Affiliation:
1. Key Laboratory of Precision Nutrition and Food Quality Department of Nutrition and Health China Agricultural University Beijing 100193 China
2. Research Center of Food Colloids and Delivery of Functionality College of Food Science and Nutritional Engineering China Agricultural University Beijing 100083 China
3. School of Life Science Ludong University Yantai 264000 China
Abstract
AbstractSustained oral uncoupler 2,4‐dinitrophenol (DNP) administration exerts prominent anti‐obesity effects, but the adipose tissue off‐target disadvantage leads to systemic adverse effects. A novel non‐cardiotoxicity DNP delivery method using a biocompatible microneedles patch containing the amphiphilic tetradecanoic acid‐DNP ester (TADNP) is described, which is synthesized via esterification on the phenolic hydroxyl of DNP. The TADNP is self‐assembled as nanomicelles, which enhance the endocytosis rate of DNP by adipocytes and its permeation in isolated adipose tissues. The microenvironment of adipose tissues promotes the massive release of DNP and plasma and simulated gastrointestinal fluids. The microneedles‐delivered TADNP nanomicelles (MN‐TADNP) effectively deliver DNP in treated adipose tissues and reduce DNP content in off‐target organs. Both oral and MN patch‐delivered TADNP micelles effectively exert anti‐obesity effects in a mouse model of high‐fat diet‐induced obesity; and noteworthily, MN‐TADNP exhibit more satisfactory biosafety than oral administration. Here, a smart MN patch loaded with tetradecanoic acid‐modified DNP is reported, which enhances its accumulation in adipose tissues and exerts an anti‐obesity effect without causing any systemic toxicity.
Funder
National Natural Science Foundation of China
Subject
Biomaterials,Biotechnology,General Materials Science,General Chemistry
Cited by
2 articles.
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