Development of pH-responsive starch-glycol chitosan nanogels for proapoptotic (KLAKLAK)2 peptide delivery

Seong Kyeong Kim; Yu Seok Youn; Kyung Taek Oh; Eun Seong Lee

doi:10.1177/0883911516676848

Development of pH-responsive starch-glycol chitosan nanogels for proapoptotic (KLAKLAK)₂ peptide delivery

Seong Kyeong Kim, Yu Seok Youn, Kyung Taek Oh, Eun Seong Lee

Department of Pharmacy

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

14 Scopus citations

Abstract

In this study, we report pH-responsive polysaccharidic nanogels for cytosolic peptide delivery. We conjugated starch to water-soluble glycol chitosan and pH-responsive 3-diethylaminopropylamine (starch-(glycol chitosan-3-diethylaminopropylamine)). Starch-(glycol chitosan-3-diethylaminopropylamine) self-organizes in aqueous solution, with the glycol chitosan blocks on the hydrophilic outer shell and starch and 3-diethylaminopropylamine blocks in the hydrogel inner core. The experimental results demonstrated that the protonation of 3-diethylaminopropylamine at pH 6.0 (endosomal pH) allowed for accelerated release of the encapsulated D-(KLAKLAK)₂ proapoptotic peptide from the nanogels as a result of electrostatic repulsion between D-(KLAKLAK)₂ and 3-diethylaminopropylamine. A hemolysis test using red blood cell membranes (as an endosomal membrane model) revealed the excellent endosomolytic activity of these nanogels, which likely stems from the proton-sponge effect of 3-diethylaminopropylamine at pH 6.0. As a result, these nanogels resulted in increased KB tumor cell ablation.

Original language	English
Pages (from-to)	345-354
Number of pages	10
Journal	Journal of Bioactive and Compatible Polymers
Volume	32
Issue number	4
DOIs	https://doi.org/10.1177/0883911516676848
State	Published - 1 Jul 2017

Keywords

3-diethylaminopropyl
D-(KLAKLAK) proapoptotic peptide
endosomolytic activity
Starch-glycol chitosan nanogels
tumor therapy

UN SDGs

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

Access to Document

10.1177/0883911516676848

Cite this

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title = "Development of pH-responsive starch-glycol chitosan nanogels for proapoptotic (KLAKLAK)2 peptide delivery",

abstract = "In this study, we report pH-responsive polysaccharidic nanogels for cytosolic peptide delivery. We conjugated starch to water-soluble glycol chitosan and pH-responsive 3-diethylaminopropylamine (starch-(glycol chitosan-3-diethylaminopropylamine)). Starch-(glycol chitosan-3-diethylaminopropylamine) self-organizes in aqueous solution, with the glycol chitosan blocks on the hydrophilic outer shell and starch and 3-diethylaminopropylamine blocks in the hydrogel inner core. The experimental results demonstrated that the protonation of 3-diethylaminopropylamine at pH 6.0 (endosomal pH) allowed for accelerated release of the encapsulated D-(KLAKLAK)2 proapoptotic peptide from the nanogels as a result of electrostatic repulsion between D-(KLAKLAK)2 and 3-diethylaminopropylamine. A hemolysis test using red blood cell membranes (as an endosomal membrane model) revealed the excellent endosomolytic activity of these nanogels, which likely stems from the proton-sponge effect of 3-diethylaminopropylamine at pH 6.0. As a result, these nanogels resulted in increased KB tumor cell ablation.",

keywords = "3-diethylaminopropyl, D-(KLAKLAK) proapoptotic peptide, endosomolytic activity, Starch-glycol chitosan nanogels, tumor therapy",

author = "Kim, \{Seong Kyeong\} and Youn, \{Yu Seok\} and Oh, \{Kyung Taek\} and Lee, \{Eun Seong\}",

note = "Publisher Copyright: {\textcopyright} SAGE Publications.",

year = "2017",

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doi = "10.1177/0883911516676848",

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AU - Kim, Seong Kyeong

AU - Youn, Yu Seok

AU - Oh, Kyung Taek

AU - Lee, Eun Seong

N1 - Publisher Copyright: © SAGE Publications.

PY - 2017/7/1

Y1 - 2017/7/1

N2 - In this study, we report pH-responsive polysaccharidic nanogels for cytosolic peptide delivery. We conjugated starch to water-soluble glycol chitosan and pH-responsive 3-diethylaminopropylamine (starch-(glycol chitosan-3-diethylaminopropylamine)). Starch-(glycol chitosan-3-diethylaminopropylamine) self-organizes in aqueous solution, with the glycol chitosan blocks on the hydrophilic outer shell and starch and 3-diethylaminopropylamine blocks in the hydrogel inner core. The experimental results demonstrated that the protonation of 3-diethylaminopropylamine at pH 6.0 (endosomal pH) allowed for accelerated release of the encapsulated D-(KLAKLAK)2 proapoptotic peptide from the nanogels as a result of electrostatic repulsion between D-(KLAKLAK)2 and 3-diethylaminopropylamine. A hemolysis test using red blood cell membranes (as an endosomal membrane model) revealed the excellent endosomolytic activity of these nanogels, which likely stems from the proton-sponge effect of 3-diethylaminopropylamine at pH 6.0. As a result, these nanogels resulted in increased KB tumor cell ablation.

AB - In this study, we report pH-responsive polysaccharidic nanogels for cytosolic peptide delivery. We conjugated starch to water-soluble glycol chitosan and pH-responsive 3-diethylaminopropylamine (starch-(glycol chitosan-3-diethylaminopropylamine)). Starch-(glycol chitosan-3-diethylaminopropylamine) self-organizes in aqueous solution, with the glycol chitosan blocks on the hydrophilic outer shell and starch and 3-diethylaminopropylamine blocks in the hydrogel inner core. The experimental results demonstrated that the protonation of 3-diethylaminopropylamine at pH 6.0 (endosomal pH) allowed for accelerated release of the encapsulated D-(KLAKLAK)2 proapoptotic peptide from the nanogels as a result of electrostatic repulsion between D-(KLAKLAK)2 and 3-diethylaminopropylamine. A hemolysis test using red blood cell membranes (as an endosomal membrane model) revealed the excellent endosomolytic activity of these nanogels, which likely stems from the proton-sponge effect of 3-diethylaminopropylamine at pH 6.0. As a result, these nanogels resulted in increased KB tumor cell ablation.

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