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

doi:10.1016/j.jddst.2019.101297

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

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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.

Original language	English
Article number	101297
Number of pages	8
Journal	Journal of Drug Delivery Science and Technology
Volume	54
Early online date	3 Oct 2019
DOIs	https://doi.org/10.1016/j.jddst.2019.101297
Publication status	Published (in print/issue) - 31 Dec 2019

Funding

The authors would like to thank International Medical University (IMU). Malaysia for providing the financial support for the project. Also, thanks to the Hunter Medical Research Institute (HMRI), The University of Newcastle, NSW 2308, Australia and the Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, NSW 2007, Australia for providing necessary research facilities. Appendix A

Keywords

Asthma
BCi-NS1.1
Inflammation
Liquid crystalline nanoparticles
Quercetin

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.jddst.2019.101297

Accepted author manuscriptAuthor Accepted Manuscript -, 1.29 MB

Cite this

Cherk Yong, D. O., Saker, S. R., Wadhwa, R., Chellappan, D. K., Madheswaran, T., Panneerselvam, J., Tambuwala, M. M., Bakshi, H. A., Kumar, P., Pillay, V., Gupta, G., Oliver, B. G., Wark, P., Hsu, A., Hansbro, P. M., 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, 54, Article 101297. https://doi.org/10.1016/j.jddst.2019.101297

@article{ec928819194544f0b71358951dd03f25,

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.",

keywords = "Asthma, BCi-NS1.1, Inflammation, Liquid crystalline nanoparticles, Quercetin",

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

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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DO - 10.1016/j.jddst.2019.101297

M3 - Article

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JO - Journal of Drug Delivery Science and Technology

JF - Journal of Drug Delivery Science and Technology

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ER -

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

Abstract

Funding

Keywords

UN SDGs

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Molecular analysis of the effects of crocin on acute myeloid leukaemia, pancreatic and colon cancer

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

Abstract

Funding

Keywords

UN SDGs

Access to Document

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Molecular analysis of the effects of crocin on acute myeloid leukaemia, pancreatic and colon cancer

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