通过基于蓝顶土的纳米杂化物来改善Riparin-A的溶解性。
Improving Riparin-A Dissolution through a Laponite Based Nanohybrid.
发表日期:2023 Aug 14
作者:
Duanne Mendes Gomes, Lyghia Maria Araújo Meirelles, Paulo Monteiro Araujo, Rayran Walter Ramos de Sousa, Paulo Michel Pinheiro Ferreira, Stanley Juan Chavez Gutierrez, Maria das Graças Freire de Medeiros, Fernanda Nervo Raffin
来源:
ANTIOXIDANTS & REDOX SIGNALING
摘要:
(1) 背景:Riparin-A已被证明具有多种药理活性,如抗微生物调节剂、抗利什曼病、抗焦虑、抗炎、抗痛和抗氧化作用。尽管具有重要的生物活性效应,但由于其在水中的溶解度低,使其在生物体液中的溶解受到限制。因此,本研究的目的是基于Riparin-A和莱蓬石的纳米杂化体系,以获得更好的溶解特性并评估其细胞毒性潜力。(2) 方法:通过X射线粉末衍射、红外光谱和热分析突出了复合体系的形成。进行了溶解度、溶解度和细胞毒性研究;(3) 结果:在粘土存在下观察到Riparin-A的溶解度和水溶解速率的增加。杂化体系的衍射分析表明了Riparin-A的非晶化,热分析表明与粘土相互作用后Riparin-A的分解和熔化过程的减弱。此外,纳米体系在正常和肿瘤细胞株上没有显示出细胞毒性活性。(4) 结论:这些结果对于开发Riparin-A/莱蓬石纳米体系用于治疗目的具有前景,表明该生物活性化合物的给药途径和生物利用度的可能性增加。
(1) Background: Riparin-A presents several pharmacological activities already elucidated, such as antimicrobial modulator, antileishmania, anxiolytic, anti-inflammatory, antinociceptive, and antioxidant. Even with important bioactive effects, the applicability of Riparin-A is limited due to its low solubility in water, impairing its dissolution in biological fluids. Thus, the objective of this study was to develop a nanohybrid based on Riparin-A and Laponite to obtain a better dissolution profile and evaluate its cytotoxic potential. (2) Methods: The formation of a hybrid system was highlighted by X-ray powder diffraction, infrared spectroscopy, and thermal analysis. Solubility, dissolution, and cytotoxicity studies were performed; (3) Results: An increase in the solubility and aqueous dissolution rate of Riparin-A was observed in the presence of clay. Diffractometric analysis of the hybrid system suggests the amorphization of Riparin-A, and thermal analyses indicated attenuation of decomposition and melting of the Riparin-A after interaction with clay. Furthermore, the nanosystem did not exhibit cytotoxic activity on normal and tumorigenic lines. (4) Conclusions: These results are promising for the development of the Riparin-A/Laponite nanosystem for therapeutic purposes, suggesting an increase in the range of possible routes of administration and bioavailability of this bioactive compound.