雷公藤内酯负载固体脂质纳米凝胶:制备与体外评估

IF 2.9 4区 医学 Q1 Medicine
Chun-Feng Lu, Ye Dai, Yun Tao, Qiu-Yi Yin, Yan Jiang, Ting-Wang Jiang
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引用次数: 0

摘要

为了局部递送曲普内酯(TPL),在研究其对 HaCaT 细胞的抑制活性之前,我们试图开发并表征基于固体脂质纳米颗粒的凝胶(SLNs-凝胶)。TPL-SLNs(TPL-SLNs)的制备方法包括熔融-乳液超超声和低温凝固。确定的 TPL-SLNs 特性包括粒度(PS)、封装效率(EE)、Zeta 电位(ZP)、显微形态学和 TPL 体外释放。将 TPL-SLNs 配制成凝胶后,我们采用弗朗兹扩散细胞法评估了 TPL-SLNs 凝胶在大鼠皮肤上的渗透性和渗透特征。成像结果表明,TPL-SLNs 颗粒均匀且分散良好。同时,TPL-SLNs 的 PS 和 ZP 分别为 89.21 ± 9.68 nm 和 -41.3 ± 6.23 mV,EE 为 89.3%。我们还观察到,与游离 TPL 相比,TPL-SLNs 的体外 TPL 释放模式有了明显改善。此外,与游离 TPL 相比,TPL-SLNs-凝胶的累积渗透率更高(5.28 倍)。此外,TPL-SLNs-凝胶对 HaCaT 细胞的细胞抑制活性大大高于游离 TPL 和 TPL-SLNs。总之,SLNs-凝胶等递送系统有可能提高 TPL 的透皮生物利用度,从而有效抑制 HaCaT 细胞的增殖。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Triptolide-Loaded Solid Lipid Nanogel: Preparation and In-Vitro Evaluation
In order to topically deliver triptolide (TPL), we sought to develop and characterize solid lipid nano-particles based gel (SLNs-gel) before we investigated its inhibitory activity on HaCaT cells. Preparation of TPL-loaded SLNs (TPL-SLNs) was performed with a method involving melt-emulsion ultra-sonication and solidification at low temperature. The determined characteristics of TPL-SLNs were particle size (PS), encapsulation efficiency (EE), zeta potential (ZP), microscopic mor phology and release of TPL In-Vitro. After TPL-SLNs have been formulated into gel, we used the Franz diffusion cell method to evaluate the skin permeation and penetration characteristics of TPL-SLNs-gel on rat’s skin. Imaging results showed that particles of TPL-SLNs were homogeneous and well-dispersed. Meanwhile, the PS and ZP of TPL-SLNs were 89.21 ± 9.68 nm and −41.3 ± 6.23 mV, respectively, with EE being 89.3%. Also, we observed a significant improvement in pattern of In-Vitro TPL release from TPL-SLNs compared to free TPL. Furthermore, the cumulative penetration of TPL-SLNs-gel was higher (5.28 times) compared to free TPL. Besides, TPL-SLNs-gel demonstrated substantial higher cytostatic activity on HaCaT cells comparable to both free TPL and TPL-SLNs. Altogether, it is evident that a delivery system like SLNs-gel can potentially increase the transdermal bioavailability of TPL for effective inhibition of proliferous HaCaT cells
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来源期刊
CiteScore
4.30
自引率
17.20%
发文量
145
审稿时长
2.3 months
期刊介绍: Information not localized
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