From concept to in vivo testing: Microcontainers for oral drug delivery

Chiara Mazzoni; Fabio Tentor; Sophie Andersen Strindberg; Line Hagner Nielsen; Stephan Sylvest Keller; Tommy Sonne Alstrøm; Carsten Gundlach; Anette Müllertz; Paolo Marizza; Anja Boisen

doi:10.1016/j.jconrel.2017.10.013

From concept to in vivo testing: Microcontainers for oral drug delivery

Chiara Mazzoni^*, Fabio Tentor, Sophie Andersen Strindberg, Line Hagner Nielsen, Stephan Sylvest Keller, Tommy Sonne Alstrøm, Carsten Gundlach, Anette Müllertz, Paolo Marizza, Anja Boisen

^*Corresponding author for this work

32 Citations (Scopus)

Abstract

This work explores the potential of polymeric micrometer sized devices (microcontainers) as oral drug delivery systems (DDS). Arrays of detachable microcontainers (D-MCs) were fabricated on a sacrificial layer to improve the handling and facilitate the collection of individual D-MCs. A model drug, ketoprofen, was loaded into the microcontainers using supercritical CO₂ impregnation, followed by deposition of an enteric coating to protect the drug from the harsh gastric environment and to provide a fast release in the intestine. In vitro, in vivo and ex vivo studies were performed to assess the viability of the D-MCs as oral DDS. D-MCs improved the relative oral bioavailability by 180% within 4 h, and increased the absorption rate by 2.4 times compared to the control. This work represents a significant step forward in the translation of these devices from laboratory to clinic.

Original language	English
Journal	Journal of Controlled Release
Volume	268
Pages (from-to)	343-351
Number of pages	9
ISSN	0168-3659
DOIs	https://doi.org/10.1016/j.jconrel.2017.10.013
Publication status	Published - 28 Dec 2017

Keywords

Enteric coating
Microtechnology
Oral drug delivery
Supercritical impregnation

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10.1016/j.jconrel.2017.10.013

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title = "From concept to in vivo testing: Microcontainers for oral drug delivery",

abstract = "This work explores the potential of polymeric micrometer sized devices (microcontainers) as oral drug delivery systems (DDS). Arrays of detachable microcontainers (D-MCs) were fabricated on a sacrificial layer to improve the handling and facilitate the collection of individual D-MCs. A model drug, ketoprofen, was loaded into the microcontainers using supercritical CO2 impregnation, followed by deposition of an enteric coating to protect the drug from the harsh gastric environment and to provide a fast release in the intestine. In vitro, in vivo and ex vivo studies were performed to assess the viability of the D-MCs as oral DDS. D-MCs improved the relative oral bioavailability by 180% within 4 h, and increased the absorption rate by 2.4 times compared to the control. This work represents a significant step forward in the translation of these devices from laboratory to clinic.",

keywords = "Enteric coating, Microtechnology, Oral drug delivery, Supercritical impregnation",

author = "Chiara Mazzoni and Fabio Tentor and Strindberg, {Sophie Andersen} and Nielsen, {Line Hagner} and Keller, {Stephan Sylvest} and Alstr{\o}m, {Tommy Sonne} and Carsten Gundlach and Anette M{\"u}llertz and Paolo Marizza and Anja Boisen",

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day = "28",

doi = "10.1016/j.jconrel.2017.10.013",

language = "English",

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T1 - From concept to in vivo testing

T2 - Microcontainers for oral drug delivery

AU - Mazzoni, Chiara

AU - Tentor, Fabio

AU - Strindberg, Sophie Andersen

AU - Nielsen, Line Hagner

AU - Keller, Stephan Sylvest

AU - Alstrøm, Tommy Sonne

AU - Gundlach, Carsten

AU - Müllertz, Anette

AU - Marizza, Paolo

AU - Boisen, Anja

PY - 2017/12/28

Y1 - 2017/12/28

N2 - This work explores the potential of polymeric micrometer sized devices (microcontainers) as oral drug delivery systems (DDS). Arrays of detachable microcontainers (D-MCs) were fabricated on a sacrificial layer to improve the handling and facilitate the collection of individual D-MCs. A model drug, ketoprofen, was loaded into the microcontainers using supercritical CO2 impregnation, followed by deposition of an enteric coating to protect the drug from the harsh gastric environment and to provide a fast release in the intestine. In vitro, in vivo and ex vivo studies were performed to assess the viability of the D-MCs as oral DDS. D-MCs improved the relative oral bioavailability by 180% within 4 h, and increased the absorption rate by 2.4 times compared to the control. This work represents a significant step forward in the translation of these devices from laboratory to clinic.

AB - This work explores the potential of polymeric micrometer sized devices (microcontainers) as oral drug delivery systems (DDS). Arrays of detachable microcontainers (D-MCs) were fabricated on a sacrificial layer to improve the handling and facilitate the collection of individual D-MCs. A model drug, ketoprofen, was loaded into the microcontainers using supercritical CO2 impregnation, followed by deposition of an enteric coating to protect the drug from the harsh gastric environment and to provide a fast release in the intestine. In vitro, in vivo and ex vivo studies were performed to assess the viability of the D-MCs as oral DDS. D-MCs improved the relative oral bioavailability by 180% within 4 h, and increased the absorption rate by 2.4 times compared to the control. This work represents a significant step forward in the translation of these devices from laboratory to clinic.

KW - Enteric coating

KW - Microtechnology

KW - Oral drug delivery

KW - Supercritical impregnation

U2 - 10.1016/j.jconrel.2017.10.013

DO - 10.1016/j.jconrel.2017.10.013

M3 - Journal article

C2 - 29054373

AN - SCOPUS:85032678984

SN - 0168-3659

VL - 268

SP - 343

EP - 351

JO - Journal of Controlled Release

JF - Journal of Controlled Release

ER -

From concept to in vivo testing: Microcontainers for oral drug delivery

Abstract

Keywords

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