雷公藤内酯负载固体脂质纳米凝胶：制备与体外评估

IF 4.6 Q2 MATERIALS SCIENCE, BIOMATERIALS

ACS Applied Bio Materials Pub Date : 2024-02-01 DOI:10.1166/jbn.2024.3781

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。

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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

ACS Applied Bio Materials Chemistry-Chemistry (all)

CiteScore

9.40

自引率

2.10%

发文量

464

期刊介绍： ACS Applied Bio Materials is an interdisciplinary journal publishing original research covering all aspects of biomaterials and biointerfaces including and beyond the traditional biosensing, biomedical and therapeutic applications. The journal is devoted to reports of new and original experimental and theoretical research of an applied nature that integrates knowledge in the areas of materials, engineering, physics, bioscience, and chemistry into important bio applications. The journal is specifically interested in work that addresses the relationship between structure and function and assesses the stability and degradation of materials under relevant environmental and biological conditions.