Alruwaili Nabil K, Almalki Waleed H, Almujri Salem Salman, Alhamyani Abdulrahman, Alzahrani Abdulaziz, Aodah Alhussain, Alrobaian Majed, Singh Tanuja, Ahmad Farhan Jalees, Singh Anjali, Lal Jonathan A, Rahman Mahfoozur
Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakakah, Saudi Arabia.
Department of Pharmacology & Toxicology, College of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia.
Nanomedicine (Lond). 2024;19(30):2555-2576. doi: 10.1080/17435889.2024.2406741. Epub 2024 Oct 15.
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). It included UPLC-MS/MS, solubility, optimization, characterization, stability, and studies. 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. HPN-Loaded LNCs results are promising, but more safety data needed in the future.
本研究旨在开发、优化和评估用于治疗肝细胞癌（HCC）的组蛋白（HPN）脂质纳米胶囊（LNCs）、固体脂质纳米粒（SLNs）和混悬液。研究内容包括超高效液相色谱-串联质谱（UPLC-MS/MS）、溶解度、优化、表征、稳定性研究。采用相转化和温度循环法制备了载HPN的LNCs，采用热均质法和研磨法制备了SLNs和混悬液。HPN-LNCs的粒径（PS）为196.9nm，多分散指数（PDI）为0.315，zeta电位为-24.3mV。HPN-S2的PS为199.90nm，PDI为0.381，zeta电位为-19.1mV。HPN-SPN3的PS为946.60nm，PDI为0.31，zeta电位为-0.1945mV。3个月的稳定性试验和在不同介质中的胃稳定性试验表明，PS、PDI、包封率（EE）和载药量（LC）均无显著变化。HPN-LNCs在25小时内实现了96.22%的药物持续释放，优于HPN-S2（87.12%）和HPN-SPN3（2小时内释放22%）。载HPN的LNCs使口服生物利用度提高了2.03倍，具有最有效的肝保护作用，且在肝肿瘤中的定位高于HPN-S2和HPN-SPN3。载HPN的LNCs的结果很有前景，但未来还需要更多的安全性数据。
