Mali Alvja, Nayak Navya U, van Doesburg Jessie, Fokkink Remco, van Riessen Koen, de Kruijf Robbin, Srinivas Mangala
Department of Cell Biology and Immunology, Wageningen University & Research, Wageningen 6708WD, The Netherlands.
Department of Agrotechnology and Food Sciences, Physical Chemistry and Soft Matter, Wageningen University, Wageningen 6700 EK, Netherlands.
ACS Omega. 2025 Feb 11;10(7):6768-6779. doi: 10.1021/acsomega.4c08663. eCollection 2025 Feb 25.
Polymeric particles, particularly poly(lactic--glycolic acid) nanoparticles (PLGA NPs), have gained widespread utility in drug delivery, including their incorporation into established clinical formulations. However, their significance is enhanced when loaded with perfluorocarbons (PFCs). This integration enables precise imaging and quantification using advanced techniques such as F nuclear magnetic resonance (NMR) or magnetic resonance imaging. These PFC-loaded nanoparticles offer substantial biomedical advantages, including quantitative cell tracking and trackable drug delivery. It is imperative to develop a stable nanoformulation with well-characterized parameters (size, PDI, and PFC content) to facilitate their translation into clinical trials. Another crucial aspect related to their clinical translation is the need for practical storage conditions that are convenient for clinical handling and long-term storage. This study provides compelling evidence of the exceptional long-term stability of PLGA-PFCE (perfluoro-15-crown-5-ether) NPs synthesized via a single-oil-in-water method. When stored at -20 °C, these NPs exhibit remarkable stability for over 6 years. Furthermore, our investigations extend to the behavior of the NPs in powder and suspension forms, demonstrating resilience even after enduring multiple freeze-thaw cycles. Additionally, we explore their stability under various conditions, including water and culture medium, revealing robustness at 4 °C, room temperature (RT), and 37 °C for up to 30 days.
聚合物颗粒，特别是聚（乳酸-乙醇酸）纳米颗粒（PLGA NPs），在药物递送中已获得广泛应用，包括将它们纳入已有的临床制剂中。然而，当负载全氟化碳（PFCs）时，它们的重要性会增强。这种结合使得能够使用先进技术，如氟核磁共振（NMR）或磁共振成像进行精确成像和定量分析。这些负载PFC的纳米颗粒具有显著的生物医学优势，包括定量细胞追踪和可追踪的药物递送。开发一种具有良好表征参数（尺寸、多分散指数和PFC含量）的稳定纳米制剂，以促进其转化为临床试验是至关重要的。与其临床转化相关的另一个关键方面是需要便于临床操作和长期储存的实用储存条件。本研究提供了令人信服的证据，证明通过单水包油法合成的PLGA-PFCE（全氟-15-冠-5-醚）纳米颗粒具有出色的长期稳定性。当储存在-20°C时，这些纳米颗粒在6年多的时间里表现出显著的稳定性。此外，我们的研究扩展到了纳米颗粒在粉末和悬浮液形式下的行为，证明即使经过多次冻融循环仍具有弹性。此外，我们还探索了它们在各种条件下的稳定性，包括水和培养基，发现在4°C、室温（RT）和37°C下长达30天都具有稳定性。
