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

doi:10.1007/s10544-015-9958-5

Cited by 30 publications

(35 citation statements)

References 31 publications

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“…To fully protect the loaded cargo, the microcontainers can be sealed with a lid of e.g. a pH-sensitive polymer to facilitate release in certain regions of the GI tract 11,12,18,19 . More advanced designs have been proposed, where the microdevices are processed as two dimensional objects and then self-fold into container structures upon exposure to liquid 20 .…”

Section: Designmentioning

confidence: 99%

“…More advanced designs have been proposed, where the microdevices are processed as two dimensional objects and then self-fold into container structures upon exposure to liquid 20 . In addition, primarily for proof-of-concept studies, microwells have been reported 18 . The microwells are formed as indentations in a surface and can be used to study e.g.…”

Section: Designmentioning

confidence: 99%

“…Hot punching PLLA, PCL 29 Sealed microcontainers Spray coating Eudragit L100 11,12,18 Sealed microcontainers Thermal bonding PLGA, PC, PMMA 21,30 Microfabrication technologies and materials…”

Section: Microcontainersmentioning

confidence: 99%

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Microfabricated devices for oral drug delivery

Nielsen

Keller

2018

Lab Chip

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Oral administration of drugs is most convenient for patients and therefore the ultimate goal when developing new medication. The physical barriers in the body, low pH of the stomach and degradation by enzymes in the gastrointestinal tract are a few of the obstacles to succeeding with oral drug delivery. Microfabricated devices show promise to overcome some of these hindrances and thereby improve the bioavailability of drugs after oral administration. There is an increasing focus on microfabricated oral drug delivery systems, and so far there have been three main groups of designs: patch-like structures, microcontainers and microwells. Here, we review the newest development in top-down microfabricated devices for oral drug delivery with coverage of the aspects of design, choice of material and fabrication techniques. Furthermore, the drug loading techniques and methods for testing are discussed. In addition, we discuss the future perspectives for microfabricated devices.

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Section: Designmentioning

confidence: 99%

Section: Designmentioning

confidence: 99%

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Microfabricated devices for oral drug delivery

Nielsen

Keller

2018

Lab Chip

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“…Nielsen et al used a modified screen printing technique that involves the use of a stencil mask pre-fabricated by laser machining that aligns on top of microdevices for accessing the vacant reservoirs [124]. The stencil has pores/holes matching the microdevice reservoirs with a high level of precision.…”

Section: Loading Of Novel Micro- and Nanoscale Oral Drug Delivery mentioning

confidence: 99%

Micro/nanofabricated platforms for oral drug delivery

Fox

Kim

et al. 2015

Journal of Controlled Release

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The oral route of drug administration is most preferred due to its ease of use, low cost, and high patient compliance. However, the oral uptake of many small molecule drugs and biotherapeutics is limited by various physiological barriers, and, as a result, drugs suffer from issues with low solubility, low permeability, and degradation following oral administration. The flexibility of micro- and nanofabrication techniques has been used to create drug delivery platforms designed to address these barriers to oral drug uptake. Specifically, micro/nanofabricated devices have been designed with planar, asymmetric geometries to promote device adhesion and unidirectional drug release toward epithelial tissue, thereby prolonging drug exposure and increasing drug permeation. Furthermore, surface functionalization, nanotopography, responsive drug release, motion-based responses, and permeation enhancers have been incorporated into such platforms to further enhance drug uptake. This review will outline the application of micro/nanotechnology to specifically address the physiological barriers to oral drug delivery and highlight technologies that may be incorporated into these oral drug delivery systems to further enhance drug uptake.

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“…After 45 min, at least 80% of the initial amoxicillin dose was released, which categorizes the formulation as an immediate release formulation according to the European Pharmacopoeia [46]. Comparable pH-dependent release profiles have previously been observed for drugs loaded in microcontainers and coated with Eudragit ® L100 [16,47]. For all three formulations, the loaded amount of amoxicillin was released after 60 min (98 ± 1%, 98 ± 3% and 94 ± 3% for the cylindrical, cubic and triangular microcontainers, respectively).…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats

Christfort

Guillot²,

Melero³

et al. 2020

Pharmaceutics

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An increased interest in colonic drug delivery has led to a higher focus on the design of delivery devices targeting this part of the gastrointestinal tract. Microcontainers have previously facilitated an increase in oral bioavailability of drugs. The surface texture and shape of microcontainers have proven to influence the mucoadhesion ex vivo. In the present work, these findings were further investigated using an in situ closed-loop perfusion technique in the rat colon, which allowed for simultaneous evaluation of mucoadhesion of the microcontainers as well as drug absorption. Cylindrical, triangular and cubic microcontainers, with the same exterior surface area, were evaluated based on in vitro release, in situ mucoadhesion and in situ absorption of amoxicillin. Additionally, the mucoadhesion of empty cylindrical microcontainers with and without pillars on the top surface was investigated. From the microscopy analysis of the colon sections after the in situ study, it was evident that a significantly higher percentage of cubic microcontainers than cylindrical microcontainers adhered to the intestinal mucus. Furthermore, the absorption rate constants and blood samples indicated that amoxicillin in cubic microcontainers was absorbed more readily than when cylindrical or triangular microcontainers were dosed. This could be due to a higher degree of mucoadhesion for these particular microcontainers.

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pH-triggered drug release from biodegradable microwells for oral drug delivery

Cited by 30 publications

References 31 publications

Microfabricated devices for oral drug delivery

Microfabricated devices for oral drug delivery

Micro/nanofabricated platforms for oral drug delivery

Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats

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