Transdermal drug delivery of triptolide-loaded nanostructured lipid carriers: Preparation, pharmacokinetic, and evaluation for rheumatoid arthritis
Transdermal drug delivery of triptolide-loaded nanostructured lipid carriers: Preparation, pharmacokinetic, and evaluation for rheumatoid arthritis
复制标题
载雷公藤甲素的纳米结构脂质载体的经皮给药：制备、药代动力学及对类风湿性关节炎的评估
DOI：
10.1016/j.ijpharm.2018.11.024
复制
发表时间：
2019-01-10
影响因子：
5.8
通讯作者：
Liu, Jiyong
中科院分区：
文献类型：
--
作者：
Gu, Yongwei;Tang, Xiaomeng;Liu, Jiyong
The objective of this present study was to develop and evaluate the triptolide-loaded nanostructured lipid carriers (TPL-NLCs) for transdermal drug delivery system (TDDS). TPL-NLCs was prepared with emulsification technique and optimized by central composite design of a response surface methodology (CCD-RSM). The optimized TPL-NLCs were spherical and physically stable with the average size of 139.6.0 +/- 2.53 nm and Zeta potential of -36.03 +/- 2.41 mV. The encapsulation efficiency and drug loading were 97.15% +/- 9.46 and 10.35% +/- 1.12, respectively. Moreover, the in vitro release study showed that TPL-NLCs had a sustained release profiles and the in vitro penetration study indicated that TPL-NLCs could effectively penetrate into skin. Besides, the methodology of skin-blood synchronous microdialysis was established to evaluate the pharmacokinetics of TPL-NLCs in vivo and the results displayed that the TPL concentration in skin was higher than that in blood. And TPL-NLCs presented a remarkable effect of decreasing knee edema, inhibiting inflammation by regulating the levels of TNF-alpha, IL-1 beta and IL-6, which indicated that TPL-NLCs was a promising topical administration in treatment of edema and inflammation associated with rheumatoid arthritis (RA).
