pH-triggered drug release from biodegradable microwells for oral drug delivery
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pH-triggered drug release from biodegradable microwells for oral drug delivery. / Nielsen, Line Hagner; Nagstrup, Johan; Gordon, Sarah; Keller, Stephan Sylvest; Østergaard, Jesper; Rades, Thomas; Müllertz, Anette; Boisen, Anja.
In: Biomedical Microdevices, Vol. 17, 55, 06.2015.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - pH-triggered drug release from biodegradable microwells for oral drug delivery
AU - Nielsen, Line Hagner
AU - Nagstrup, Johan
AU - Gordon, Sarah
AU - Keller, Stephan Sylvest
AU - Østergaard, Jesper
AU - Rades, Thomas
AU - Müllertz, Anette
AU - Boisen, Anja
PY - 2015/6
Y1 - 2015/6
N2 - Microwells fabricated from poly-L-lactic acid (PLLA) were evaluated for their application as an oral drug delivery system using the amorphous sodium salt of furosemide (ASSF) as a model drug. Hot embossing of PLLA resulted in fabrication of microwells with an inner diameter of 240 μm and a height of 100 μm. The microwells were filled with ASSF using a modified screen printing technique, followed by coating of the microwell cavities with a gastro-resistant lid of Eudragit® L100. The release behavior of ASSF from the coated microwells was investigated using a μ-Diss profiler and a UV imaging system, and under conditions simulating the changing environment of the gastrointestinal tract. Biorelevant gastric medium (pH 1.6) was employed, after which a change to biorelevant intestinal release medium (pH 6.5) was carried out. Both μ-Diss profiler and UV imaging release experiments showed that sealing of microwell cavities with an Eudragit® layer prevented drug release in biorelevant gastric medium. An immediate release of the ASSF from coated microwells was observed in the intestinal medium. This pH-triggered release behavior demonstrates the future potential of PLLA microwells as a site-specific oral drug delivery system.
AB - Microwells fabricated from poly-L-lactic acid (PLLA) were evaluated for their application as an oral drug delivery system using the amorphous sodium salt of furosemide (ASSF) as a model drug. Hot embossing of PLLA resulted in fabrication of microwells with an inner diameter of 240 μm and a height of 100 μm. The microwells were filled with ASSF using a modified screen printing technique, followed by coating of the microwell cavities with a gastro-resistant lid of Eudragit® L100. The release behavior of ASSF from the coated microwells was investigated using a μ-Diss profiler and a UV imaging system, and under conditions simulating the changing environment of the gastrointestinal tract. Biorelevant gastric medium (pH 1.6) was employed, after which a change to biorelevant intestinal release medium (pH 6.5) was carried out. Both μ-Diss profiler and UV imaging release experiments showed that sealing of microwell cavities with an Eudragit® layer prevented drug release in biorelevant gastric medium. An immediate release of the ASSF from coated microwells was observed in the intestinal medium. This pH-triggered release behavior demonstrates the future potential of PLLA microwells as a site-specific oral drug delivery system.
U2 - 10.1007/s10544-015-9958-5
DO - 10.1007/s10544-015-9958-5
M3 - Journal article
C2 - 25981751
VL - 17
JO - Biomedical Microdevices
JF - Biomedical Microdevices
SN - 1387-2176
M1 - 55
ER -
ID: 144456645