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AuthorAbouzid, Afaf
AuthorMoustafa, Abdelrhman Y.
AuthorAllcock, Natalie
AuthorNajlah, Mohammad
AuthorElhissi, Abdelbary
AuthorStanley, Chi Wi
AuthorAhmed, Waqar
AuthorSeville, Peter
AuthorCrean, StJohn
AuthorForbes, Robert T.
AuthorElsawy, Mohamed A.
Available date2023-02-28T10:10:25Z
Publication Date2023
Publication NameJournal of Drug Delivery Science and Technology
ResourceScopus
URIhttp://dx.doi.org/10.1016/j.jddst.2022.104052
URIhttp://hdl.handle.net/10576/40528
AbstractOral aphthous stomatitis is a common disorder treated with the immunomodulatory drug Amlexanox (AMX), that was administered as a mucoadhesive paste (Aphthasol®). This product was discontinued by FDA in 2014 due to the associated undesired adverse reactions of the formulation. Here, we have developed AMX-loaded nanoliposome formulation as a potential alternative for the localised oromucosal delivery of AMX. Nanoliposomes were prepared using Soya phosphatidylcholine (SPC) and Cholesterol (Chol) mixtures at three different molar ratios to formulate vesicles using thin-film hydration, and were characterised for size, zeta potential and entrapment efficiency. The optimal formulation was found to be SPC:Chol 3:1 with drug entrapment efficiency of 94%, post sonication. To evaluate anti-inflammatory activity, macrophages developed by differentiation of human leukaemia monocytic cell line, THP-1, were polarised by Interferon gamma (IFNγ) and lipopolysaccharide (LPS) to M1 state. Macrophages M1 cells treated with D-L1 formulation (SPC:Chol 3:1, 500 μg/mL total lipid, and 27.6 μM AMX) showed a significant suppression in TNF-α expression levels (43 ± 2.7% of untreated control, p < 0.05) compared to those treated with either empty liposomes or AMX alone. Notably, %TNF-α dramatically decreased to 57 ± 4.05% of control, for cells treated with drug-free liposomes (500 μg/mL total lipid) indicating the anti-inflammatory activity of SPC lipid component per se, which led to synergistic effect as evident from the augmentation of AMX anti-inflammatory activity in D-L1 formulation. Our findings highlight the potential of using AMX nanoliposomes as a promising advanced formulation for reviving AMX treatment for management of inflammatory conditions of oral mucosa.
SponsorThis research was funded by the Egyptian Government missions sector PhD scholarship awarded to A.Y.M. and was supported by the self-funded PhD project for A.A.Authors would like to thank the University of Leicester Core Biotechnology Services Electron Microscopy Facility, for the use of their Transmission Electron Microscope. Authors would also like to thank Dr Abdullah Isreb, Dr Sim Singhrao and Dr Sarah Dennison from University of Central Lancashire (UCLan), as well as Abdulwahhab Khedr and Mohamed Soliman from De Montfort University for their support and scientific discussions. Authors are grateful to Dr Julie Burrows and Dr Antony Ashton from UCLan for training A.A. on the basics of in vitro cell culture techniques and bioassays used in this work. Authors would like to thank Dr Gail Welsby for providing A.A. training for the use of the fluorescence microscope. Thanks to the technical staff in JB Firth analytical suite at UCLan for their assistance and training of A.A. on some of the analytical techniques used in this work. Authors are grateful to Dr Philip Welsby for providing the aspirin used in this project as in-kind contribution.
Languageen
PublisherElsevier
SubjectAmlexanox
Anti-inflammatory
Aphthous stomatitis
Liposomes
Macrophages
Oral ulcers
TitleAmlexanox-loaded nanoliposomes showing enhanced anti-inflammatory activity in cultured macrophages: A potential formulation for treatment of oral aphthous stomatitis
TypeArticle
Volume Number79
dc.accessType Open Access


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