脂肪组织
脂肪生成
硬脂酸
化学
脂肪细胞
药理学
生物物理学
生物化学
医学
有机化学
生物
作者
Shuang Liang,Zekun Li,Cheng Bao,Bin Liu,Huijuan Zhang,Yuan Yu,Huiling Yan,Shanan Chen,Hui Zhang,Wenbiao Shi,Wendi Teng,Yuan Li
出处
期刊:Small
[Wiley]
日期:2023-06-01
卷期号:19 (39)
被引量:4
标识
DOI:10.1002/smll.202301751
摘要
Sustained 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.
科研通智能强力驱动
Strongly Powered by AbleSci AI