Parihar Akshay, Prajapati Bhupendra G, Paliwal Himanshu
Faculty of Pharmacy, Ganpat University, Mehsana, Gujarat, India.
Faculty of Pharmaceutical Sciences, The ICFAI University, Himachal Pradesh, India.
Front Pharmacol. 2025 Aug 20;16:1619481. doi: 10.3389/fphar.2025.1619481. eCollection 2025.
Cystic fibrosis (CF) is a systemic disease which primarily affects pulmonary system, but also extends to different important organs to cause multitude of associated diseases, leading to rise in rate of morbidity and mortality. The present investigation is focused on the development and optimization of SLN (Solid Lipid Nanoparticles) formulation of IVF (Ivacaftor) for effective treatment of cystic fibrosis.
IVF-SLN was formulated with the help of homogenization and ultrasonication methods by incorporating Labrasol as liquid lipid, Cetyl palmitate as solid lipid and Polysorbate 20 as the surfactant. The independent variables such as the amount of Lipid (X) and amount of surfactant (X) were studied for their effect on dependent variables namely entrapment efficiency and particle size.
The final formulation of IVF-SLN showed a narrow range in size distribution with the particle size of 150.23 ± 1.59 nm, PDI of 0.256 ± 0.014 and entrapment efficiency of 90.54 ± 1.32%. IVF incorporation into the imperfect crystal lattice was confirmed with the help of a DSC (Differential Scanning Calorimetry) study. The dissolution study showed improved release pattern from the optimized formulation and release profile followed first-order model indicating a sustained release pattern from lipid matrix.
This delivery system presented development of stable nanoparticle formulation exhibiting sustained release pattern, which may contribute to therapeutic outcomes in comparison with drug alone. The outcomes of the research highlighted its potential as an efficient therapeutic strategy for CF management.
囊性纤维化（CF）是一种全身性疾病，主要影响肺部系统，但也会累及不同重要器官，引发多种相关疾病，导致发病率和死亡率上升。本研究聚焦于开发和优化依伐卡托（Ivacaftor）的固体脂质纳米粒（SLN）制剂，用于有效治疗囊性纤维化。
借助均质化和超声处理方法，以Labrasol作为液体脂质、十六烷基棕榈酸酯作为固体脂质、聚山梨酯20作为表面活性剂来制备依伐卡托固体脂质纳米粒（IVF - SLN）。研究脂质用量（X）和表面活性剂用量（X）等自变量对包封率和粒径等因变量的影响。
IVF - SLN的最终制剂粒径分布范围窄，粒径为150.23±1.59 nm，多分散指数（PDI）为0.256±0.014，包封率为90.54±1.32%。通过差示扫描量热法（DSC）研究证实依伐卡托掺入了不完善的晶格中。溶出度研究表明优化后的制剂具有改善的释放模式，释放曲线符合一级模型，表明从脂质基质中持续释放。
该给药系统呈现出稳定的纳米粒制剂的开发，具有持续释放模式，与单独使用药物相比可能有助于治疗效果。研究结果突出了其作为囊性纤维化管理的有效治疗策略的潜力。
