在水滑石纳米载体中配制甘草酸,以作为肝脏保护剂。

IF 5 3区 医学 Q1 PHARMACOLOGY & PHARMACY AAPS Journal Pub Date : 2024-11-19 DOI:10.1208/s12248-024-00986-8
Magali Hernández, Enrique Lima, Jonathan J Magaña, Adriana Ganem-Rondero
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引用次数: 0

摘要

这篇文章的重点是制备一种基于水滑石和甘草酸(GA)的纳米制剂,以寻求保护肝脏的效果。为此,通过改变以下条件制备了水滑石-GA 配方,以获得尺寸和 PDI(最低值)以及 Z 电位(最高值)方面的最佳系统:(i) 水滑石的类型(通过共沉淀或煅烧获得);使用的方法(超声波或高剪切搅拌);以及 (iii) 稳定剂的类型(Tween®80 或 Pluronic® F-127)。通过共沉淀、高剪切搅拌和添加稳定剂(Tween®80(HT-T80-GA:平均粒径 = 315 nm,PDI = 0.18,Z 电位 = -20.93)或 Pluronic® F-127(HT-PF127-GA:平均粒径 = 307 nm;PDI = 0.27,Z 电位 = -21.03)获得的水滑石效果最佳。经过稳定性研究后,我们选择了 HT-T80-GA 配方来研究抗氧化活性、细胞毒性和细胞内渗透能力。虽然溶液中的 GA 具有保肝作用,因而具有较高的存活率和抗氧化活性,但 HT-T80-GA 制剂中含有 GA 这一事实有利于其在肝细胞内的渗透,经 H2O2 处理的 C-9 肝细胞的 Caspase-3/7 表达减少,表明其具有抑制细胞凋亡的能力。
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Glycyrrhizic Acid Formulated in Hydrotalcite Nanocarriers Intended to Act as a Hepatoprotective Agent.

The article focuses on preparing a nanoformulation based on hydrotalcite and glycyrrhizic acid (GA), seeking a hepatoprotective effect. For this purpose, hydrotalcite-GA formulations were prepared by varying the following conditions to obtain optimal systems in terms of size and PDI (the lowest values), and Z potential (the highest values): (i) type of hydrotalcite (obtained by co-precipitation or calcined hydrotalcite); method used (ultrasound or high shear stirring), and (iii) type of stabilizer (Tween®80 or Pluronic® F-127). The best results were obtained using hydrotalcite obtained by co-precipitation, with high shear stirring and adding a stabilizer, either Tween®80 (HT-T80-GA: mean particle size = 315 nm, PDI = 0.18, Z potential = -20.93) or Pluronic® F-127 (HT-PF127-GA: mean particle size = 307 nm; PDI = 0.27, Z potential = -21.03). After stability studies, the HT-T80-GA formulation was chosen to study antioxidant activity, cytotoxicity, and intracellular penetration capacity. Although the hepatoprotective effect of GA in solution allowed a high viability and antioxidant activity, the fact of including GA in the HT-T80-GA formulation favored its penetration into hepatocytes, with a decrease in Caspase-3/7 expression of C-9 hepatocyte cells treated with H2O2, suggesting the capacity to inhibit apoptosis.

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来源期刊
AAPS Journal
AAPS Journal 医学-药学
CiteScore
7.80
自引率
4.40%
发文量
109
审稿时长
1 months
期刊介绍: The AAPS Journal, an official journal of the American Association of Pharmaceutical Scientists (AAPS), publishes novel and significant findings in the various areas of pharmaceutical sciences impacting human and veterinary therapeutics, including: · Drug Design and Discovery · Pharmaceutical Biotechnology · Biopharmaceutics, Formulation, and Drug Delivery · Metabolism and Transport · Pharmacokinetics, Pharmacodynamics, and Pharmacometrics · Translational Research · Clinical Evaluations and Therapeutic Outcomes · Regulatory Science We invite submissions under the following article types: · Original Research Articles · Reviews and Mini-reviews · White Papers, Commentaries, and Editorials · Meeting Reports · Brief/Technical Reports and Rapid Communications · Regulatory Notes · Tutorials · Protocols in the Pharmaceutical Sciences In addition, The AAPS Journal publishes themes, organized by guest editors, which are focused on particular areas of current interest to our field.
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