Preparation, characterization and in-vitro efficacy of quercetin loaded liquid crystalline nanoparticles for the treatment of asthma

David Ong Cherk Yong, Sanggetha Raja Saker, Ridhima Wadhwa, Dinesh Kumar Chellappan, Thiagarajan Madheswaran, Jithendra Panneerselvam, Murtaza M. Tambuwala, Hamid A. Bakshi, Pradeep Kumar, Viness Pillay, Gaurav Gupta, Brian G. Oliver, Peter Wark, Alan Hsu, Philip Michael Hansbro, Kamal Dua, Farrukh Zeeshan

    Research output: Contribution to journalArticle

    Abstract

    The present study aims to formulate quercetin loaded liquid crystalline nanoparticles (LCN) and surface modified liquid crystalline nanoparticles (sm-LCN) as well as investigate their anti-inflammatory activity in human primary bronchial epithelial cell line (BCi-NS1.1) induced with lipopolysaccharide (LPS). Quercetin LCN were prepared using ultrasonication method. The formulated LCNs and sm-LCNs were characterised in terms of particle size, zeta potential as well as the drug encapsulation efficiency. Furthermore, their morphology and in vitro release profile were also studied. In addition, the anti-inflammatory activity of quercetin LCN and sm-LCNs were evaluated by measuring the concentration of pro-inflammatory markers namely interleukin (IL)-1β, IL-6 and IL-8 in BCI-NS1.1 cell lines via cytometric bead array. The molecular mechanism inherent to the inclusion of quercetin into monoolein nanosystem and surface modification of the nanosystem with chitosan was elucidated via molecular mechanics simulations. Quercetin LCN and sm-LCN significantly (p < 0.05) decreased the production of IL-1β, IL-6 and IL-8 compared to LPS only group. Encapsulation of quercetin into LCN and sm-LCN further enhanced its anti-inflammatory activity compared to quercetin in dimethyl sulfoxide (DMSO). In addition to that, quercetin LCN and sm-LCN also exhibited comparable activity to fluticasone in terms of significantly (p < 0.05) reducing the production of IL-1β and IL-6. Quercetin loaded LCN and sm-LCN could be a potential therapeutic intervention for asthma as they are efficacious in suppressing the production of key pro-inflammatory cytokines associated with the development of asthma.

    LanguageEnglish
    Article number101297
    Number of pages8
    JournalJournal of Drug Delivery Science and Technology
    Volume54
    Early online date3 Oct 2019
    DOIs
    Publication statusPublished - 31 Dec 2019

    Fingerprint

    Quercetin
    Nanoparticles
    Asthma
    Interleukin-1beta
    Interleukin-6
    Anti-Inflammatory Agents
    Interleukin-8
    Lipopolysaccharides
    In Vitro Techniques
    Cell Line
    Chitosan
    Dimethyl Sulfoxide
    Mechanics
    Particle Size
    Human Activities
    Epithelial Cells
    Cytokines

    Keywords

    • Asthma
    • BCi-NS1.1
    • Inflammation
    • Liquid crystalline nanoparticles
    • Quercetin

    Cite this

    Cherk Yong, David Ong ; Saker, Sanggetha Raja ; Wadhwa, Ridhima ; Chellappan, Dinesh Kumar ; Madheswaran, Thiagarajan ; Panneerselvam, Jithendra ; Tambuwala, Murtaza M. ; Bakshi, Hamid A. ; Kumar, Pradeep ; Pillay, Viness ; Gupta, Gaurav ; Oliver, Brian G. ; Wark, Peter ; Hsu, Alan ; Hansbro, Philip Michael ; Dua, Kamal ; Zeeshan, Farrukh. / Preparation, characterization and in-vitro efficacy of quercetin loaded liquid crystalline nanoparticles for the treatment of asthma. In: Journal of Drug Delivery Science and Technology. 2019 ; Vol. 54.
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    title = "Preparation, characterization and in-vitro efficacy of quercetin loaded liquid crystalline nanoparticles for the treatment of asthma",
    abstract = "The present study aims to formulate quercetin loaded liquid crystalline nanoparticles (LCN) and surface modified liquid crystalline nanoparticles (sm-LCN) as well as investigate their anti-inflammatory activity in human primary bronchial epithelial cell line (BCi-NS1.1) induced with lipopolysaccharide (LPS). Quercetin LCN were prepared using ultrasonication method. The formulated LCNs and sm-LCNs were characterised in terms of particle size, zeta potential as well as the drug encapsulation efficiency. Furthermore, their morphology and in vitro release profile were also studied. In addition, the anti-inflammatory activity of quercetin LCN and sm-LCNs were evaluated by measuring the concentration of pro-inflammatory markers namely interleukin (IL)-1β, IL-6 and IL-8 in BCI-NS1.1 cell lines via cytometric bead array. The molecular mechanism inherent to the inclusion of quercetin into monoolein nanosystem and surface modification of the nanosystem with chitosan was elucidated via molecular mechanics simulations. Quercetin LCN and sm-LCN significantly (p < 0.05) decreased the production of IL-1β, IL-6 and IL-8 compared to LPS only group. Encapsulation of quercetin into LCN and sm-LCN further enhanced its anti-inflammatory activity compared to quercetin in dimethyl sulfoxide (DMSO). In addition to that, quercetin LCN and sm-LCN also exhibited comparable activity to fluticasone in terms of significantly (p < 0.05) reducing the production of IL-1β and IL-6. Quercetin loaded LCN and sm-LCN could be a potential therapeutic intervention for asthma as they are efficacious in suppressing the production of key pro-inflammatory cytokines associated with the development of asthma.",
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    author = "{Cherk Yong}, {David Ong} and Saker, {Sanggetha Raja} and Ridhima Wadhwa and Chellappan, {Dinesh Kumar} and Thiagarajan Madheswaran and Jithendra Panneerselvam and Tambuwala, {Murtaza M.} and Bakshi, {Hamid A.} and Pradeep Kumar and Viness Pillay and Gaurav Gupta and Oliver, {Brian G.} and Peter Wark and Alan Hsu and Hansbro, {Philip Michael} and Kamal Dua and Farrukh Zeeshan",
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    Cherk Yong, DO, Saker, SR, Wadhwa, R, Chellappan, DK, Madheswaran, T, Panneerselvam, J, Tambuwala, MM, Bakshi, HA, Kumar, P, Pillay, V, Gupta, G, Oliver, BG, Wark, P, Hsu, A, Hansbro, PM, Dua, K & Zeeshan, F 2019, 'Preparation, characterization and in-vitro efficacy of quercetin loaded liquid crystalline nanoparticles for the treatment of asthma', Journal of Drug Delivery Science and Technology, vol. 54, 101297. https://doi.org/10.1016/j.jddst.2019.101297

    Preparation, characterization and in-vitro efficacy of quercetin loaded liquid crystalline nanoparticles for the treatment of asthma. / Cherk Yong, David Ong; Saker, Sanggetha Raja; Wadhwa, Ridhima; Chellappan, Dinesh Kumar; Madheswaran, Thiagarajan; Panneerselvam, Jithendra; Tambuwala, Murtaza M.; Bakshi, Hamid A.; Kumar, Pradeep; Pillay, Viness; Gupta, Gaurav; Oliver, Brian G.; Wark, Peter; Hsu, Alan; Hansbro, Philip Michael; Dua, Kamal; Zeeshan, Farrukh.

    In: Journal of Drug Delivery Science and Technology, Vol. 54, 101297, 31.12.2019.

    Research output: Contribution to journalArticle

    TY - JOUR

    T1 - Preparation, characterization and in-vitro efficacy of quercetin loaded liquid crystalline nanoparticles for the treatment of asthma

    AU - Cherk Yong, David Ong

    AU - Saker, Sanggetha Raja

    AU - Wadhwa, Ridhima

    AU - Chellappan, Dinesh Kumar

    AU - Madheswaran, Thiagarajan

    AU - Panneerselvam, Jithendra

    AU - Tambuwala, Murtaza M.

    AU - Bakshi, Hamid A.

    AU - Kumar, Pradeep

    AU - Pillay, Viness

    AU - Gupta, Gaurav

    AU - Oliver, Brian G.

    AU - Wark, Peter

    AU - Hsu, Alan

    AU - Hansbro, Philip Michael

    AU - Dua, Kamal

    AU - Zeeshan, Farrukh

    PY - 2019/12/31

    Y1 - 2019/12/31

    N2 - The present study aims to formulate quercetin loaded liquid crystalline nanoparticles (LCN) and surface modified liquid crystalline nanoparticles (sm-LCN) as well as investigate their anti-inflammatory activity in human primary bronchial epithelial cell line (BCi-NS1.1) induced with lipopolysaccharide (LPS). Quercetin LCN were prepared using ultrasonication method. The formulated LCNs and sm-LCNs were characterised in terms of particle size, zeta potential as well as the drug encapsulation efficiency. Furthermore, their morphology and in vitro release profile were also studied. In addition, the anti-inflammatory activity of quercetin LCN and sm-LCNs were evaluated by measuring the concentration of pro-inflammatory markers namely interleukin (IL)-1β, IL-6 and IL-8 in BCI-NS1.1 cell lines via cytometric bead array. The molecular mechanism inherent to the inclusion of quercetin into monoolein nanosystem and surface modification of the nanosystem with chitosan was elucidated via molecular mechanics simulations. Quercetin LCN and sm-LCN significantly (p < 0.05) decreased the production of IL-1β, IL-6 and IL-8 compared to LPS only group. Encapsulation of quercetin into LCN and sm-LCN further enhanced its anti-inflammatory activity compared to quercetin in dimethyl sulfoxide (DMSO). In addition to that, quercetin LCN and sm-LCN also exhibited comparable activity to fluticasone in terms of significantly (p < 0.05) reducing the production of IL-1β and IL-6. Quercetin loaded LCN and sm-LCN could be a potential therapeutic intervention for asthma as they are efficacious in suppressing the production of key pro-inflammatory cytokines associated with the development of asthma.

    AB - The present study aims to formulate quercetin loaded liquid crystalline nanoparticles (LCN) and surface modified liquid crystalline nanoparticles (sm-LCN) as well as investigate their anti-inflammatory activity in human primary bronchial epithelial cell line (BCi-NS1.1) induced with lipopolysaccharide (LPS). Quercetin LCN were prepared using ultrasonication method. The formulated LCNs and sm-LCNs were characterised in terms of particle size, zeta potential as well as the drug encapsulation efficiency. Furthermore, their morphology and in vitro release profile were also studied. In addition, the anti-inflammatory activity of quercetin LCN and sm-LCNs were evaluated by measuring the concentration of pro-inflammatory markers namely interleukin (IL)-1β, IL-6 and IL-8 in BCI-NS1.1 cell lines via cytometric bead array. The molecular mechanism inherent to the inclusion of quercetin into monoolein nanosystem and surface modification of the nanosystem with chitosan was elucidated via molecular mechanics simulations. Quercetin LCN and sm-LCN significantly (p < 0.05) decreased the production of IL-1β, IL-6 and IL-8 compared to LPS only group. Encapsulation of quercetin into LCN and sm-LCN further enhanced its anti-inflammatory activity compared to quercetin in dimethyl sulfoxide (DMSO). In addition to that, quercetin LCN and sm-LCN also exhibited comparable activity to fluticasone in terms of significantly (p < 0.05) reducing the production of IL-1β and IL-6. Quercetin loaded LCN and sm-LCN could be a potential therapeutic intervention for asthma as they are efficacious in suppressing the production of key pro-inflammatory cytokines associated with the development of asthma.

    KW - Asthma

    KW - BCi-NS1.1

    KW - Inflammation

    KW - Liquid crystalline nanoparticles

    KW - Quercetin

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