Ghodke Shraddha S, Taylor K M G, Somavarapu Satyanarayana
Department of Pharmaceutics, UCL School of Pharmacy, London, UK.
J Microencapsul. 2025 Aug;42(5):459-471. doi: 10.1080/02652048.2025.2495246. Epub 2025 May 5.
A spray-dried DPI formulation was developed to enhance solubility, stability, and pulmonary delivery of curcumin-loaded CS-HA dual-coated micelles for lung cancer therapy. Curcumin was encapsulated in Pluronic F68 micelles via thin-film hydration and coated with CS-HA to improve colloidal stability and cellular interaction. The micellar suspension was spray-dried using lactose and L-leucine as dispersibility enhancers. Formulation characterisation was conducted using DLS to determine mean diameter and PDI, zeta potential analysis, and HPLC for drug loading and encapsulation efficiency, along with TEM. Spray-dried formulations were further characterised by SEM, laser diffraction (Sympatec), FTIR, and XRPD. aerosol characterisation was performed using NGI. The micelles exhibited a mean diameter of 209 nm, PDI of 0.21, zeta potential of -14 mV, encapsulation efficiency of 50-90%, and loading capacity of 5.6% (w/w). XRPD and FTIR confirmed amorphous conversion and stability. The optimized DPI showed favourable aerodynamic properties for targeted pulmonary delivery in NSCLC.
开发了一种喷雾干燥的干粉吸入剂（DPI）制剂，以提高用于肺癌治疗的载姜黄素的壳聚糖-透明质酸（CS-HA）双涂层胶束的溶解度、稳定性和肺部递送效果。通过薄膜水化法将姜黄素包封在普朗尼克F68胶束中，并用CS-HA进行包衣，以提高胶体稳定性和细胞相互作用。使用乳糖和L-亮氨酸作为分散性增强剂对胶束悬浮液进行喷雾干燥。使用动态光散射（DLS）来测定平均直径和多分散指数（PDI）、zeta电位分析以及用于药物负载和包封率的高效液相色谱（HPLC），同时结合透射电子显微镜（TEM）对制剂进行表征。通过扫描电子显微镜（SEM）、激光衍射（Sympatec）、傅里叶变换红外光谱（FTIR）和X射线粉末衍射（XRPD）对喷雾干燥制剂进行进一步表征。使用下一代撞击器（NGI）进行气溶胶表征。胶束的平均直径为209 nm，PDI为0.21，zeta电位为-14 mV，包封率为50-90%，负载量为5.6%（w/w）。XRPD和FTIR证实了无定形转化和稳定性。优化后的DPI对非小细胞肺癌（NSCLC）的靶向肺部递送显示出良好的空气动力学特性。
