Pitolisant nanofibers: A promising frontier in drug delivery for narcolepsy - Formulation, optimisation, and characterization insights

J. Nandhini , E. Karthikeyan , C. Jegatheshwaran , K. Vignesh , G. Muthuboopathi , S. Rajeshkumar
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Abstract

The study focuses on developing a new way to deliver the narcolepsy medication pitolisant. Electrospinning was used to make polyvinyl alcohol (PVA) and hyperbranched polyglycerol (HPG) polymers into pitolisant nanofibers (PT-NF). A design expert created the best formulation to optimise the process variables like applied voltage, distance, and feed rate. The nanofibers were characterised using scanning electron microscopy, X-ray diffraction, FT-IR, entrapment efficiency, and in-vitro drug release studies. Results showed that the optimal PT-NF formulation had an average diameter of 172 ​nm with an entrapment efficacy of 95 ​% and 92 ​% drug release within 45 ​min. HPG polymer was included in the optimised formulation, whose average fibre diameter was 118 ​nm with 98 ​% entrapment efficacy and 98 ​± ​2 ​% drug release within 30 ​min. These findings strongly suggest that PT nanofibers hold substantial promise as a viable alternative to conventional solid dosage forms for brain-targeted administration, especially when administered via a transdermal patch to a patient during sleep.

Abstract Image

抗缩纳米纤维:治疗发作性睡病的前沿药物——配方、优化和特性分析
这项研究的重点是开发一种新的方法来提供发作性睡病药物。采用静电纺丝法将聚乙烯醇(PVA)和超支化聚甘油(HPG)聚合物制备成抗压纳米纤维(PT-NF)。设计专家创造了最佳配方,以优化过程变量,如施加电压,距离和进给速度。利用扫描电子显微镜、x射线衍射、红外光谱、包封效率和体外药物释放研究对纳米纤维进行了表征。结果表明,最佳PT-NF配方的平均粒径为172 nm,包封率为95%,45 min内释药92%。优化后的配方采用HPG聚合物,其平均纤维直径为118 nm,包封率为98%,30 min内释药率为98±2%。这些发现有力地表明,PT纳米纤维作为一种可行的替代传统固体剂型用于脑靶向给药,尤其是在患者睡眠时通过透皮贴片给药。
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