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Will a water gradient in oral mucosa affect transbuccal drug absorption?
Malmö University, Faculty of Health and Society (HS), Department of Biomedical Science (BMV). Malmö University, Biofilms Research Center for Biointerfaces.
Food Technology, Engineering and Nutrition, Lund University, P.O. Box 124, SE-221 00, Lund, Sweden.
Malmö University, Faculty of Health and Society (HS), Department of Biomedical Science (BMV). Malmö University, Biofilms Research Center for Biointerfaces.
Malmö University, Faculty of Health and Society (HS), Department of Biomedical Science (BMV). Malmö University, Biofilms Research Center for Biointerfaces.
2018 (English)In: Journal of Drug Delivery Science and Technology, ISSN 1773-2247, Vol. 48, p. 338-345Article in journal (Refereed) Published
Abstract [en]

Formulations for buccal drug delivery often comprise polymers to facilitate mucoadhesion based on water sorption. The main objective of the current study was therefore to evaluate the effect of dehydration on drug uptake through oral mucosa. We have used diffusion cells with excised porcine mucosa to study uptake of three alternative drugs (i.e., Metronidazole, Benzydamine and Xylometazoline) together with polyethylene glycol (PEG) as the model polymer for adjusting water activity in the test solutions. Taking drug activity into account, we can conclude that addition of PEG results in a drug flux through mucosa that is about two times lower for Metronidazole and more than 40 times lower for Xylometazoline compared to that from a pure PBS-solution. However, for Benzydamine the uptake through mucosa was more or less the same, which could possibly be due to the high PEG-concentration (65 wt%) affecting the dissociation constant and thus the permeability. These results indicate that an increased water gradient may have the same limiting effect on permeability through oral mucosa as previously seen for skin. Thus, water gradient effects should be a factor to consider when developing buccal adhesive formulations.

Place, publisher, year, edition, pages
Elsevier, 2018. Vol. 48, p. 338-345
Keywords [en]
Buccal drug delivery, Oral mucosa, Permeability, Hydration, Drug transport, Formulation
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:mau:diva-15172DOI: 10.1016/j.jddst.2018.10.004ISI: 000451008000038Local ID: 27250OAI: oai:DiVA.org:mau-15172DiVA, id: diva2:1418693
Available from: 2020-03-30 Created: 2020-03-30 Last updated: 2023-04-15Bibliographically approved
In thesis
1. Topical formulations, design and drug delivery: "A dive into water"
Open this publication in new window or tab >>Topical formulations, design and drug delivery: "A dive into water"
2021 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

Water is a vital component regulating the properties of topical formulations and their interaction with biological barriers, such as skin and mucosa. Changing the watercontent within the frame of the pharmaceutical triangle will have a huge impact on which type of formulation, such as a cream, ointment, gel, or lotion, is formed, as well as the physical properties of the formulation. The composition of a formulation, and the subsequent reformulation after application, will govern the features of the residual film. This will in turn affect the barrier properties of the underlying tissue and consequently the penetration of various substances across skin or mucosa.The primary aim of this thesis has been to provide further understanding on differences between traditional surfactant-based formulations and particle-stabilized, Pickering, formulations and how specific excipients, like alcohols, emollients, and thickeners can affect their physical and/or sensorial properties. The secondary aim has been to gain more knowledge on the role of water in topical formulations and how it affects the properties of the underlaying tissue on application.

By combining a portfolio of physicochemical techniques combined with sensory science, we have been able to identify differences between Pickering and surfactantstabilized formulations. Starch-based Pickering emulsions were perceived as less greasy and sticky than traditional creams, even at high oil content. Moreover, we were able develop a novel type of alcohol-based Pickering emulsion with combined moisturizing and antiseptic properties. We have also been able to link sensory attributes, evaluated by human volunteers, with physicochemical characterizations. Furthermore, the in vitro ForceBoard™ method was developed further and we evaluated its potential to be used as an ex vivo method using excised skin. In addition, we have shown that that the water gradient over a biological barrier has a general relevance with respect to drug absorption and should be considered not only in dermaldrug delivery but also for buccal and nasal drug delivery.

Place, publisher, year, edition, pages
Malmö: Malmö universitet, 2021. p. 72
Series
Malmö University Health and Society Dissertations, ISSN 1653-5383 ; 3
Keywords
water, topical formulations, Pickering emulsion, skin cream, drug delivery, tactile friction, sensory panel, nasal, buccal, mucosa, skin, triglycerides, ethanol, drug transport, cosmetic appeal
National Category
Basic Medicine
Identifiers
urn:nbn:se:mau:diva-44964 (URN)10.24834/isbn.9789178772049 (DOI)9789178772032 (ISBN)9789178772049 (ISBN)
Public defence
2021-09-03, Aulan, Fakulteten för Hälsa och samhälle, Jan Waldenströms g. 25, Malmö, 13:30 (English)
Opponent
Available from: 2021-08-18 Created: 2021-08-18 Last updated: 2023-04-15Bibliographically approved

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Ali, AbdullahEngblom, Johan

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