TY - JOUR
T1 - N-Trimethylated chitosan coating white adipose tissue vascular-targeting oral nano-system for the enhanced anti-obesity effects of celastrol
AU - Xian, Jing
AU - Zhong, Xuemei
AU - Huang, Qi
AU - Gu, Huan
AU - Feng, Yixuan
AU - Sun, Jiayi
AU - Wang, Di
AU - Li, Jingjing
AU - Zhang, Chen
AU - Wu, Yihan
AU - Zhang, Jinming
N1 - Publisher Copyright:
© 2023 Elsevier B.V.
PY - 2023/5/1
Y1 - 2023/5/1
N2 - Oral nanoparticles (NPs) are more suitable for obesity control compared to NPs administered intravenously, as their convenience increases patient compliance. Herein, we developed an oral nano-system to improve the anti-obesity efficacy of celastrol (Cel). The observed enhanced efficacy was mediated by zein core NPs decorated with adipose-homing peptides that were coated with N-trimethylated chitosan. The optimized Cel/AHP-NPs@TMC exhibited spherical morphology by TEM, as well as narrow size distribution (221.76 ± 6.73 nm) and adequate stability in a gastrointestinal environment. Based on the combined delivery advantages of AHP-NPs@TMC – i.e., improved cellular internalization within Caco-2 cells and enhanced white adipose tissue (WAT) vascular targeting – Cel/AHP-NPs@TMC significantly reduced the body weight, blood lipid levels, adipose inflammation, and WAT distribution in diet-induced obese mice without side-effects. In short, this study provides clear evidence that TMC-based oral NPs can effectively improve celastrol for obesity treatment.
AB - Oral nanoparticles (NPs) are more suitable for obesity control compared to NPs administered intravenously, as their convenience increases patient compliance. Herein, we developed an oral nano-system to improve the anti-obesity efficacy of celastrol (Cel). The observed enhanced efficacy was mediated by zein core NPs decorated with adipose-homing peptides that were coated with N-trimethylated chitosan. The optimized Cel/AHP-NPs@TMC exhibited spherical morphology by TEM, as well as narrow size distribution (221.76 ± 6.73 nm) and adequate stability in a gastrointestinal environment. Based on the combined delivery advantages of AHP-NPs@TMC – i.e., improved cellular internalization within Caco-2 cells and enhanced white adipose tissue (WAT) vascular targeting – Cel/AHP-NPs@TMC significantly reduced the body weight, blood lipid levels, adipose inflammation, and WAT distribution in diet-induced obese mice without side-effects. In short, this study provides clear evidence that TMC-based oral NPs can effectively improve celastrol for obesity treatment.
KW - Celastrol
KW - Inflammation
KW - N-trimethylated chitosan
KW - Obesity
KW - Oral targeting nanoparticles
UR - http://www.scopus.com/inward/record.url?scp=85150857018&partnerID=8YFLogxK
U2 - 10.1016/j.ijbiomac.2023.124023
DO - 10.1016/j.ijbiomac.2023.124023
M3 - Journal article
C2 - 36924876
AN - SCOPUS:85150857018
SN - 0141-8130
VL - 236
JO - International Journal of Biological Macromolecules
JF - International Journal of Biological Macromolecules
M1 - 124023
ER -