Lamotrigine is used for neurological disorders and antiepileptic therapy at frequent dosing due to its poor solubility. The present work aims to study the influence of combining the Lamotrigine nanoparticles and polymer composite oral dissolving film to improve the solubility and dissolution kinetics of the drug. The Lamotrigine-Eudragit E100 nanoparticles were synthesized through solvent evaporation followed by precipitation process, which were laden in oral dissolving films through solvent casting technique. The optimized nanoparticles were assessed for particle size, colloidal stability, drug entrapment efficiency, in vitro release profile, physicochemical characteristics, and cytotoxicity. The optimized polymeric nanoparticles of Lamotrigine: Eudragit E100 (1:0.5) exhibited monodispersed particles with 103 nm average size, +7.96 mV zeta potential, and 82.96% ± 1.2% entrapment efficiency. The composite oral matrix films blended with polyvinyl alcohol and polyvinyl pyrrolidone (0.5:0.5 ratio) incorporated with the polymeric nanoparticles demonstrated >64% drug release within 2 h. The nanoparticles and its composite films exhibited 9- and 11-fold higher drug release than pure drug, respectively. The analytical characterization studies proved the formation of nanoparticles with mild drug–polymer interactions and optimum stability, which resulted in enhanced solubility and dissolution of drug. The nanoparticles displayed lesser cytotoxicity to the normal (Vero) cells at concentration of 10–50 μg/mL compared to pure drug. The optimized polymeric nanoparticle loaded oral films could be suitable for in vivo administration of Lamotrigine at low doses to improve bioavailability and therapeutic efficiency with reduced side effects.

中文翻译：

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拉莫三嗪纳米颗粒负载聚合物复合口腔溶解膜，用于提高疏水性抗癫痫分子的治疗潜力

拉莫三嗪因其溶解性差而经常用于神经系统疾病和抗癫痫治疗。本工作旨在研究拉莫三嗪纳米粒与聚合物复合口腔溶出膜相结合对改善药物溶解度和溶出动力学的影响。Lamotrigine-Eudragit E100 纳米颗粒是通过溶剂蒸发和沉淀过程合成的，通过溶剂浇铸技术将其装入口腔溶解膜中。对优化后的纳米颗粒进行了粒径、胶体稳定性、药物包封率、体外评估释放曲线、理化特性和细胞毒性。拉莫三嗪的优化聚合物纳米颗粒：Eudragit E100 (1:0.5) 表现出平均尺寸为 103 nm、+7.96 mV zeta 电位和 82.96% ± 1.2% 截留效率的单分散颗粒。与聚乙烯醇和聚乙烯吡咯烷酮（0.5:0.5 比例）混合的复合口腔基质膜与聚合物纳米颗粒混合，在 2 小时内表现出>64% 的药物释放。纳米颗粒及其复合膜的药物释放分别比纯药物高 9 倍和 11 倍。分析表征研究证明纳米颗粒的形成具有温和的药物-聚合物相互作用和最佳稳定性，从而提高了药物的溶解度和溶出度。与纯药物相比，纳米颗粒在 10–50 μg/mL 的浓度下对正常 (Vero) 细胞显示出较小的细胞毒性。优化的聚合物纳米颗粒负载口腔膜可适用于以低剂量在体内给药拉莫三嗪，以提高生物利用度和治疗效率，同时减少副作用。