Herneisey Michele, Janjic Jelena M
Graduate School of Pharmaceutical Sciences, School of Pharmacy, Duquesne University, Pittsburgh, PA 15282, USA.
Pharmaceutics. 2023 Mar 29;15(4):1103. doi: 10.3390/pharmaceutics15041103.
Perfluorocarbon nanoemulsions (PFC-NEs) are widely used as theranostic nanoformulations with fluorescent dyes commonly incorporated for tracking PFC-NEs in tissues and in cells. Here, we demonstrate that PFC-NE fluorescence can be fully stabilized by controlling their composition and colloidal properties. A quality-by-design (QbD) approach was implemented to evaluate the impact of nanoemulsion composition on colloidal and fluorescence stability. A full factorial, 12-run design of experiments was used to study the impact of hydrocarbon concentration and perfluorocarbon type on nanoemulsion colloidal and fluorescence stability. PFC-NEs were produced with four unique PFCs: perfluorooctyl bromide (PFOB), perfluorodecalin (PFD), perfluoro(polyethylene glycol dimethyl ether) oxide (PFPE), and perfluoro-15-crown-5-ether (PCE). Multiple linear regression modeling (MLR) was used to predict nanoemulsion percent diameter change, polydispersity index (PDI), and percent fluorescence signal loss as a function of PFC type and hydrocarbon content. The optimized PFC-NE was loaded with curcumin, a known natural product with wide therapeutic potential. Through MLR-supported optimization, we identified a fluorescent PFC-NE with stable fluorescence that is unaffected by curcumin, which is known to interfere with fluorescent dyes. The presented work demonstrates the utility of MLR in the development and optimization of fluorescent and theranostic PFC nanoemulsions.
全氟碳纳米乳剂(PFC-NEs)被广泛用作治疗诊断纳米制剂,通常会掺入荧光染料以追踪组织和细胞中的PFC-NEs。在此,我们证明通过控制其组成和胶体性质,可以使PFC-NE荧光完全稳定。采用质量源于设计(QbD)方法来评估纳米乳剂组成对胶体和荧光稳定性的影响。使用全因子12次运行实验设计来研究烃浓度和全氟碳类型对纳米乳剂胶体和荧光稳定性的影响。用四种独特的全氟碳制备PFC-NEs:全氟辛基溴(PFOB)、全氟萘烷(PFD)、全氟(聚乙二醇二甲醚)氧化物(PFPE)和全氟-15-冠-5-醚(PCE)。使用多元线性回归建模(MLR)来预测纳米乳剂直径变化百分比、多分散指数(PDI)以及荧光信号损失百分比作为全氟碳类型和烃含量的函数。优化后的PFC-NE负载了姜黄素,一种具有广泛治疗潜力的已知天然产物。通过MLR支持的优化,我们确定了一种荧光稳定且不受姜黄素影响的荧光PFC-NE,已知姜黄素会干扰荧光染料。所展示的工作证明了MLR在荧光和治疗诊断用PFC纳米乳剂的开发和优化中的实用性。