罗素转移体用于透皮输送:设计,优化和体外评估
Jiawen Wang1, Yuanyuan Zhao2, Bingtao Zhai1
1State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), and Shaanxi Key Laboratory of Chinese Medicine Fundamentals and New Drugs Research, and Shaanxi Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Shaanxi University of Chinese Medicine, Xi'an 712046, China.
Molecules (Basel, Switzerland)
|October 14, 2023
概括
这项研究开发了一种用于改善通过皮肤递送的洛转移体凝 (PTG). 这种PTG配方增强了花素的作用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 皮肤病学 皮肤病学
背景情况:
- 罗 (Phl) 是一种具有抗氧化和抗癌特性的黄类化合物,其水溶性差,生物可用性低.
- 仅限于Phl的临床应用,需要采取战略来提高其溶解性和皮肤健康的有效性.
- 开发有效的透皮传递系统对于对抗皮肤衰老和氧化损伤至关重要.
研究的目的:
- 开发和评估一种用于增强透皮药物递送的洛转移体凝 (PTG).
- 为了提高罗的生物可用性和抗衰老潜力.
- 创建一个稳定有效的局部抗氧化剂产品.
主要方法:
- 用薄膜分散超声波制备了素转移体 (Phl-TFs).
- 描述涉及TEM,DSC,FTIR和XRD;可溶性通过Log P.进行评估.
- 评估了体外皮肤透率 (弗朗兹细胞),小鼠体内药理动力学以及D-gal小鼠模型中的抗氧化活性.
主要成果:
- 优化了Phl-TFs成功地准备了特定的比率和参数.
- 与phloretin.TF相比,Phl-TFs表现出显著更高的Log P (2.26),与phloretin.TF相比,Phl-TFs表现出明显更高的Log P (2.26).
- 与对照剂相比,PTG配方表现出增强的累积皮肤透 (842.73μg/cm2),增加Cmax (1.39倍) 和AUC (1.97倍) 和在老老鼠中表现出优异的抗氧化作用.
结论:
- 成功开发出稳定且安全的氨酸转移体 (Phl-TFs) 和氨酸转移体凝 (PTG) 制剂.
- 在体内研究证实了PTG配方的透皮透和抗氧化疗效.
- 开发的PTG为未来的抗衰老和抗氧化剂局部产品开发提供了有希望的基础.
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