载昆诺酸的环糊精纳米海绵的增溶能力、抗氧化活性和细胞毒性研究评价。
Evaluation of solubility enhancement, antioxidant activity, and cytotoxicity studies of kynurenic acid loaded cyclodextrin nanosponge.
机构信息
Department of Chemistry, University of Torino, via P. Giuria 7, 10125, Torino, Italy.
Department of Drug Science and Technology, University of Torino, via P. Giuria 9, 10125, Torino, Italy.
出版信息
Carbohydr Polym. 2019 Nov 15;224:115168. doi: 10.1016/j.carbpol.2019.115168. Epub 2019 Aug 5.
Kynurenic acid demonstrates antioxidant, neuroprotective and free radical scavenging properties. However, low aqueous solubility of kynurenic acid limits its therapeutic activity. In the present study, cyclodextrin nanosponges were used to improve the solubility and therapeutic activity of kynurenic acid. The formation of kynurenic acid loaded nanosponge was confirmed by different characterization techniques. The solubility of kynurenic acid was significantly increased with nanosponge (111.1 μg/ml) compared to free kynurenic acid (16.4 μg/ml) and β-cyclodextrin (28.6 μg/ml). High drug loading (19.06%) and encapsulation efficiency (95.31%) were achieved with NS. The particle size and zeta potential of kynurenic acid loaded nanosponge was around 255.8 nm and -23 mV respectively. Moreover, higher solubilization of kynurenic acid loaded nanosponge produced better antioxidant activity compared to free kynurenic acid. The kynurenic acid loaded nanosponge and blank nanosponge were found nontoxic in the cytotoxicity assay. Thus, these studies demonstrated that nanosponges can be used as a carrier for the delivery of kynurenic acid.
犬尿酸具有抗氧化、神经保护和清除自由基的特性。然而，犬尿酸的低水溶性限制了其治疗活性。在本研究中，使用环糊精纳米海绵来提高犬尿酸的溶解度和治疗活性。通过不同的表征技术证实了犬尿酸负载纳米海绵的形成。与游离犬尿酸（16.4μg/ml）和β-环糊精（28.6μg/ml）相比，犬尿酸纳米海绵的溶解度显著增加（111.1μg/ml）。NS 实现了高载药量（19.06%）和包封效率（95.31%）。犬尿酸负载纳米海绵的粒径和 Zeta 电位分别约为 255.8nm 和-23mV。此外，犬尿酸负载纳米海绵的更高溶解度产生了比游离犬尿酸更好的抗氧化活性。犬尿酸负载纳米海绵和空白纳米海绵在细胞毒性测定中被发现无毒性。因此，这些研究表明纳米海绵可用作犬尿酸的递送载体。
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