Gastro intestinal tracking and gastric emptying of solid dosage forms in rats using X-ray imagining

Saphier, Sigal; Rosner, Amir; Brandeis, Rachel; Karton, Yishai

doi:10.1016/j.ijpharm.2010.01.001

Cited by 48 publications

(48 citation statements)

References 41 publications

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“…5), consistent with previous studies in rats regarding capsule size and gastric retention (24,27). When 19 F-FDG is dissolved, diffused out of the capsule and taken up by cells/in the blood stream, it leads to the loss of a clearly localized 19 F-MRI signal (Fig.…”

Section: In Vivo Imagingsupporting

confidence: 90%

“…5(A)). The feeding status of animals is a known factor that influences the transit of capsules (24). In our study, all animals were in a fed state.…”

Section: In Vivo Imagingmentioning

confidence: 99%

“…In this study, 2-fluoro-2-deoxy-D-glucose ( 19 F-FDG) is used as the contrast agent for 19 F-MRI as it is only MR detectable when dissolved in water and, as a glucose analog, is considered to be safe (22). On the other hand, barium sulfate (BaSO 4 ), based on the high atomic number and hence high X-ray absorption of barium, is used as a CT contrast agent for gastrointestinal tract imaging to increase the contrast between the gastrointestinal contents and the surrounding soft tissues (23,24). Moreover, BaSO 4 can be safely used for oral administration because of the absence of toxicity (25).…”

Section: Introductionmentioning

confidence: 99%

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Visualization of delayed release of compounds from pH‐sensitive capsules in vitro and in vivo in a hamster model

Staelens

Liang

Appeltans

et al. 2015

Contrast Media & Molecular

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Delayed controlled release is an innovative strategy to locally administer therapeutic compounds (e.g. chemotherapeutics, antibodies etc.). This would improve efficiency and reduce side effects compared with systemic administration. To enable the evaluation of the efficacy of controlled release strategies both in vitro and in vivo, we investigated the release of contrast agents (19 F‐FDG and BaSO4) to the intestinal tract from capsules coated with pH‐sensitive polymers (EUDRAGIT L‐100) by using two complementary techniques, i.e. 19 F magnetic resonance imaging (MRI) and computed tomography (CT). Using in vitro 19 F‐MRI, we were able to non‐destructively and dynamically establish a time window of 2 h during which the capsules are resistant to low pH. With 19 F‐MRI, we could establish the exact time point when the capsules became water permeable, before physical degradation of the capsule. This was complemented by CT imaging, which provided longitudinal information on physical degradation of the capsule at low pH that was only seen after 230 min. After oral administration to hamsters, 19 F‐MRI visualized the early event whereby the capsule becomes water permeable after 2 h. Additionally, using CT, the integrity and location (stomach and small intestines) of the capsule after administration could be monitored. In conclusion, we propose combined 19 F‐MRI and CT to non‐invasively visualize the different temporal and spatial events regarding the release of compounds, both in an in vitro setting and in the gastrointestinal tract of small animal models. This multimodal imaging approach will enable the in vitro and in vivo evaluation of further technical improvements to controlled release strategies. Copyright © 2015 John Wiley & Sons, Ltd.

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Section: In Vivo Imagingsupporting

confidence: 90%

“…5(A)). The feeding status of animals is a known factor that influences the transit of capsules (24). In our study, all animals were in a fed state.…”

Section: In Vivo Imagingmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Visualization of delayed release of compounds from pH‐sensitive capsules in vitro and in vivo in a hamster model

Staelens

Liang

Appeltans

et al. 2015

Contrast Media & Molecular

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“…The latter was simple, cheap and offers simultaneous visualization of both capsule and the GI tract using contrast agents [35]. The passage of coated minispheres through the GI tract confirmed minisphere dissolution at the intended sites.…”

Section: Discussionmentioning

confidence: 88%

“…Techniques described on the literature for tracking of solid oral dosage forms in rodents include gamma scintigraphy [31], magnetic resonance imaging (MRI) [32], positron emission tomography (PET) [33], micro-computerized tomography (μCT) [34] and Xray [35]. The latter was simple, cheap and offers simultaneous visualization of both capsule and the GI tract using contrast agents [35].…”

Section: Discussionmentioning

confidence: 99%

Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

Aguirre

Aversa

Rosa

et al. 2016

Journal of Controlled Release

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Achieving oral peptide delivery is an elusive challenge. Emulsion-based minispheres of salmon calcitonin (sCT) were synthesized using single multiple pill (SmPill ® ) technology incorporating the permeation enhancers (PEs): sodium taurodeoxycholate (NaTDC), sodium caprate (C 10 ), or coco-glucoside (CG), or the pH acidifier, citric acid (CA). Minispheres were coated with an outer layer of Eudragit ® L30 D-55 (designed for jejunal release) or Surelease ® /Pectin (designed for colonic release). The process was mild and in vitro biological activity of sCT was retained upon release from minispheres stored up to 4 months. In vitro release profiles suggested that sCT was released from minispheres by diffusion through coatings due to swelling of gelatin and the polymeric matrix upon contact with PBS at pH 6.8.X-ray analysis confirmed that coated minispheres dissolved at the intended intestinal region of rats following oral gavage. Uncoated minispheres at a dose of ~2000 I.U. sCT/kg were administered to rats by intra-jejunal (i.j.) or intra-colonic (i.c.) instillation and caused hypocalcaemia. Notable sCT absolute bioavailability (F) values were: 5.5% from minispheres containing NaTDC (i.j), 17.3% with CG (i.c.) and 18.2 % with C 10 (i.c.). Coated minispheres administered by oral gavage at threefold higher doses also induced hypocalcaemia. A highly competitive F value of 2.7% was obtained for orally-administered sCT-minispheres containing CG (45 μmol/kg) and coated with Eudragit ® . In conclusion, the SmPill ® technology is a potential dosage form for several peptides when formulated with PEs and coated for regional delivery. PK data from instillations over-estimates oral bioavailability and poorly predicts rank ordering of formulations .

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3D‐Printed Radiopaque Microdevices with Enhanced Mucoadhesive Geometry for Oral Drug Delivery

Chang

Kjeldsen

Christfort

et al. 2022

Adv Healthcare Materials

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During the past decades, microdevices have been evaluated as a means to overcome challenges within oral drug delivery, thus improving bioavailability. Fabrication of microdevices is often limited to planar or simple 3D designs. Therefore, this work explores how microscale stereolithography 3D printing can be used to fabricate radiopaque microcontainers with enhanced mucoadhesive geometries, which can enhance bioavailability by increasing gastrointestinal retention. Ex vivo force measurements suggest increased mucoadhesion of microcontainers with adhering features, such as pillars and arrows, compared to a neutral design. In vivo studies, utilizing planar X-ray imaging, show the time-dependent gastrointestinal location of microcontainers, whereas computed tomography scanning and cryogenic scanning electron microscopy reveal information about their spatial dynamics and mucosal interactions, respectively. For the first time, the effect of 3D microdevice modifications on gastrointestinal retention is traced in vivo, and the applied methods provide a much-needed approach for investigating the impact of device design on gastrointestinal retention.

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Gastro intestinal tracking and gastric emptying of solid dosage forms in rats using X-ray imagining

Cited by 48 publications

References 41 publications

Visualization of delayed release of compounds from pH‐sensitive capsules in vitro and in vivo in a hamster model

Visualization of delayed release of compounds from pH‐sensitive capsules in vitro and in vivo in a hamster model

Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

3D‐Printed Radiopaque Microdevices with Enhanced Mucoadhesive Geometry for Oral Drug Delivery

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