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Effects of cholesterol incorporation on the physicochemical, colloidal, and biological characteristics of pH-sensitive AB2 miktoarm polymer-based polymersomes

In our previous study, a histidine-based AB miktoarm polymer, methoxy poly(ethylene glycol)- -poly( -histidine) (mPEG- -(PolyHis) ), was designed to construct pH-sensitive polymersomes that transform in acidic pH; the polymer self-assembles into a structure that mimics phospholipids. In this study,... Full description

Journal Title: Colloids and Surfaces B: Biointerfaces 01 April 2014, Vol.116, pp.128-137
Main Author: Yin, Haiqing
Other Authors: Kang, Han Chang , Huh, Kang Moo , Bae, You Han
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0927-7765 ; E-ISSN: 1873-4367 ; DOI: 10.1016/j.colsurfb.2013.12.041
Link: https://www.sciencedirect.com/science/article/pii/S0927776513007960
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recordid: elsevier_sdoi_10_1016_j_colsurfb_2013_12_041
title: Effects of cholesterol incorporation on the physicochemical, colloidal, and biological characteristics of pH-sensitive AB2 miktoarm polymer-based polymersomes
format: Article
creator:
  • Yin, Haiqing
  • Kang, Han Chang
  • Huh, Kang Moo
  • Bae, You Han
subjects:
  • Cholesterol
  • Colloidal Stability
  • Miktoarm Polymer
  • Ph-Sensitive
  • Poly(Histidine)
  • Polymersome
  • Engineering
  • Chemistry
  • Anatomy & Physiology
ispartof: Colloids and Surfaces B: Biointerfaces, 01 April 2014, Vol.116, pp.128-137
description: In our previous study, a histidine-based AB miktoarm polymer, methoxy poly(ethylene glycol)- -poly( -histidine) (mPEG- -(PolyHis) ), was designed to construct pH-sensitive polymersomes that transform in acidic pH; the polymer self-assembles into a structure that mimics phospholipids. In this study, the polymersomes further imitated liposomes due to the incorporation of cholesterol (CL). The hydrodynamic radii of the polymersomes increased with increasing CL wt% ( , 70 nm for 0 wt% 91 nm for 1 wt%), resulting in an increased capacity for encapsulating hydrophilic drugs ( , 0.92 μL/mg for 0 wt% 1.42 μL/mg for 1 wt%). The CL incorporation enhanced the colloidal stability of the polymersomes in the presence of serum protein and retarded their payload release. However, CL-incorporating polymersomes still demonstrated accelerated release of a hydrophilic dye ( , 5(6)-carboxyfluorescein (CF)) below pH 6.8 without losing their desirable pH sensitivity. CF-loaded CL-incorporating polymersomes showed better cellular internalization than the hydrophilic CF, whereas doxorubicin (DOX)-loaded CL-incorporating polymersomes presented similar or somewhat lower anti-tumor effects than free hydrophobic DOX. The findings suggest that CL-incorporating mPEG- -(PolyHis) -based polymersomes may have potential for intracellular drug delivery of chemical drugs due to their improved colloidal stability, lower drug loss during circulation, acidic pH-induced drug release, and endosomal disruption.
language: eng
source:
identifier: ISSN: 0927-7765 ; E-ISSN: 1873-4367 ; DOI: 10.1016/j.colsurfb.2013.12.041
fulltext: fulltext
issn:
  • 0927-7765
  • 09277765
  • 1873-4367
  • 18734367
url: Link


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titleEffects of cholesterol incorporation on the physicochemical, colloidal, and biological characteristics of pH-sensitive AB2 miktoarm polymer-based polymersomes
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subjectCholesterol ; Colloidal Stability ; Miktoarm Polymer ; Ph-Sensitive ; Poly(Histidine) ; Polymersome ; Engineering ; Chemistry ; Anatomy & Physiology
descriptionIn our previous study, a histidine-based AB miktoarm polymer, methoxy poly(ethylene glycol)- -poly( -histidine) (mPEG- -(PolyHis) ), was designed to construct pH-sensitive polymersomes that transform in acidic pH; the polymer self-assembles into a structure that mimics phospholipids. In this study, the polymersomes further imitated liposomes due to the incorporation of cholesterol (CL). The hydrodynamic radii of the polymersomes increased with increasing CL wt% ( , 70 nm for 0 wt% 91 nm for 1 wt%), resulting in an increased capacity for encapsulating hydrophilic drugs ( , 0.92 μL/mg for 0 wt% 1.42 μL/mg for 1 wt%). The CL incorporation enhanced the colloidal stability of the polymersomes in the presence of serum protein and retarded their payload release. However, CL-incorporating polymersomes still demonstrated accelerated release of a hydrophilic dye ( , 5(6)-carboxyfluorescein (CF)) below pH 6.8 without losing their desirable pH sensitivity. CF-loaded CL-incorporating polymersomes showed better cellular internalization than the hydrophilic CF, whereas doxorubicin (DOX)-loaded CL-incorporating polymersomes presented similar or somewhat lower anti-tumor effects than free hydrophobic DOX. The findings suggest that CL-incorporating mPEG- -(PolyHis) -based polymersomes may have potential for intracellular drug delivery of chemical drugs due to their improved colloidal stability, lower drug loss during circulation, acidic pH-induced drug release, and endosomal disruption.
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