Patel Priya, Raval Mihir, Airao Vishal, Ali Nemat, Shazly Gamal A, Khan Rehan, Prajapati Bhupendra
Department of Pharmaceutical Sciences, Saurashtra University, Rajkot 360005, Gujarat, India.
Department of Pharmaceutical Sciences, Sardar Patel University, Vallabh Vidya Nagar 388120, Gujarat, India.
ACS Omega. 2024 Feb 24;9(9):10353-10370. doi: 10.1021/acsomega.3c07954. eCollection 2024 Mar 5.
: Targeted delivery of chemotherapeutics by functionalized nanoparticles exhibits a wonderful prospect for cancer treatment. The main objective of this research was to develop folate receptor-targeted silibinin (SB)-loaded inhalable polymeric nanoparticles (FA-CS-SB-NPs) for the treatment of lung cancer. : The qbD approach was implemented to prepare SB-loaded nanoparticles. Folic acid was conjugated by electrostatic conjugation in an optimized batch. The therapeutic potentials of formulations were determined using a lung cancer cell-bearing rat model. : Optimized formulation exhibited a spherical surface with a mean particle size of 275 ± 1.20 nm, a PDI of 0.234 ± 0.07, a ζ-potential of 32.50 ± 0.21, an entrapment efficiency of 75.52 ± 0.87%, and a CDR of 63.25 ± 1.21% at 48 h. Aerodynamic behaviors such as the mass median aerodynamic diameter (MMAD) and geometric size distribution (GSD) were found to be 2.75 ± 1.02 and 3.15 ± 0.88 μm, respectively. After 24 h of incubation with FA-CS-SB-NPs, the IC50 value was found to be 24.5 g/mL. FA-SB-CS-NPs maintained a significantly higher deposition of SB in lung tissues. : Thus, the noninvasive nature and target specificity of FA-CS-SB-NPs pave the way for pulmonary delivery for treating lung cancer.
功能化纳米颗粒对化疗药物的靶向递送在癌症治疗中展现出良好的前景。本研究的主要目的是开发用于治疗肺癌的叶酸受体靶向的载水飞蓟宾（SB）可吸入聚合物纳米颗粒（FA-CS-SB-NPs）。采用质量源于设计（qbD）方法制备载SB纳米颗粒。通过静电共轭在优化批次中偶联叶酸。使用荷肺癌细胞大鼠模型确定制剂的治疗潜力。优化后的制剂呈现球形表面，平均粒径为275±1.20nm，多分散指数（PDI）为0.234±0.07，ζ电位为32.50±0.21，包封率为75.52±0.87%，48小时时的药物累积释放率（CDR）为63.25±1.21%。发现空气动力学行为如质量中值空气动力学直径（MMAD）和几何尺寸分布（GSD）分别为2.75±1.02和3.15±0.88μm。与FA-CS-SB-NPs孵育24小时后，IC50值为24.5μg/mL。FA-SB-CS-NPs在肺组织中保持了显著更高的水飞蓟宾沉积量。因此，FA-CS-SB-NPs的无创性质和靶向特异性为肺癌的肺部给药治疗铺平了道路。
