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Buccal

The Experts below are selected from a list of 321 Experts worldwide ranked by ideXlab platform

H E Junginger – 1st expert on this subject based on the ideXlab platform

  • recent advances in Buccal drug delivery and absorption in vitro and in vivo studies
    Journal of Controlled Release, 1999
    Co-Authors: H E Junginger, Janet A Hoogstraate, Coos J Verhoef

    Abstract:

    Abstract In the first part of this study, the aim was to characterize transport of fluorescein isothiocyanate (FITC)-labelled dextrans of different molecular weights as model compounds for peptides and proteins through Buccal mucosa. The penetration of these dextrans through porcine Buccal mucosa (a nonkeratinized epithelium, comparable to human Buccal mucosa) was investigated by measuring transBuccal fluxes and by analyzing the distribution of the fluorescent probe in the epithelium, using confocal laser scanning microscopy for visualizing permeation pathways. The results revealed that passage of hydrophilic compounds such as the FITC–dextrans through porcine Buccal epithelium is restricted to permeants with a molecular weight lower than 20 kDa. The permeabilities of Buccal mucosa for the 4 and 10 kDa FITC–dextran (of the order of 10 −8 cm/s) were not significantly different from each other or from the much smaller compound FITC. The confocal images of the distribution pattern of FITC–dextrans showed that the paracellular route is the major pathway through Buccal epithelium. In the in vivo part of this study, Buccal delivery of FITC-labelled dextran 4400 (FD4) and the peptide drug buserelin was investigated in vivo, in pigs. The delivery device consisted of an application chamber with a solution of FD4 or buserelin, and was attached to the Buccal mucosa for 4 h using an adhesive patch. A randomized cross-over study including intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as an absorption enhancer was performed in pigs. After Buccal administration, steady-state plasma levels were rapidly achieved. Co-administration of 10 mM GDC increased the absolute bioavailability from 1.8±0.5 to 12.7±2.0% for FD4. From the present studies, it is concluded that Buccal administration is a suitable route for the delivery for macromolecules and hydrophilic compounds such as peptide drugs.

  • in vivo Buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs
    Pharmaceutical Research, 1996
    Co-Authors: Janet A Hoogstraate, Coos J Verhoef, A Pijpers, Leo Van Leengoed, J H M Verheijden, H E Junginger, H E Bodde

    Abstract:

    Purpose. To study the potential of Buccal delivery of the peptide drug in pigs.
    Methods. Intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer were investigated as a randomised cross-over study in six pigs. The Buccal delivery device consisted of an application chamber with a solution of buserelin and was attached to the Buccal mucosa for 4 hours using an adhesive patch.
    Results. Buccal administration of buserelin resulted in rapidly reached steady state plasma levels. The absolute bioavailability of the peptide after Buccal delivery for 4 hours could be increased from 1.0 ± 0.3 to 5.3 ± 1.1% (mean ± S.D.) by co-administration of 10 mM GDC (0.45% w/v)).
    Conclusions. The results of this study demonstrate that Buccal administration with the use of absorption enhancers is a useful approach for the delivery of peptide drugs such as buserelin.

  • Buccal delivery of fluorescein isothiocyanate dextran 4400 and the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs
    Journal of Controlled Release, 1996
    Co-Authors: A J Hoogstraate, A Pijpers, Leo Van Leengoed, J H M Verheijden, H E Junginger, J C Verhoef, H E Bodde

    Abstract:

    Delivery of drugs via the Buccal mucosa is an alternative for the low oral absorption and inconvenient parenteral administration of hydrophilic macromolecular drugs. Due to the low permeability of the Buccal epithelium the use of absorption enhancers is a prerequisite. In this study, Buccal delivery of fluorescein isothiocyanate-labelled dextran 4400 (FD4) and the peptide drug buserelin was investigated in vivo, in pigs. The delivery device consisted of an application chamber with a solution of FD4 or buserelin, and was attached to the Buccal mucosa for 4 h using an adhesive patch. A randomized cross-over study including intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer was performed in pigs. After Buccal administration steady-state plasma levels were rapidly achieved. Co-administration of 10 mM GDC increased the absolute bioavailability from 1.8 ± 0.5% to 12.7 ± 2.0% for FD4, and from 1.0 ± 0.3% to 5.3 ± 1.1% for buserelin. From the present studies it is concluded that Buccal administration is a suitable route of delivery for macromolecules and hydrophilic compounds such as peptide drugs.

H E Bodde – 2nd expert on this subject based on the ideXlab platform

  • in vivo Buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs
    Pharmaceutical Research, 1996
    Co-Authors: Janet A Hoogstraate, Coos J Verhoef, A Pijpers, Leo Van Leengoed, J H M Verheijden, H E Junginger, H E Bodde

    Abstract:

    Purpose. To study the potential of Buccal delivery of the peptide drug in pigs.
    Methods. Intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer were investigated as a randomised cross-over study in six pigs. The Buccal delivery device consisted of an application chamber with a solution of buserelin and was attached to the Buccal mucosa for 4 hours using an adhesive patch.
    Results. Buccal administration of buserelin resulted in rapidly reached steady state plasma levels. The absolute bioavailability of the peptide after Buccal delivery for 4 hours could be increased from 1.0 ± 0.3 to 5.3 ± 1.1% (mean ± S.D.) by co-administration of 10 mM GDC (0.45% w/v)).
    Conclusions. The results of this study demonstrate that Buccal administration with the use of absorption enhancers is a useful approach for the delivery of peptide drugs such as buserelin.

  • Buccal delivery of fluorescein isothiocyanate dextran 4400 and the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs
    Journal of Controlled Release, 1996
    Co-Authors: A J Hoogstraate, A Pijpers, Leo Van Leengoed, J H M Verheijden, H E Junginger, J C Verhoef, H E Bodde

    Abstract:

    Delivery of drugs via the Buccal mucosa is an alternative for the low oral absorption and inconvenient parenteral administration of hydrophilic macromolecular drugs. Due to the low permeability of the Buccal epithelium the use of absorption enhancers is a prerequisite. In this study, Buccal delivery of fluorescein isothiocyanate-labelled dextran 4400 (FD4) and the peptide drug buserelin was investigated in vivo, in pigs. The delivery device consisted of an application chamber with a solution of FD4 or buserelin, and was attached to the Buccal mucosa for 4 h using an adhesive patch. A randomized cross-over study including intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer was performed in pigs. After Buccal administration steady-state plasma levels were rapidly achieved. Co-administration of 10 mM GDC increased the absolute bioavailability from 1.8 ± 0.5% to 12.7 ± 2.0% for FD4, and from 1.0 ± 0.3% to 5.3 ± 1.1% for buserelin. From the present studies it is concluded that Buccal administration is a suitable route of delivery for macromolecules and hydrophilic compounds such as peptide drugs.

  • in vivo Buccal delivery of fluorescein isothiocyanate dextran 4400 with glycodeoxycholate as an absorption enhancer in pigs
    Journal of Pharmaceutical Sciences, 1996
    Co-Authors: A J Hoogstraate, A Pijpers, Leo Van Leengoed, J H M Verheijden, H E Junginger, J C Verhoef, H E Bodde

    Abstract:

    Buccal delivery of fluorescein isothiocyanate labeled dextran 4400 (FD4) was investigated in-vivo in pigs. The delivery device consisted of an application chamber with a solution of FD4 and was adhered to the Buccal mucosa for 4 h using an adhesive patch. A randomized crossover study including intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer was performed in five pigs. After Buccal administration, steady state plasma levels were rapidly reached. Coadministration of 10 mM GDC increased the absolute bioavailability of FD4 from 1.8 ± 0.5% to 12.7 ± 2.0%. Since FD4 is a macromolecular and hydrophilic compound such as peptide and protein drugs, Buccal delivery would provide an adequate alternative to the parenteral administration of these drugs.

Coos J Verhoef – 3rd expert on this subject based on the ideXlab platform

  • recent advances in Buccal drug delivery and absorption in vitro and in vivo studies
    Journal of Controlled Release, 1999
    Co-Authors: H E Junginger, Janet A Hoogstraate, Coos J Verhoef

    Abstract:

    Abstract In the first part of this study, the aim was to characterize transport of fluorescein isothiocyanate (FITC)-labelled dextrans of different molecular weights as model compounds for peptides and proteins through Buccal mucosa. The penetration of these dextrans through porcine Buccal mucosa (a nonkeratinized epithelium, comparable to human Buccal mucosa) was investigated by measuring transBuccal fluxes and by analyzing the distribution of the fluorescent probe in the epithelium, using confocal laser scanning microscopy for visualizing permeation pathways. The results revealed that passage of hydrophilic compounds such as the FITC–dextrans through porcine Buccal epithelium is restricted to permeants with a molecular weight lower than 20 kDa. The permeabilities of Buccal mucosa for the 4 and 10 kDa FITC–dextran (of the order of 10 −8 cm/s) were not significantly different from each other or from the much smaller compound FITC. The confocal images of the distribution pattern of FITC–dextrans showed that the paracellular route is the major pathway through Buccal epithelium. In the in vivo part of this study, Buccal delivery of FITC-labelled dextran 4400 (FD4) and the peptide drug buserelin was investigated in vivo, in pigs. The delivery device consisted of an application chamber with a solution of FD4 or buserelin, and was attached to the Buccal mucosa for 4 h using an adhesive patch. A randomized cross-over study including intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as an absorption enhancer was performed in pigs. After Buccal administration, steady-state plasma levels were rapidly achieved. Co-administration of 10 mM GDC increased the absolute bioavailability from 1.8±0.5 to 12.7±2.0% for FD4. From the present studies, it is concluded that Buccal administration is a suitable route for the delivery for macromolecules and hydrophilic compounds such as peptide drugs.

  • in vivo Buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs
    Pharmaceutical Research, 1996
    Co-Authors: Janet A Hoogstraate, Coos J Verhoef, A Pijpers, Leo Van Leengoed, J H M Verheijden, H E Junginger, H E Bodde

    Abstract:

    Purpose. To study the potential of Buccal delivery of the peptide drug in pigs.
    Methods. Intravenous administration and Buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer were investigated as a randomised cross-over study in six pigs. The Buccal delivery device consisted of an application chamber with a solution of buserelin and was attached to the Buccal mucosa for 4 hours using an adhesive patch.
    Results. Buccal administration of buserelin resulted in rapidly reached steady state plasma levels. The absolute bioavailability of the peptide after Buccal delivery for 4 hours could be increased from 1.0 ± 0.3 to 5.3 ± 1.1% (mean ± S.D.) by co-administration of 10 mM GDC (0.45% w/v)).
    Conclusions. The results of this study demonstrate that Buccal administration with the use of absorption enhancers is a useful approach for the delivery of peptide drugs such as buserelin.

  • diffusion rates and transport pathways of fluorescein isothiocyanate fitc labeled model compounds through Buccal epithelium
    Pharmaceutical Research, 1994
    Co-Authors: Janet A Hoogstraate, Coos J Verhoef, H E Junginger, Christopher Cullander, Fred J Nagelkerke, S Senel, H E Bodde

    Abstract:

    The aim of this study was to characterize transport of FITC-labeled dextrans of different molecular weights as model compounds for peptides and proteins through Buccal mucosa. The penetration of these dextrans through porcine Buccal mucosa (a nonkeratinized epithelium, comparable to human Buccal mucosa) was investigated by measuring transBuccal fluxes and by analyzing the distribution of the fluorescent probe in the epithelium, using confocal laser scanning microscopy for visualizing permeation pathways. The results revealed that passage of porcine Buccal epithelium by hydrophilic compounds such as the FITC-dextrans is restricted to permeants with a molecular weight lower than 20 kDa. The permeabilities of Buccal mucosa for the 4- and 10-kDa FITC-dextran (of the order of 10−8 cm/sec) were not significantly different from each other or from the much smaller compound FITC. The confocal images of the distribution pattern of FITC-dextrans showed that the paracellular route is the major pathway through Buccal epithelium.