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载卡马西平及左乙拉西坦的 PLGA 纳米粒的制备及其评价

Carbamazepine and levetiracetam-loaded PLGA nanoparticles prepared by nanoprecipitation method: and studies.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey.

Department of Medical Pharmacology, Faculty of Medicine, Usak University, Usak, Turkey.

出版信息

Drug Dev Ind Pharm. 2020 Jul;46(7):1063-1072. doi: 10.1080/03639045.2020.1769127. Epub 2020 May 27.

Abstract

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.

摘要

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。

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