Comparative in vivo mucoadhesion studies of thiomer formulations using magnetic resonance imaging and fluorescence detection

Albrecht, Karin; Greindl, Melanie; Kremser, Christian; Wolf, Christian; Debbage, Paul; Bernkop‐Schnürch, Andreas

doi:10.1016/j.jconrel.2006.06.023

Cited by 57 publications

(27 citation statements)

References 22 publications

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“…Several research groups are performing in vivo studies to analyze the mucoadhesive and mucus penetration properties of nanoparticles in different mucus layers [2,26,[73][74][75][76][77][78][79][80]. They focused on the fate of particulate drug delivery systems in mucus especially on their uptake into the epithelium of the GI-tract after oral administration [43].…”

Section: In Vivo Methodsmentioning

confidence: 99%

Methods to determine the interactions of micro- and nanoparticles with mucus

Grießinger¹,

Dünnhaupt²,

Cattoz

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

100

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Section: In Vivo Methodsmentioning

confidence: 99%

Methods to determine the interactions of micro- and nanoparticles with mucus

Grießinger¹,

Dünnhaupt²,

Cattoz

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

100

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Section: Discussionmentioning

confidence: 99%

“…Enteric-coated gelatin capsules of approximately 2.5 mm diameter were emptied from rat stomach between 2 and 8 h, but there was also high variability [36]. With the help of the pro-kinetic, metoclopramide, those capsules exited rat stomach earlier and more consistently [36]. Others demonstrated that 14 days of a fixed feeding regimen to rats led to an accelerated solid gastric emptying due to presence of inter-digestive gastric contractions, and also due to an increase in their maximal amplitude [37].…”

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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“…Measurement of the residence time of fluorescent polymers contained in the dosage form at the site of application [90].…”

Section: Magnetic Resonance Imaging Techniquementioning

confidence: 99%

“…The mucoadhesive properties of thiolated polymers are linked to their capability to form covalent bonds (disulfide bridges) with cysteine-rich sub-domains of the glycoproteins of the mucus gel layer through thiol/disulfide exchange reactions or through a simple oxidation of free thiol groups in order to achieved an increased residence time and improved bioavailability [49,52,90]. With this behaviour, they mimic the natural mechanism of mucus glycoproteins which are linked to the mucus network through disulphide covalent bonds.…”

mentioning

confidence: 99%

Mucoadhesive Polymers for Oral Transmucosal Drug Delivery: A Review

Bagán¹,

Paderni²,

Termine³

et al. 2012

CPD

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Abstract:The oral mucosa offers an interesting site for the application of dosage forms that release drugs within/throughout the oral mucosa, by assuring a high drug bioavailability for topic and systemic effects. However, the relative permeability of the oral mucosa and the washing effect related to the oral fluids and mechanical stresses must be considered in the formulation of oral dosage forms. Since a sustained drug release can be guaranteed only if dosage forms remain in contact with the oral site of absorption/application for a prolonged time, the development of mucoadhesive dosage forms is mandatory. The mucoadhesion is a complex phenomenon and the mucoadhesive bond consists of two different parts, the mucoadhesive polymers and the mucous substrate. In addition to factors related to the oral mucosa and oral environment features, the physical-chemical characteristics of mucoadhesive polymers must be also considered as factors influencing the mucoadhesive bonds. While it is not possible to modify the mucosal features or it is possible to modify or inhibit only in part certain mucosal processes, the knowledge of polymer properties influencing mucoadhesive bonds allows to modify or to control these properties in developing increasingly effective mucoadhesive systems. The aims of this review are to discuss the several mechanisms and factors behind the phenomenon of mucoadhesion with particular reference to the features of the oral environment, oral mucosa, and polymeric compounds influencing mucoadhesion process. Finally, a brief mention to the main mucoadhesive dosage forms designed for oral transmucosal drug delivery is made.

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Comparative in vivo mucoadhesion studies of thiomer formulations using magnetic resonance imaging and fluorescence detection

Cited by 57 publications

References 22 publications

Methods to determine the interactions of micro- and nanoparticles with mucus

Methods to determine the interactions of micro- and nanoparticles with mucus

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

Mucoadhesive Polymers for Oral Transmucosal Drug Delivery: A Review

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