Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies

Kyriaki Hatziagapiou; Maria Braoudaki; Kostas Bethanis; Konstantina Yannakopoulou; Athanasios Anastasiou; Georgia Koutsouri; Dimitrios Koutsouris; George I. Lambrou

doi:10.1109/BHI.2018.8333402

Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies

Kyriaki Hatziagapiou, Maria Braoudaki, Kostas Bethanis, Konstantina Yannakopoulou, Athanasios Anastasiou, Georgia Koutsouri, Dimitrios Koutsouris, George I. Lambrou

Research output: Chapter in Book/Report/Conference proceeding › Conference contribution

Abstract

Cyclodextrins (CD) have been playing a very important role in the formulation of poorly water-soluble drugs by improving apparent drug solubility and/or dissolution. In the current study we focused on the investigation of the cytotoxic effect of cyclodextrin/Gefitinib in inclusion with three types of cyclodextrin, as well as in its inhibitory activity of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity using biological assays. The activity of Gefitinib and Gefitinib/cyclodextrin were measured in pediatric neuroblastoma (NB) tumor cell lines. We have shown that CD/Gefitinib complexes are effective against neuroblastoma cells in vitro. Our studies provided a detailed picture of inclusion of Gefitinib in cyclodextrins and verify improved efficacy of the CD-encapsulated drug in cytotoxicity assays on pediatric tumor cell lines. An understanding of the structural details of guest inclusion in CDs may be useful in the engineering of modified guest-host preparations with optimized pharmacological properties and shape future therapeutic strategies.

Original language	English
Title of host publication	2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018
Publisher	Institute of Electrical and Electronics Engineers (IEEE)
Pages	194-197
Number of pages	4
Volume	2018-January
ISBN (Electronic)	9781538624050
DOIs	https://doi.org/10.1109/BHI.2018.8333402
Publication status	Published - 9 Apr 2018
Event	2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018 - Las Vegas, United States Duration: 4 Mar 2018 → 7 Mar 2018

Conference

Conference	2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018
Country/Territory	United States
City	Las Vegas
Period	4/03/18 → 7/03/18

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10.1109/BHI.2018.8333402

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Hatziagapiou, K., Braoudaki, M., Bethanis, K., Yannakopoulou, K., Anastasiou, A., Koutsouri, G., Koutsouris, D., & Lambrou, G. I. (2018). Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies. In 2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018 (Vol. 2018-January, pp. 194-197). Institute of Electrical and Electronics Engineers (IEEE). https://doi.org/10.1109/BHI.2018.8333402

Hatziagapiou, Kyriaki ; Braoudaki, Maria ; Bethanis, Kostas et al. / Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies. 2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018. Vol. 2018-January Institute of Electrical and Electronics Engineers (IEEE), 2018. pp. 194-197

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title = "Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies",

abstract = "Cyclodextrins (CD) have been playing a very important role in the formulation of poorly water-soluble drugs by improving apparent drug solubility and/or dissolution. In the current study we focused on the investigation of the cytotoxic effect of cyclodextrin/Gefitinib in inclusion with three types of cyclodextrin, as well as in its inhibitory activity of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity using biological assays. The activity of Gefitinib and Gefitinib/cyclodextrin were measured in pediatric neuroblastoma (NB) tumor cell lines. We have shown that CD/Gefitinib complexes are effective against neuroblastoma cells in vitro. Our studies provided a detailed picture of inclusion of Gefitinib in cyclodextrins and verify improved efficacy of the CD-encapsulated drug in cytotoxicity assays on pediatric tumor cell lines. An understanding of the structural details of guest inclusion in CDs may be useful in the engineering of modified guest-host preparations with optimized pharmacological properties and shape future therapeutic strategies.",

author = "Kyriaki Hatziagapiou and Maria Braoudaki and Kostas Bethanis and Konstantina Yannakopoulou and Athanasios Anastasiou and Georgia Koutsouri and Dimitrios Koutsouris and Lambrou, {George I.}",

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doi = "10.1109/BHI.2018.8333402",

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Hatziagapiou, K, Braoudaki, M, Bethanis, K, Yannakopoulou, K, Anastasiou, A, Koutsouri, G, Koutsouris, D & Lambrou, GI 2018, Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies. in 2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018. vol. 2018-January, Institute of Electrical and Electronics Engineers (IEEE), pp. 194-197, 2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018, Las Vegas, United States, 4/03/18. https://doi.org/10.1109/BHI.2018.8333402

Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies. / Hatziagapiou, Kyriaki; Braoudaki, Maria; Bethanis, Kostas et al.
2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018. Vol. 2018-January Institute of Electrical and Electronics Engineers (IEEE), 2018. p. 194-197.

Research output: Chapter in Book/Report/Conference proceeding › Conference contribution

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AU - Bethanis, Kostas

AU - Yannakopoulou, Konstantina

AU - Anastasiou, Athanasios

AU - Koutsouri, Georgia

AU - Koutsouris, Dimitrios

AU - Lambrou, George I.

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N2 - Cyclodextrins (CD) have been playing a very important role in the formulation of poorly water-soluble drugs by improving apparent drug solubility and/or dissolution. In the current study we focused on the investigation of the cytotoxic effect of cyclodextrin/Gefitinib in inclusion with three types of cyclodextrin, as well as in its inhibitory activity of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity using biological assays. The activity of Gefitinib and Gefitinib/cyclodextrin were measured in pediatric neuroblastoma (NB) tumor cell lines. We have shown that CD/Gefitinib complexes are effective against neuroblastoma cells in vitro. Our studies provided a detailed picture of inclusion of Gefitinib in cyclodextrins and verify improved efficacy of the CD-encapsulated drug in cytotoxicity assays on pediatric tumor cell lines. An understanding of the structural details of guest inclusion in CDs may be useful in the engineering of modified guest-host preparations with optimized pharmacological properties and shape future therapeutic strategies.

AB - Cyclodextrins (CD) have been playing a very important role in the formulation of poorly water-soluble drugs by improving apparent drug solubility and/or dissolution. In the current study we focused on the investigation of the cytotoxic effect of cyclodextrin/Gefitinib in inclusion with three types of cyclodextrin, as well as in its inhibitory activity of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity using biological assays. The activity of Gefitinib and Gefitinib/cyclodextrin were measured in pediatric neuroblastoma (NB) tumor cell lines. We have shown that CD/Gefitinib complexes are effective against neuroblastoma cells in vitro. Our studies provided a detailed picture of inclusion of Gefitinib in cyclodextrins and verify improved efficacy of the CD-encapsulated drug in cytotoxicity assays on pediatric tumor cell lines. An understanding of the structural details of guest inclusion in CDs may be useful in the engineering of modified guest-host preparations with optimized pharmacological properties and shape future therapeutic strategies.

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BT - 2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018

PB - Institute of Electrical and Electronics Engineers (IEEE)

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Hatziagapiou K, Braoudaki M, Bethanis K, Yannakopoulou K, Anastasiou A, Koutsouri G et al. Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies. In 2018 IEEE EMBS International Conference on Biomedical and Health Informatics, BHI 2018. Vol. 2018-January. Institute of Electrical and Electronics Engineers (IEEE). 2018. p. 194-197 doi: 10.1109/BHI.2018.8333402

Computational analysis of Gefitinib and methylated-hydroxypropylated cyclodextrin inclusion complexes for the treatment of childhood malignancies

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