Canbolat Fadime, Demir Neslihan, Yayıntas Ozlem Tonguc, Pehlivan Melek, Eldem Aslı, Ayna Tulay Kilicaslan, Senel Mehmet
Department of Pharmacy Services, Vocational School of Health Services, Çanakkale Onsekiz Mart University, Çanakkale 17100, Türkiye.
Faculty of Science, Çanakkale Onsekiz Mart University, Çanakkale 17100, Türkiye.
Biomedicines. 2024 Jan 26;12(2):287. doi: 10.3390/biomedicines12020287.
Multiple drug-delivery systems obtained by loading nanoparticles (NPs) with different drugs that have different physicochemical properties present a promising strategy to achieve synergistic effects between drugs or overcome undesired effects. This study aims to develop a new NP by loading quercetin (Que) and valproic acid (VPA) into chitosan. In this context, our study investigated the antioxidant activities of chitosan NPs loaded with single and dual drugs containing Que against oxidative stress.
The synthesis of chitosan NPs loaded with a single (Que or VPA) and dual drug (Que and VPA), the characterization of the NPs, the conducting of in vitro antioxidant activity studies, and the analysis of the cytotoxicity and antioxidant activity of the NPs in human neuroblastoma SH-SY5Y cell lines were performed.
The NP applications that protected cell viability to the greatest extent against HO-induced cell damage were, in order, 96 µg/mL of Que-loaded chitosan NP (77.30%, 48 h), 2 µg/mL of VPA-loaded chitosan NP (70.06%, 24 h), 96 µg/mL of blank chitosan NP (68.31%, 48 h), and 2 µg/mL of Que- and VPA-loaded chitosan NP (66.03%, 24 h).
Our study establishes a successful paradigm for developing drug-loaded NPs with a uniform and homogeneous distribution of drugs into NPs. Chitosan NPs loaded with both single and dual drugs possessing antioxidant activity were successfully developed. The capability of chitosan NPs developed at the nanometer scale to sustain cell viability in SH-SY5Y cell lines implies the potential of intranasal administration of chitosan NPs for future studies, offering protective effects in central nervous system diseases.
通过将具有不同物理化学性质的不同药物负载到纳米颗粒(NP)中获得的多种药物递送系统,是实现药物间协同作用或克服不良影响的一种有前景的策略。本研究旨在通过将槲皮素(Que)和丙戊酸(VPA)负载到壳聚糖中来开发一种新的纳米颗粒。在此背景下,我们的研究调查了负载单一和含Que的双重药物的壳聚糖纳米颗粒对氧化应激的抗氧化活性。
进行了负载单一(Que或VPA)和双重药物(Que和VPA)的壳聚糖纳米颗粒的合成、纳米颗粒的表征、体外抗氧化活性研究以及纳米颗粒在人神经母细胞瘤SH-SY5Y细胞系中的细胞毒性和抗氧化活性分析。
在抵御HO诱导的细胞损伤方面,对细胞活力保护程度最高的纳米颗粒应用依次为:96μg/mL负载Que的壳聚糖纳米颗粒(77.30%,48小时)、2μg/mL负载VPA的壳聚糖纳米颗粒(70.06%,24小时)、96μg/mL空白壳聚糖纳米颗粒(68.31%,48小时)以及2μg/mL负载Que和VPA的壳聚糖纳米颗粒(66.03%,24小时)。
我们的研究建立了一个成功的范例,用于开发药物在纳米颗粒中均匀分布的载药纳米颗粒。成功开发了负载单一和双重具有抗氧化活性药物的壳聚糖纳米颗粒。在纳米尺度开发的壳聚糖纳米颗粒在SH-SY5Y细胞系中维持细胞活力的能力意味着壳聚糖纳米颗粒鼻内给药在未来研究中的潜力,可为中枢神经系统疾病提供保护作用。