用于治疗肝细胞癌的希波龙负载脂质纳米胶囊:与固体脂质纳米颗粒和悬浮液的比较研究。

Nabil K Alruwaili, Waleed H Almalki, Salem Salman Almujri, Abdulrahman Alhamyani, Abdulaziz Alzahrani, Alhussain Aodah, Majed Alrobaian, Tanuja Singh, Farhan Jalees Ahmad, Anjali Singh, Jonathan A Lal, Mahfoozur Rahman
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引用次数: 0

摘要

目的:本研究旨在开发、优化和评估肝宝隆(HPN)脂质纳米胶囊(LNCs)、固体脂质纳米颗粒(SLNs)和悬浮液,用于治疗肝细胞癌(HCC):包括UPLC-MS/MS、溶解度、优化、表征、稳定性、体外和体内研究:结果:采用相位转换和温度循环法研制出了HPN负载的LNCs,而采用热均质法和三次饱和法研制出了SLNs和悬浮液。HPN-LNCs 的粒径(PS)为 196.9 nm,PDI 为 0.315,zeta 电位为 -24.3 mV。HPN-S2 的 PS 值为 199.90 nm,PDI 为 0.381,zeta 电位为 -19.1 mV。HPN-SPN3 的 PS 值为 946.60 nm,PDI 值为 0.31,zeta 电位为-0.1945 mV。3 个月的稳定性测试和在不同介质中的胃稳定性测试表明,PS、PDI、包埋效率(EE)和负载能力(LC)均无明显变化。HPN-LNCs在25小时内的药物持续释放率为96.22%,优于HPN-S2(87.12%)和HPN-SPN3(22%在2小时内释放)。与 HPN-S2 和 HPN-SPN3 相比,HPN 负载 LNCs 的口服生物利用度提高了 2.03 倍,具有最有效的保肝作用,在肝脏肿瘤中的定位也更高:结论:HPN负载型LNCs的结果很有希望,但未来需要更多的安全性数据。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Hispolon-loaded lipid nanocapsules for the management of hepatocellular carcinoma: comparative study with solid lipid nanoparticles and suspension.

Aim: The present study aims to develop, optimize and assess hispolon (HPN) lipid nanocapsules (LNCs), solid lipid nanoparticles (SLNs) and suspension for treating hepatocellular carcinoma (HCC).Materials & methods: It included UPLC-MS/MS, solubility, optimization, characterization, stability, in vitro and in vivo studies.Results: HPN-loaded LNCs were developed using phase-inversion and temperature cycling, while SLNs and suspension using hot homogenization and trituration methods. HPN-LNCs had a particle size (PS) of 196.9 nm, a PDI of 0.315 and a zeta potential of -24.3 mV. HPN-S2 had a PS of 199.90 nm, a PDI of 0.381 and a zeta potential of -19.1 mV. HPN-SPN3 showed a PS of 946.60 nm, a PDI of 0.31 and a zeta potential of -0.1945 mV. Stability tests over 3 months and gastric stability testing in different media showed no significant changes in PS, PDI, entrapment efficiency (EE) and loading capacity (LC). HPN-LNCs demonstrated 96.22% sustained drug release over 25 h, outperforming HPN-S2 (87.12%) and HPN-SPN3 (22% within 2 h). HPN-loaded LNCs improved oral bioavailability by 2.03-times, the most effective hepatoprotective action and higher localization in liver tumors over HPN-S2 and HPN-SPN3.Conclusion: HPN-Loaded LNCs results are promising, but more safety data needed in the future.

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