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Exploration of a double emulsion formulation strategy to increase alendronic acid permeability

Abd Jalil, Muhammad Fauzi; (2021) Exploration of a double emulsion formulation strategy to increase alendronic acid permeability. Doctoral thesis (Ph.D), UCL (University College London). Green open access

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Abstract

Alendronic acid (ALD) is a drug used to treat osteoporosis and has low oral bioavailability of 0.7 %. Furthermore, ALD has a complicated dosing regimen and can cause oesophageal irritation. ALD is ionised in water causing it to be less permeable in the gastrointestinal tract. To improve the permeability and absorption of ALD in the gastrointestinal tract, encapsulation of ALD within a double emulsion formulation was examined. Double emulsions were fabricated using a single-step homogenisation process using ALD, soybean oil and two surfactants, Span 80 and Tween 80. Fabricated double emulsions were characterised for ALD encapsulation and imaged using a light microscope so that emulsion morphology and size could be analysed. Double emulsions with greater than 90% ALD encapsulation were selected for in vitro permeation studies with Caco-2 and HDLEC cells to assess the potential permeability of ALD in intestinal lymphatic cells. ALD permeation improved by approximately 40% when double emulsion was used on Caco-2 cells pre-treated with oleic acid and taurocholic acid (OCTC), compared to non-pre-treated cells. Similarly, when the double emulsions were evaluated using HDLEC cells, the permeation of ALD was approximately 65% to 73%, with formulation B18 displaying the highest permeation. Interestingly, both studies revealed the integrity of the tight junction was not affected by the ALD double emulsion formulation. These studies also suggested improvement of ALD permeation could be from the absorption of double emulsion could be either via transcellular or paracellular pathways. These findings reveal that there may be potential to formulate ALD with improved permeation gastrointestinal tract.

Type: Thesis (Doctoral)
Qualification: Ph.D
Title: Exploration of a double emulsion formulation strategy to increase alendronic acid permeability
Event: UCL (University College London
Open access status: An open access version is available from UCL Discovery
Language: English
Additional information: Copyright © The Author 2021. Original content in this thesis is licensed under the terms of the Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0) Licence (https://creativecommons.org/licenses/by-nc/4.0/). Any third-party copyright material present remains the property of its respective owner(s) and is licensed under its existing terms. Access may initially be restricted at the author’s request.
UCL classification: UCL
UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
URI: https://discovery.ucl.ac.uk/id/eprint/10124503
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