Laboratorio de Investigación y Posgrado en Tecnología Farmacéutica (L-322), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de México, Av. 1 de Mayo S/N, Cuautitlán Izcalli, CP 54740, Edo. de Méx, México.
Laboratorio de Fisicoquímica y Reactividad de Superficies (LaFReS), Instituto de Investigaciones en Materiales, Universidad Nacional Autónoma de México, Circuito Exterior S/N, Cd. Universitaria, Del. Coyoacán, CP 04510, Ciudad de Mexico, México.
AAPS J. 2024 Nov 19;27(1):2. doi: 10.1208/s12248-024-00986-8.
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 HO, suggesting the capacity to inhibit apoptosis.
这篇文章主要关注的是制备基于水滑石和甘草酸(GA)的纳米制剂,以寻求其肝保护作用。为此,通过改变以下条件来制备水滑石-GA 制剂,以获得在尺寸和 PDI(最低值)以及 Z 电位(最高值)方面具有最佳性能的体系:(i)水滑石的类型(通过共沉淀或煅烧水滑石获得);所使用的方法(超声或高剪切搅拌)和(iii)稳定剂的类型(Tween®80 或 Pluronic® F-127)。使用共沉淀法获得的水滑石、高剪切搅拌并添加稳定剂(Tween®80 或 Pluronic® F-127)时,得到的结果最好,即 Tween®80(HT-T80-GA:平均粒径=315nm,PDI=0.18,Z 电位=-20.93)或 Pluronic® F-127(HT-PF127-GA:平均粒径=307nm;PDI=0.27,Z 电位=-21.03)。在进行稳定性研究后,选择 HT-T80-GA 制剂来研究其抗氧化活性、细胞毒性和细胞内穿透能力。虽然 GA 在溶液中的肝保护作用可以使细胞保持高活力和抗氧化活性,但将 GA 包含在 HT-T80-GA 制剂中的事实有利于其穿透肝细胞,降低 HO 处理的 C-9 肝细胞中 Caspase-3/7 的表达,表明其抑制细胞凋亡的能力。