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Dehydration affects drug transport over nasal mucosa
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, Lund, Sweden.
Bioglan AB, Malmö, Sweden.
Malmö University, Faculty of Health and Society (HS), Department of Biomedical Science (BMV). Malmö University, Biofilms Research Center for Biointerfaces.
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2019 (English)In: Drug Delivery, ISSN 1071-7544, E-ISSN 1521-0464, Vol. 26, no 1, p. 831-840Article in journal (Refereed) Published
Abstract [en]

Formulations for nasal drug delivery often rely on water sorption to adhere to the mucosa, which also causes a higher water gradient over the tissue and subsequent dehydration. The primary aim of this study was therefore to evaluate mucosal response to dehydration and resolve the hypothesis that mucoadhesion achieved through water sorption could also be a constraint for drug absorption via the nasal route. The effect of altering water activity of the vehicle on Xylometazoline HCl and Cr-EDTA uptake was studied separately using flow through diffusion cells and excised porcine mucosa. We have shown that a modest increase in the water gradient over mucosa induces a substantial decrease in drug uptake for both Xylometazoline HCl and Cr-EDTA. A similar result was obtained when comparing two different vehicles on the market; Nasoferm (Nordic Drugs, Sweden) and BLOX4 (Bioglan, Sweden). Mucoadhesion based on water sorption can slow down drug uptake in the nasal cavity. However, a clinical study is required to determine whether prolonged duration of the vehicle or preventing dehydration of the mucosa is the most important factor for improving bioavailability.

Place, publisher, year, edition, pages
Taylor & Francis, 2019. Vol. 26, no 1, p. 831-840
Keywords [en]
Mucoadhesion, dehydration, drug transport, nasal drug delivery, water activity
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:mau:diva-15215DOI: 10.1080/10717544.2019.1650848ISI: 000480247200001PubMedID: 31401887Scopus ID: 2-s2.0-85071047269Local ID: 29688OAI: oai:DiVA.org:mau-15215DiVA, id: diva2:1418736
Available from: 2020-03-30 Created: 2020-03-30 Last updated: 2024-02-05Bibliographically 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, AbdullahFalkman, PeterEngblom, Johan

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