette ; Boisen, Anja. / Polymeric microcontainers improve oral bioavailability of furosemide. In: International Journal of Pharmaceutics. 2016 ; Vol. 504, No. 1-2. pp. 98-109.

Bibtex

@article{3e251dd48cca40028369492ab938e2da,
title = "Polymeric microcontainers improve oral bioavailability of furosemide",
abstract = "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.",
keywords = "Journal Article, Research Support, Non-U.S. Gov't",
author = "Nielsen, {Line Hagner} and Ana Melero and Keller, {Stephan Sylvest} and Jette Jacobsen and Teresa Garrigues and Thomas Rades and Anette M{\"u}llertz and Anja Boisen",
note = "Copyright {\circledC} 2016. Published by Elsevier B.V.",
year = "2016",
month = "5",
day = "17",
doi = "10.1016/j.ijpharm.2016.03.050",
language = "English",
volume = "504",
pages = "98--109",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

RIS

TY - JOUR

T1 - Polymeric microcontainers improve oral bioavailability of furosemide

AU - Nielsen, Line Hagner

AU - Melero, Ana

AU - Keller, Stephan Sylvest

AU - Jacobsen, Jette

AU - Garrigues, Teresa

AU - Rades, Thomas

AU - Müllertz, Anette

AU - Boisen, Anja

N1 - Copyright © 2016. Published by Elsevier B.V.

PY - 2016/5/17

Y1 - 2016/5/17

N2 - 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.

AB - 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.

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

U2 - 10.1016/j.ijpharm.2016.03.050

DO - 10.1016/j.ijpharm.2016.03.050

M3 - Journal article

C2 - 27033999

VL - 504

SP - 98

EP - 109

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

ID: 169133008