Aldeeb Mohamed Mahmud E, Wilar Gofarana, Suhandi Cecep, Mohammed Ahmed Fouad Abdelwahab, El-Rayyes Ali, Elamin Khaled M, Wathoni Nasrul
Doctoral Program of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, 45363, Indonesia.
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, 45363, Indonesia.
Int J Nanomedicine. 2025 Apr 27;20:5457-5473. doi: 10.2147/IJN.S511602. eCollection 2025.
This study aimed to develop a nanosuspension formulation of L. folium to enhance its antihyperlipidemic effectiveness by optimizing its particle size, stability, and pharmaceutical availability.
Nanosuspensions were prepared using an antisolvent technique, with Tween 80 as the stabilizing agent. The formulations were characterized by particle size analysis, zeta potential, and polydispersity index (PDI) to evaluate their stability and uniformity. Transmission electron microscopy (TEM) confirmed nanoparticle formation, and stability assessments were conducted over 28 days under refrigerated conditions. In vitro release studies were conducted to assess sustained drug release, and antioxidant activity and lipid-lowering efficacy were compared to those of simvastatin.
The NS-Sa-4:1 formulation exhibited optimal properties, including an average particle size of 12.9 nm, zeta potential of -12.5 mV, and PDI of 0.317, indicating a stable and uniform nanosuspension. TEM images revealed well-dispersed nanoparticles, and stability tests demonstrated the retention of these properties for up to 28 days. In vitro release studies showed sustained drug release, with 92.51% released within 24 h, surpassing the crude extract and other formulations. NS-Sa-4:1 also demonstrated enhanced antioxidant activity and significant lipid-lowering effects compared with simvastatin.
The nanosuspension of L. folium, particularly NS-Sa-4:1, shows significant potential as an effective antihyperlipidemic therapy with improved stability, pharmaceutical availability, and therapeutic efficacy. Future research should focus on pharmacokinetics and in vivo studies to further validate these results.
本研究旨在开发一种番泻叶纳米混悬液制剂，通过优化其粒径、稳定性和药物可利用性来提高其降血脂效果。
采用抗溶剂技术制备纳米混悬液，以吐温80作为稳定剂。通过粒径分析、zeta电位和多分散指数（PDI）对制剂进行表征，以评估其稳定性和均匀性。透射电子显微镜（TEM）证实了纳米颗粒的形成，并在冷藏条件下进行了28天的稳定性评估。进行体外释放研究以评估药物的持续释放，并将抗氧化活性和降脂功效与辛伐他汀进行比较。
NS-Sa-4:1制剂表现出最佳性能，平均粒径为12.9nm，zeta电位为-12.5mV，PDI为0.317，表明该纳米混悬液稳定且均匀。TEM图像显示纳米颗粒分散良好，稳定性测试表明这些性能在长达28天内保持不变。体外释放研究显示药物持续释放，24小时内释放92.51%，超过粗提物和其他制剂。与辛伐他汀相比，NS-Sa-4:1还表现出增强的抗氧化活性和显著的降脂作用。
番泻叶纳米混悬液，特别是NS-Sa-4:1，作为一种有效的降血脂疗法具有显著潜力，具有改善的稳定性、药物可利用性和治疗效果。未来的研究应集中在药代动力学和体内研究，以进一步验证这些结果。
