A pharmacokinetic study of GC-1 delivery using a nanochannel membrane device

被引:6
作者
Filgueira, Carly S. [1 ]
Ballerini, Andrea [1 ,2 ]
Nicolov, Eugenia [1 ]
Chua, Corrine Ying Xuan [1 ]
Jain, Priya [1 ]
Smith, Zachary W. [1 ]
Gilbert, April L. [1 ]
Scaglione, Francesco [2 ]
Grattoni, Alessandro [1 ]
机构
[1] Houston Methodist Res Inst, Dept Nanomed, Houston, TX USA
[2] Univ Milan, Dept Oncol & Oncohematol, Milan, Italy
关键词
Thyroid gland; Nanochannel membrane device (NMD); GC-1 (Sobetirome); Pharmacokinetic; Weight loss; THYROID-HORMONE RECEPTOR; TESTOSTERONE REPLACEMENT THERAPY; AGONIST GC-1; BODY-WEIGHT; CHOLESTEROL; ACTIVATION; DRUG; ASSOCIATION; VOLUME; RATS;
D O I
10.1016/j.nano.2017.02.012
中图分类号
TB3 [工程材料学];
学科分类号
0805 ; 080502 ;
摘要
This study demonstrated a nanochannel membrane device (NMD) for controlled and sustained release of GC-1 in rats, in the context of the treatment of metabolic syndrome. Release profiles were established in vitro both with and without 5% labrasol for over 2 months. In vivo pharmacokinetic evaluation showed effective GC-1 plasma concentrations, which resulted in significant reductions in body weight after just one week of treatment when compared to the NMD releasing vehicle only (PBS). We also provided evidence that rats treated with NMD-GC-1 present sub-active thyroids and clear differences in the morphology of the epithelium and follicles as compared to the controls, while the heart showed changes in weight. Moreover, body temperatures remained stable throughout treatment, and glucose, pancreatic islet size, and liver histology appeared similar between the treated and control groups. Prolonged constant administration of GC-1 from the NMD proved to be a valid strategy to facilitate weight loss. (c) 2017 Elsevier Inc. All rights reserved.
引用
收藏
页码:1739 / 1744
页数:6
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