Colonic delivery of celastrol-loaded layer-by-layer liposomes with pectin/trimethylated chitosan coating to enhance its anti-ulcerative colitis effects

Jing Xian; Xuemei Zhong; Huan Gu; Xiao Wang; Jiaxin Li; Jingjing Li; Yihan Wu; Chen Zhang; Jinming Zhang

doi:10.3390/pharmaceutics13122005

Colonic delivery of celastrol-loaded layer-by-layer liposomes with pectin/trimethylated chitosan coating to enhance its anti-ulcerative colitis effects

Jing Xian, Xuemei Zhong, Huan Gu, Xiao Wang, Jiaxin Li, Jingjing Li, Yihan Wu, Chen Zhang (Corresponding Author), Jinming Zhang (Corresponding Author)

Research output: Journal article publication › Journal article › Academic research › peer-review

28 Citations (Scopus)

Abstract

Herein, a flexible oral colon-targeting delivery system, mediated by electrostatic layer-by-layer alternate deposition with pectin-trimethyl chitosan (TMC) onto liposomes-loading celastrol (Cel/PT-LbL Lipo), was fabricated to enhance anti-UC efficacy. Along with layer-by-layer coating, Cel/Lipo exhibited surface charge reversal, a slight increase in particle size, and a sustained drug release profile in a simulative gastrointestinal tract medium. Based on its bilayer coating of polysaccharides, Cel/PT-LbL Lipo alleviated cytotoxicity of celastrol in colon epithelial NCM460 cells. Due to the strong mucoadhesion of TMC with mucin, PT-LbL Lipo benefited colon localization and prolonged retention ability of its payloads. Ultimately, Cel/PT-LbL Lipo significantly mitigated colitis symptoms and accelerated colitis repair in DSS-treated mice by regulating the levels of proinflammatory factors related to the TLR4/MyD88/NF-κB signaling pathway. Collectively, this study demonstrates that the pectin/trimethylated chitosan coating may allow for Cel/PT-LbL Lipo to function as a more beneficial therapeutic strategy for UC treatment.

Original language	English
Article number	2005
Journal	Pharmaceutics
Volume	13
Issue number	12
DOIs	https://doi.org/10.3390/pharmaceutics13122005
Publication status	Published - Dec 2021

Keywords

Celastrol
Layer-by-layer
Liposomes
Trimethylated chitosan
Ulcerative colitis

ASJC Scopus subject areas

Pharmaceutical Science

More information

10.3390/pharmaceutics13122005

Cite this

@article{059ea8a4bfc84576833c8095c96f617d,

title = "Colonic delivery of celastrol-loaded layer-by-layer liposomes with pectin/trimethylated chitosan coating to enhance its anti-ulcerative colitis effects",

abstract = "Herein, a flexible oral colon-targeting delivery system, mediated by electrostatic layer-by-layer alternate deposition with pectin-trimethyl chitosan (TMC) onto liposomes-loading celastrol (Cel/PT-LbL Lipo), was fabricated to enhance anti-UC efficacy. Along with layer-by-layer coating, Cel/Lipo exhibited surface charge reversal, a slight increase in particle size, and a sustained drug release profile in a simulative gastrointestinal tract medium. Based on its bilayer coating of polysaccharides, Cel/PT-LbL Lipo alleviated cytotoxicity of celastrol in colon epithelial NCM460 cells. Due to the strong mucoadhesion of TMC with mucin, PT-LbL Lipo benefited colon localization and prolonged retention ability of its payloads. Ultimately, Cel/PT-LbL Lipo significantly mitigated colitis symptoms and accelerated colitis repair in DSS-treated mice by regulating the levels of proinflammatory factors related to the TLR4/MyD88/NF-κB signaling pathway. Collectively, this study demonstrates that the pectin/trimethylated chitosan coating may allow for Cel/PT-LbL Lipo to function as a more beneficial therapeutic strategy for UC treatment.",

keywords = "Celastrol, Layer-by-layer, Liposomes, Trimethylated chitosan, Ulcerative colitis",

author = "Jing Xian and Xuemei Zhong and Huan Gu and Xiao Wang and Jiaxin Li and Jingjing Li and Yihan Wu and Chen Zhang and Jinming Zhang",

note = "Publisher Copyright: {\textcopyright} 2021 by the authors. Licensee MDPI, Basel, Switzerland.",

year = "2021",

month = dec,

doi = "10.3390/pharmaceutics13122005",

language = "English",

volume = "13",

journal = "Pharmaceutics",

issn = "1999-4923",

publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",

number = "12",

}

TY - JOUR

T1 - Colonic delivery of celastrol-loaded layer-by-layer liposomes with pectin/trimethylated chitosan coating to enhance its anti-ulcerative colitis effects

AU - Xian, Jing

AU - Zhong, Xuemei

AU - Gu, Huan

AU - Wang, Xiao

AU - Li, Jiaxin

AU - Li, Jingjing

AU - Wu, Yihan

AU - Zhang, Chen

AU - Zhang, Jinming

PY - 2021/12

Y1 - 2021/12

N2 - Herein, a flexible oral colon-targeting delivery system, mediated by electrostatic layer-by-layer alternate deposition with pectin-trimethyl chitosan (TMC) onto liposomes-loading celastrol (Cel/PT-LbL Lipo), was fabricated to enhance anti-UC efficacy. Along with layer-by-layer coating, Cel/Lipo exhibited surface charge reversal, a slight increase in particle size, and a sustained drug release profile in a simulative gastrointestinal tract medium. Based on its bilayer coating of polysaccharides, Cel/PT-LbL Lipo alleviated cytotoxicity of celastrol in colon epithelial NCM460 cells. Due to the strong mucoadhesion of TMC with mucin, PT-LbL Lipo benefited colon localization and prolonged retention ability of its payloads. Ultimately, Cel/PT-LbL Lipo significantly mitigated colitis symptoms and accelerated colitis repair in DSS-treated mice by regulating the levels of proinflammatory factors related to the TLR4/MyD88/NF-κB signaling pathway. Collectively, this study demonstrates that the pectin/trimethylated chitosan coating may allow for Cel/PT-LbL Lipo to function as a more beneficial therapeutic strategy for UC treatment.

AB - Herein, a flexible oral colon-targeting delivery system, mediated by electrostatic layer-by-layer alternate deposition with pectin-trimethyl chitosan (TMC) onto liposomes-loading celastrol (Cel/PT-LbL Lipo), was fabricated to enhance anti-UC efficacy. Along with layer-by-layer coating, Cel/Lipo exhibited surface charge reversal, a slight increase in particle size, and a sustained drug release profile in a simulative gastrointestinal tract medium. Based on its bilayer coating of polysaccharides, Cel/PT-LbL Lipo alleviated cytotoxicity of celastrol in colon epithelial NCM460 cells. Due to the strong mucoadhesion of TMC with mucin, PT-LbL Lipo benefited colon localization and prolonged retention ability of its payloads. Ultimately, Cel/PT-LbL Lipo significantly mitigated colitis symptoms and accelerated colitis repair in DSS-treated mice by regulating the levels of proinflammatory factors related to the TLR4/MyD88/NF-κB signaling pathway. Collectively, this study demonstrates that the pectin/trimethylated chitosan coating may allow for Cel/PT-LbL Lipo to function as a more beneficial therapeutic strategy for UC treatment.

KW - Celastrol

KW - Layer-by-layer

KW - Liposomes

KW - Trimethylated chitosan

KW - Ulcerative colitis

UR - http://www.scopus.com/inward/record.url?scp=85120804703&partnerID=8YFLogxK

U2 - 10.3390/pharmaceutics13122005

DO - 10.3390/pharmaceutics13122005

M3 - Journal article

AN - SCOPUS:85120804703

SN - 1999-4923

VL - 13

JO - Pharmaceutics

JF - Pharmaceutics

IS - 12

M1 - 2005

ER -

Colonic delivery of celastrol-loaded layer-by-layer liposomes with pectin/trimethylated chitosan coating to enhance its anti-ulcerative colitis effects

Abstract

Keywords

ASJC Scopus subject areas

More information

Other files and links

Fingerprint

Cite this