تحضير و توصيف جسيمات الكيتوزان النانوية المحملة بمادتي الكورسيتين و الفنتوئين لتعزيز التوصيل الدماغي لمادة الفنتوئين التابع للتجريع الأنفي عند فئران فصيلة Balb-c

الملخص EN

The use of nanoparticles in brain drug delivery following the nasal adminstration is an important strategy to enhance the brain targeting of antiepileptic drug.

On the other hand, co-adminstration of glycoprotein P inhibitors aims to increase the brain therapeutic concentration of antiepileptic drug in refractory epilepsy.

In our work, chitosan and lecithin nanoparticles loaded both phenytoin as an antiepileptic drug and quercetin as a glycoprotein P-inhibitor flavonoid were prepared using the nano precipitation method.

The spherical shape of the prepared particles was confirmed using scanning electron microscope, while a dynamic light scattering was used to measure the diameter and surface charge of the prepared particles.

The encapsulation efficiency was 60% for each of the two drugs, which showed sustained release from prepared particles using the dialysis method.

The nanoparticles particles were administered intranasally in Balb / c mice, and the amount of phenytoin was measured in the brain parenchyma, capillaries, and plasma.

The peritoneal delivery of phenytoin solution was used as a positive control for the experiment.

The results were also compared with the brain ratios after the administration of phenytoin with verapamil as a standard P-GP inhibitor and with quercetin as the tested flavonoid in this study.

The results showed that the highest concentrations of phenytoin in the brain parenchyma was detected following intranasal administration of nanoparticles loaded with phenytoin and quercetin, reaching 9.7 ± 1.44% of the administered dose relative to the weight of the studied organ.

Data showed that nasal delivery of nanoparticles loaded with phenytoin and quercetin is considered as a promising system, as it increases the safety and reduces side effects related to the limited drug concentrations in the systemic blood circulation and their high in the brain.

On the other hand, the sustained release could improve patient compliance in a clinical setting.