Yousfan Amal, Rubio Noelia, Natouf Abdul Hakim, Daher Aamal, Al-Kafry Nedal, Venner Kerrie, Kafa Houmam
Department of Pharmaceutics and Pharmaceutical Technology, Pharmacy Collage, Damascus University Syria.
Department of Chemistry and Materials, Imperial College London London SW7 2AZ UK.
RSC Adv. 2020 Aug 5;10(48):28992-29009. doi: 10.1039/d0ra04890a. eCollection 2020 Aug 3.
The use of nanoparticles (NPs) for intranasal (IN) drug delivery to the brain represents a hopeful strategy to enhance brain targeting of anti-epileptic drugs. In the present work, chitosan-lecithin NPs loaded with phenytoin (PHT), were prepared using the nano-precipitation method. The spherical nature of the NPs and their stability were confirmed using scanning and transmission electron microscopy, while the average dynamic size and zeta potential were measured using dynamic light scattering. The encapsulation efficiency of PHT was higher than 60% for all prepared NPs. Release studies showed that the amount of released PHT was directly related to the amount of chitosan used. The optimum preparation, LC was administered the IN route, and the levels of PHT in the brain were measured in three-time points. Two experimental controls were given the intraperitoneal (IP) and IN routes. The highest PHT amount reaching 1.01 ± 0.55% for LC , which was associated with a sustained release of PHT. These preliminary findings show that the IN delivery of PHT-loaded NPs is very promising for managing epilepsy. The direct nose-to-brain approach increases the safety margins of PHT, while the sustained release could improve patient compliance in a clinical setting.
使用纳米颗粒（NPs）经鼻内（IN）给药至脑是增强抗癫痫药物脑靶向性的一种有前景的策略。在本研究中，采用纳米沉淀法制备了负载苯妥英（PHT）的壳聚糖 - 卵磷脂纳米颗粒。使用扫描和透射电子显微镜确认了纳米颗粒的球形性质及其稳定性，同时使用动态光散射测量了平均动态尺寸和zeta电位。所有制备的纳米颗粒中PHT的包封率均高于60%。释放研究表明，释放的PHT量与壳聚糖的用量直接相关。将最佳制剂LC经鼻内途径给药，并在三个时间点测量脑中PHT的水平。设置了两个实验对照，分别经腹腔内（IP）和鼻内途径给药。LC组中到达脑内的PHT最高量为1.01±0.55%，这与PHT的持续释放相关。这些初步研究结果表明，经鼻内递送负载PHT的纳米颗粒在治疗癫痫方面非常有前景。直接的鼻至脑途径提高了PHT的安全边际，而持续释放可改善临床环境中患者的依从性。
