Wei Hanmei, Lai Sisi, Wei Jiabao, Yang Lei, Jiang Ning, Wang Qing, Yu Yang
School of Chinese Materia Medical, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
J Nanosci Nanotechnol. 2018 Aug 1;18(8):5274-5282. doi: 10.1166/jnn.2018.15371.
The blood-brain barrier (BBB) restricts the delivery of most drugs to the brain. In our previous study, the feasibility of cyclovirobuxine D delivery to the brain by a non-invasive nasal route was evaluated. In this study, a suitable drug delivery system by way of intranasal administration was developed, which could improve brain targeting. First, a formulation of cyclovirobuxine D (CVB-D) based on chitosan nanoparticles (CS-CVB-D-NPs) was prepared by the modified ionotropic gelation method through single-factor screening experiment. The CS-CVB-D-NPs with a entrapment efficiency (EE) of (62.82±2.59)% were found to be of a narrow polydispersity index (PI) (0.19±0.01) and (235.37± 12.71) nm in size, with a zeta potential of (33.9 ± 1.7) mV. The NPs possessed a sustained release characterization with in vitro release of 88.03 ± 2.30% at 24 h. In vivo, the higher AUC0-t(brain) of CS-CVB-D-NPs by intranasal administration revealed the development of a novel brain-targeting delivery method of CVB-D.
血脑屏障（BBB）限制了大多数药物进入大脑。在我们之前的研究中，评估了环维黄杨星D通过非侵入性鼻腔途径进入大脑的可行性。在本研究中，开发了一种通过鼻腔给药的合适药物递送系统，该系统可以改善脑靶向性。首先，通过单因素筛选实验，采用改良的离子凝胶法制备了基于壳聚糖纳米粒（CS-CVB-D-NPs）的环维黄杨星D制剂。发现包封率（EE）为（62.82±2.59）%的CS-CVB-D-NPs具有窄的多分散指数（PI）（0.19±0.01），粒径为（235.37±12.71）nm，zeta电位为（33.9±1.7）mV。这些纳米粒具有缓释特性，24小时体外释放率为88.03±2.30%。在体内，鼻腔给药的CS-CVB-D-NPs具有更高的AUC0-t（脑），这表明开发了一种新型的环维黄杨星D脑靶向递送方法。
