Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity

This study prepared nanocapsules (NCs) with excellent self-controlled antimicrobial activity at pH 6–7 and humidity 45–100%, conditions in which most bacterial and fungal strains thrive. The nanocapsule substrate (NC@SiO<sub>2</sub>) was 676 nm in diameter, and the ligand-grafted capsule...

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Main Authors: Eunjoo Koh, Yong Taek Lee
Format: Article
Language:English
Published: MDPI AG 2022-01-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/14/2/280
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author Eunjoo Koh
Yong Taek Lee
author_facet Eunjoo Koh
Yong Taek Lee
author_sort Eunjoo Koh
collection DOAJ
description This study prepared nanocapsules (NCs) with excellent self-controlled antimicrobial activity at pH 6–7 and humidity 45–100%, conditions in which most bacterial and fungal strains thrive. The nanocapsule substrate (NC@SiO<sub>2</sub>) was 676 nm in diameter, and the ligand-grafted capsule (NC@SiO<sub>2</sub>-g-MAA) was 888 nm. The large surface area and outer ligand brush of the NCs induced a rapid, self-controlled antibacterial response in the pH and humidity conditions needed for industrial and medical applications. Ligand-brush NCs containing an anionic antimicrobial drug had a rapid release effect because of the repellent electrostatic force and swelling properties of the ligand brushes. Controlled release of the drug was achieved at pH 6 and humidity of 45% and 100%. As many carboxylic acid groups are deprotonated into carboxylic acids at pH 5, the NC@SiO<sub>2</sub>-g-MAA had a high negative charge density. Carboxylic acid groups are anionized (–COO<sup>−</sup>) at pH 6 and above and push each other out of the capsule, expanding the outer shell as in a polymer brush to create the release behavior. The surface potential of the NC intermediate (NC@SiO<sub>2</sub>-MPS) was −23.45 [mV], and the potential of the capsule surface decreased to −36.4 [mV] when the MAA ligand brushes were grafted onto the surface of the capsule intermediate. In an antimicrobial experiment using <i>Escherichia coli</i>, a clear zone of 13–20 mm formed at pH 6, and the <i>E. coli</i> was eradicated completely at pH 6 and pH 7 when the humidity was 100%.
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spelling doaj.art-39ada60536e34288a09b249eaafacc822023-11-23T21:36:37ZengMDPI AGPharmaceutics1999-49232022-01-0114228010.3390/pharmaceutics14020280Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and HumidityEunjoo Koh0Yong Taek Lee1Department of Chemical Engineering, Faculty of Chemical Engineering, Kyung Hee University, Deogyeong-daero, Giheung-gu, Yongin-si 17104, KoreaDepartment of Chemical Engineering, Faculty of Chemical Engineering, Kyung Hee University, Deogyeong-daero, Giheung-gu, Yongin-si 17104, KoreaThis study prepared nanocapsules (NCs) with excellent self-controlled antimicrobial activity at pH 6–7 and humidity 45–100%, conditions in which most bacterial and fungal strains thrive. The nanocapsule substrate (NC@SiO<sub>2</sub>) was 676 nm in diameter, and the ligand-grafted capsule (NC@SiO<sub>2</sub>-g-MAA) was 888 nm. The large surface area and outer ligand brush of the NCs induced a rapid, self-controlled antibacterial response in the pH and humidity conditions needed for industrial and medical applications. Ligand-brush NCs containing an anionic antimicrobial drug had a rapid release effect because of the repellent electrostatic force and swelling properties of the ligand brushes. Controlled release of the drug was achieved at pH 6 and humidity of 45% and 100%. As many carboxylic acid groups are deprotonated into carboxylic acids at pH 5, the NC@SiO<sub>2</sub>-g-MAA had a high negative charge density. Carboxylic acid groups are anionized (–COO<sup>−</sup>) at pH 6 and above and push each other out of the capsule, expanding the outer shell as in a polymer brush to create the release behavior. The surface potential of the NC intermediate (NC@SiO<sub>2</sub>-MPS) was −23.45 [mV], and the potential of the capsule surface decreased to −36.4 [mV] when the MAA ligand brushes were grafted onto the surface of the capsule intermediate. In an antimicrobial experiment using <i>Escherichia coli</i>, a clear zone of 13–20 mm formed at pH 6, and the <i>E. coli</i> was eradicated completely at pH 6 and pH 7 when the humidity was 100%.https://www.mdpi.com/1999-4923/14/2/280controlled drug releaseself-antibacterial activityligand brush nanocapsulepH and humidity responsecytotoxicity
spellingShingle Eunjoo Koh
Yong Taek Lee
Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
Pharmaceutics
controlled drug release
self-antibacterial activity
ligand brush nanocapsule
pH and humidity response
cytotoxicity
title Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
title_full Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
title_fullStr Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
title_full_unstemmed Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
title_short Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
title_sort preparation of ligand brush nanocapsules for robust self controlled antimicrobial activity with low cytotoxicity at target ph and humidity
topic controlled drug release
self-antibacterial activity
ligand brush nanocapsule
pH and humidity response
cytotoxicity
url https://www.mdpi.com/1999-4923/14/2/280
work_keys_str_mv AT eunjookoh preparationofligandbrushnanocapsulesforrobustselfcontrolledantimicrobialactivitywithlowcytotoxicityattargetphandhumidity
AT yongtaeklee preparationofligandbrushnanocapsulesforrobustselfcontrolledantimicrobialactivitywithlowcytotoxicityattargetphandhumidity