Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey.
Department of Medical Pharmacology, Faculty of Medicine, Usak University, Usak, Turkey.
Drug Dev Ind Pharm. 2020 Jul;46(7):1063-1072. doi: 10.1080/03639045.2020.1769127. Epub 2020 May 27.
The aim of this study was to develop the PLGA nanoparticles (NPs) containing carbamazepine (CBZ) and levetiracetam (LEV) combination (CBZ + LEV) for the treatment of epilepsy and to characterize the prepared NPs. LEV and CBZ, which are antiepileptic drugs, are used in the treatment of epilepsy. Nano-sized formulations are prepared to use for different purposes such as to improve the solubility/the physicochemical properties and bioavailability of drugs, to decrease their doses and frequency of administration, and to reduce side effects of drugs. CBZ + LEV-PLGA-NPs were prepared by a modified nanoprecipitation method and and characterized. Also, the antiepileptic effect of the NPs was evaluated in a rat epilepsy model. The mean particle size and zeta potential of CBZ + LEV-PLGA-NPs were 180.62 ± 6.260 nm and -27.08 ± 3.110 mV, respectively. The values of encapsulation efficiency (EE%) of CBZ and LEV were 51.00 ± 5.944% and 2.05 ± 0.367%, respectively. CBZ showed a biphasic release profile with initial burst release followed by a sustained release. Ninety percent of CBZ was released from NPs within two days; however, % LEV release from NPs reached about 80% within 30 min. Our results showed that a decrease in seizure scores in the group treated with CBZ + LEV was observed and also, CBZ + LEV and CBZ + LEV-PLGA-NPs had similar antiepileptic activity. The NPs containing CBZ + LEV might be beneficial in the treatment of epilepsy.
本研究旨在开发载有卡马西平(CBZ)和左乙拉西坦(LEV)组合(CBZ+LEV)的 PLGA 纳米粒子(NPs)用于治疗癫痫,并对制备的 NPs 进行表征。LEV 和 CBZ 是抗癫痫药物,用于治疗癫痫。纳米级制剂的制备用于不同的目的,例如提高药物的溶解度/物理化学性质和生物利用度,减少药物的剂量和给药频率,并降低药物的副作用。通过改进的纳米沉淀法制备 CBZ+LEV-PLGA-NPs,并对其进行表征。还在大鼠癫痫模型中评估了 NPs 的抗癫痫作用。CBZ+LEV-PLGA-NPs 的平均粒径和 Zeta 电位分别为 180.62±6.260nm 和-27.08±3.110mV。CBZ 和 LEV 的包封效率(EE%)分别为 51.00±5.944%和 2.05±0.367%。CBZ 呈现出两相释放曲线,初始突释后持续释放。90%的 CBZ 在两天内从 NPs 中释放出来;然而,NPs 中 LEV 的释放百分比在 30 分钟内达到约 80%。我们的结果表明,CBZ+LEV 治疗组的癫痫发作评分降低,并且 CBZ+LEV 和 CBZ+LEV-PLGA-NPs 具有相似的抗癫痫活性。载有 CBZ+LEV 的 NPs 可能有益于治疗癫痫。