Gomes Duanne Mendes, Meirelles Lyghia Maria Araújo, Araujo Paulo Monteiro, de Sousa Rayran Walter Ramos, Ferreira Paulo Michel Pinheiro, Gutierrez Stanley Juan Chavez, de Medeiros Maria das Graças Freire, Raffin Fernanda Nervo
Post Program on Pharmaceutical Sciences, Federal University of Piauí-UFPI, Teresina 64049-550, Piauí, Brazil.
Department of Pharmacy, Federal University of Piauí-UFPI, Teresina 64049-550, Piauí, Brazil.
Pharmaceutics. 2023 Aug 14;15(8):2136. doi: 10.3390/pharmaceutics15082136.
(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.
(1) 背景：瑞帕林 - A已展现出多种药理活性，如抗菌调节剂、抗利什曼原虫、抗焦虑、抗炎、抗伤害感受和抗氧化活性。即便具有重要的生物活性效应，但由于瑞帕林 - A在水中溶解度低，影响其在生物流体中的溶解，其应用受到限制。因此，本研究的目的是开发一种基于瑞帕林 - A和锂皂石的纳米杂化物，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杂化体系的形成。进行了溶解度、溶解和细胞毒性研究；(3) 结果：在存在黏土的情况下，观察到瑞帕林 - A的溶解度和水溶解速率增加。杂化体系的衍射分析表明瑞帕林 - A发生了非晶化，热分析表明瑞帕林 - A与黏土相互作用后分解和熔化减弱。此外，该纳米体系对正常细胞系和致瘤细胞系均未表现出细胞毒性活性。(4) 结论：这些结果对于开发用于治疗目的的瑞帕林 - A/锂皂石纳米体系很有前景，表明该生物活性化合物可能的给药途径范围和生物利用度有所增加。
