Dattani Shradha, Li Xiaoling, Lampa Charina, Barriscale Amanda, Damadzadeh Behzad, Lechuga-Ballesteros David, Jasti Bhaskara R
Department of Pharmaceutics and Medicinal Chemistry, University of the Pacific, Stockton, CA 95211, USA.
Inhalation Product Development, PT&D AstraZeneca, LLC, South San Francisco, CA 94080, USA.
Pharmaceutics. 2025 Jan 17;17(1):122. doi: 10.3390/pharmaceutics17010122.
Micelles, liposomes, and solid lipid nanoparticles (SLNs) are promising drug delivery vehicles; however, poor aqueous stability requires post-processing drying methods for maintaining long-term stability. The objective of this study was to compare the potential of lipid-based micelles, liposomes, and SLNs for producing stable re-dispersible spray-dried powders with trehalose or a combination of trehalose and L-leucine. This study provides novel insights into the implementation of spray drying as a technique to enhance long-term stability for these lipid-based nanocarriers. Aqueous dispersions of LDV-targeted micelles, liposomes, and SLNs loaded with paclitaxel (PTX) were converted into re-dispersible powders using spray drying. The physicochemical properties of the nanocarriers were determined via scanning electron microscopy (SEM), Karl Fischer titration, differential scanning calorimetry (DSC), and dynamic light scattering (DLS). Short-term stability of all nanocarrier formulations was compared by measuring particle size, polydispersity index (PDI), and paclitaxel retention over 7 days at room temperature and at 4 °C. Paclitaxel-loaded micelles, liposomes, and SLN formulations were successfully converted into well-dispersed spray-dried powders with acceptable yields (71.5 to 83.5%), low moisture content (<2%), and high transition temperatures (95.1 to 100.8 °C). SEM images revealed differences in morphology, where nanocarriers spray-dried with trehalose or a combination of trehalose and L-leucine produced smooth or corrugated particle surfaces, respectively. Reconstituted spray-dried nanocarriers maintained their nanosize and paclitaxel content over 7 days at 4 °C. The results of this study demonstrate the potential for the development of spray-dried lipid-based nanocarriers for long-term stability.
胶束、脂质体和固体脂质纳米粒（SLNs）是很有前景的药物递送载体；然而，较差的水稳定性需要采用后处理干燥方法来维持长期稳定性。本研究的目的是比较基于脂质的胶束、脂质体和SLNs在与海藻糖或海藻糖和L-亮氨酸组合使用时制备稳定的可再分散喷雾干燥粉末的潜力。本研究为将喷雾干燥作为一种增强这些基于脂质的纳米载体长期稳定性的技术的实施提供了新的见解。使用喷雾干燥将负载紫杉醇（PTX）的靶向LDV的胶束、脂质体和SLNs的水分散体转化为可再分散粉末。通过扫描电子显微镜（SEM）、卡尔费休滴定法、差示扫描量热法（DSC）和动态光散射（DLS）测定纳米载体的物理化学性质。通过在室温及4℃下测量7天内的粒径、多分散指数（PDI）和紫杉醇保留率，比较了所有纳米载体制剂的短期稳定性。负载紫杉醇的胶束、脂质体和SLN制剂成功转化为分散良好的喷雾干燥粉末，产率可接受（71.5%至83.5%），水分含量低（<2%），转变温度高（95.1至100.8℃）。SEM图像显示了形态上的差异，其中用海藻糖或海藻糖和L-亮氨酸组合喷雾干燥的纳米载体分别产生了光滑或有波纹的颗粒表面。重构的喷雾干燥纳米载体在4℃下7天内保持其纳米尺寸和紫杉醇含量。本研究结果证明了开发用于长期稳定性的喷雾干燥脂质基纳米载体的潜力。
