Honeycomb-like pH-responsive γ-cyclodextrin electrospun particles for highly efficient tumor therapy

Hyeong Sup Yu; Eun Seong Lee

doi:10.1016/j.carbpol.2019.115563

Honeycomb-like pH-responsive γ-cyclodextrin electrospun particles for highly efficient tumor therapy

Hyeong Sup Yu, Eun Seong Lee

Department of Biomedical-Chemical Engineering

The Catholic University of Korea

Research output: Contribution to journal › Article › peer-review

23 Scopus citations

Abstract

We report here the tumor-implantable microparticles with a honeycomb-like porous structure. These microparticles were prepared by electrospinning using γ-cyclodextrin (γ-CD) conjugated with 3-(diethylamino)propylamine (DEAP, as a pH-responsive moiety), named γ-CD-DEAP. The resulting microparticles had pore channels (constructed using γ-CD-DEAP) extending into the deep compartment of the microparticles and allowing efficient paclitaxel (PTX, as a chemotherapeutic model drug) entrapment by a simple hole-filling encapsulation process. Importantly, the hydrophobic DEAP (at pH 7.4) in the γ-CD-DEAP microparticles changed to hydrophilic DEAP (at pH 6.8) because of its acidic pH-induced protonation. This phenomenon resulted in an acidic pH-activated particle destruction by a charge-charge repulsion between the protonated DEAP moieties and allowed a pH-triggered release of the encapsulated PTX from the collapsed microparticles. Consequently, γ-CD-DEAP microparticles implanted at the tumor site caused a significant enhancement of the in vitro/in vivo tumor cell ablation, suggesting their significant potential as a chemotherapeutic implant for tumor therapy.

Original language	English
Article number	115563
Journal	Carbohydrate Polymers
Volume	230
DOIs	https://doi.org/10.1016/j.carbpol.2019.115563
State	Published - 15 Feb 2020

Bibliographical note

Funding Information:
This work was financially supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: NRF-2018R1A2B6000970 ) and by the Research Fund, 2019 of the Catholic University of Korea . Appendix A

Funding Information:
This work was financially supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: NRF-2018R1A2B6000970) and by the Research Fund, 2019 of the Catholic University of Korea.

Publisher Copyright:
© 2019 Elsevier Ltd

Keywords

Chemotherapy
Electrospinning
Paclitaxel
pH-responsive microparticles
γ-Cyclodextrin

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10.1016/j.carbpol.2019.115563

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title = "Honeycomb-like pH-responsive γ-cyclodextrin electrospun particles for highly efficient tumor therapy",

abstract = "We report here the tumor-implantable microparticles with a honeycomb-like porous structure. These microparticles were prepared by electrospinning using γ-cyclodextrin (γ-CD) conjugated with 3-(diethylamino)propylamine (DEAP, as a pH-responsive moiety), named γ-CD-DEAP. The resulting microparticles had pore channels (constructed using γ-CD-DEAP) extending into the deep compartment of the microparticles and allowing efficient paclitaxel (PTX, as a chemotherapeutic model drug) entrapment by a simple hole-filling encapsulation process. Importantly, the hydrophobic DEAP (at pH 7.4) in the γ-CD-DEAP microparticles changed to hydrophilic DEAP (at pH 6.8) because of its acidic pH-induced protonation. This phenomenon resulted in an acidic pH-activated particle destruction by a charge-charge repulsion between the protonated DEAP moieties and allowed a pH-triggered release of the encapsulated PTX from the collapsed microparticles. Consequently, γ-CD-DEAP microparticles implanted at the tumor site caused a significant enhancement of the in vitro/in vivo tumor cell ablation, suggesting their significant potential as a chemotherapeutic implant for tumor therapy.",

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author = "Yu, {Hyeong Sup} and Lee, {Eun Seong}",

note = "Funding Information: This work was financially supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: NRF-2018R1A2B6000970 ) and by the Research Fund, 2019 of the Catholic University of Korea . Appendix A Funding Information: This work was financially supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: NRF-2018R1A2B6000970) and by the Research Fund, 2019 of the Catholic University of Korea. Publisher Copyright: {\textcopyright} 2019 Elsevier Ltd",

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AU - Lee, Eun Seong

N1 - Funding Information: This work was financially supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: NRF-2018R1A2B6000970 ) and by the Research Fund, 2019 of the Catholic University of Korea . Appendix A Funding Information: This work was financially supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: NRF-2018R1A2B6000970) and by the Research Fund, 2019 of the Catholic University of Korea. Publisher Copyright: © 2019 Elsevier Ltd

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N2 - We report here the tumor-implantable microparticles with a honeycomb-like porous structure. These microparticles were prepared by electrospinning using γ-cyclodextrin (γ-CD) conjugated with 3-(diethylamino)propylamine (DEAP, as a pH-responsive moiety), named γ-CD-DEAP. The resulting microparticles had pore channels (constructed using γ-CD-DEAP) extending into the deep compartment of the microparticles and allowing efficient paclitaxel (PTX, as a chemotherapeutic model drug) entrapment by a simple hole-filling encapsulation process. Importantly, the hydrophobic DEAP (at pH 7.4) in the γ-CD-DEAP microparticles changed to hydrophilic DEAP (at pH 6.8) because of its acidic pH-induced protonation. This phenomenon resulted in an acidic pH-activated particle destruction by a charge-charge repulsion between the protonated DEAP moieties and allowed a pH-triggered release of the encapsulated PTX from the collapsed microparticles. Consequently, γ-CD-DEAP microparticles implanted at the tumor site caused a significant enhancement of the in vitro/in vivo tumor cell ablation, suggesting their significant potential as a chemotherapeutic implant for tumor therapy.

AB - We report here the tumor-implantable microparticles with a honeycomb-like porous structure. These microparticles were prepared by electrospinning using γ-cyclodextrin (γ-CD) conjugated with 3-(diethylamino)propylamine (DEAP, as a pH-responsive moiety), named γ-CD-DEAP. The resulting microparticles had pore channels (constructed using γ-CD-DEAP) extending into the deep compartment of the microparticles and allowing efficient paclitaxel (PTX, as a chemotherapeutic model drug) entrapment by a simple hole-filling encapsulation process. Importantly, the hydrophobic DEAP (at pH 7.4) in the γ-CD-DEAP microparticles changed to hydrophilic DEAP (at pH 6.8) because of its acidic pH-induced protonation. This phenomenon resulted in an acidic pH-activated particle destruction by a charge-charge repulsion between the protonated DEAP moieties and allowed a pH-triggered release of the encapsulated PTX from the collapsed microparticles. Consequently, γ-CD-DEAP microparticles implanted at the tumor site caused a significant enhancement of the in vitro/in vivo tumor cell ablation, suggesting their significant potential as a chemotherapeutic implant for tumor therapy.

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Honeycomb-like pH-responsive γ-cyclodextrin electrospun particles for highly efficient tumor therapy

Abstract

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Keywords

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