Ex Vivo  Correlation of the Permeability of Metoprolol Across Human and Porcine Buccal Mucosa

Meng-Lund, Emil; Marxen, Eva; Pedersen, Anne Marie Lynge; Müllertz, Anette; Hyrup, Birgitte; Holm, René; Jacobsen, Jette Bredahl

doi:10.1002/jps.24010

Cited by 20 publications

(10 citation statements)

References 26 publications

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“…Permeability across excised mucosal tissue can be studied in side-by-side diffusion cells such as modified Ussing chambers or Franz cells [7]. To the authors' knowledge it has not been confirmed that the mucus layer on the epithelium is intact after handling the excised tissue [8]. Filter grown cell cultures, such as TR146 cells derived from human buccal carcinoma have also been used to model oral mucosa [9,10].…”

Section: Introductionmentioning

confidence: 99%

Mucin dispersions as a model for the oromucosal mucus layer in in vitro and ex vivo buccal permeability studies of small molecules

Marxen

Mosgaard

Pedersen

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

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Section: Introductionmentioning

confidence: 99%

Mucin dispersions as a model for the oromucosal mucus layer in in vitro and ex vivo buccal permeability studies of small molecules

Marxen

Mosgaard

Pedersen

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

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“…The dog buccal mucosa is similar to human morphology and immunohistology; it shows high drug permeability with moderate correlation with the human study [62,63]. The most common tissue type is porcine, which shows a high correlation; meanwhile, the cost is low and easy to obtain [64]. The thickness is large, so the permeability is low [65].…”

Section: Ex Vivomentioning

confidence: 83%

Recent Options and Techniques to Assess Improved Bioavailability: In Vitro and Ex Vivo Methods

et al. 2023

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Bioavailability assessment in the development phase of a drug product is vital to reveal the disadvantageous properties of the substance and the possible technological interventions. However, in vivo pharmacokinetic studies provide strong evidence for drug approval applications. Human and animal studies must be designed on the basis of preliminary biorelevant experiments in vitro and ex vivo. In this article, the authors have reviewed the recent methods and techniques from the last decade that are in use for assessing the bioavailability of drug molecules and the effects of technological modifications and drug delivery systems. Four main administration routes were selected: oral, transdermal, ocular, and nasal or inhalation. Three levels of methodologies were screened for each category: in vitro techniques with artificial membranes; cell culture, including monocultures and co-cultures; and finally, experiments where tissue or organ samples were used. Reproducibility, predictability, and level of acceptance by the regulatory organizations are summarized for the readers.

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“…However, previous studies have confirmed ex vivo buccal porcine tissue is the closest model to human tissue and serves as an excellent model to assess feasibility of buccal drug delivery. 12 , 15 That said, the degree of keratinisation, cell wall thickness and intercellular spacing may well be different in the neonatal epithelium as compared to the young child or adult, which may explain some of the anecdotal reports of efficacy in the use of buccal MS in infants and young children.…”

Section: Discussionmentioning

confidence: 99%

“… 12 – 14 The pig is the closest model to humans with respect to buccal or sublingual permeation properties. 12 , 15 The knowledge of a drug’s buccal permeation properties, along with reported pharmacokinetic data, allows for calculation of plasma values following buccal administration in vivo. 12 …”

Section: Designmentioning

confidence: 99%

“…[12][13][14] The pig is the closest model to humans with respect to buccal or sublingual permeation properties. 12,15 The knowledge of a drug's buccal permeation properties, along with reported pharmacokinetic data, allows for calculation of plasma values following buccal administration in vivo. 12 Effective oral transmucosal delivery is usually associated with those molecules which are also administered via the transdermal route because of the inherent physicochemical properties of drugs required for absorption via both routes.…”

Section: Designmentioning

confidence: 99%

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Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study

McCulloch

Sattar

Henderson³

et al. 2017

Palliat Med

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Background:Children and infants with impaired swallow or compromised enteral absorption require alternative routes for administration of analgesia. Recent clinical guidance and practice for paediatric palliative care teams, who often treat such children, supports buccal morphine sulphate as a fast acting, effective and easily administered agent for pain relief. However, a consideration of the physicochemical properties and potency of morphine would suggest that it is not a suitable candidate for delivery via the transmucosal route, raising questions about its use in children and infants.Aim:To explore the permeability of buccal morphine sulphate in an established ex vivo porcine buccal mucosa as a necessary step in examining efficacy for use in children with life-limiting conditions and life-threatening illnesses.Design:A permeation study conducted with morphine sulphate in an ex vivo porcine buccal tissue model. Flux values and pharmacokinetic data were used to calculate the plasma values of morphine that would result following buccal administration in a 20kg child.Results:Results show that the estimated steady state plasma values of morphine sulphate following buccal administration in this model do not achieve minimum therapeutic concentration.Conclusion:These data strongly suggest that morphine sulphate is not suitable for buccal administration and that further research is needed to establish its efficacy in relief of pain in children with life-limiting conditions and life-threatening illnesses.

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Ex Vivo Correlation of the Permeability of Metoprolol Across Human and Porcine Buccal Mucosa

Cited by 20 publications

References 26 publications

Mucin dispersions as a model for the oromucosal mucus layer in in vitro and ex vivo buccal permeability studies of small molecules

Mucin dispersions as a model for the oromucosal mucus layer in in vitro and ex vivo buccal permeability studies of small molecules

Recent Options and Techniques to Assess Improved Bioavailability: In Vitro and Ex Vivo Methods

Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study

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