Mushtaq Asim, Li Li, A Anitha, Grøndahl Lisbeth
School of Chemistry and Molecular Biosciences, The University of Queensland, Cooper Road, Brisbane, Queensland, 4072, Australia.
Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, Corner of College and Cooper Road, Brisbane, Queensland, 4072, Australia.
Macromol Biosci. 2025 Jul;25(7):e2400627. doi: 10.1002/mabi.202400627. Epub 2025 Apr 10.
Bone metastasized breast cancer reduces the quality of life and median survival. Targeted delivery of twist1-siRNA using nanoparticles (NPs) is a promising strategy to overcome current limitations in treating such metastatic breast cancers. This research evaluates two types of chitosan (CHI)-based NPs for the delivery of twist1-siRNA. Alendronate conjugated PEG functionalized chitosan (ALD-PEG-CHI) NPs are developed for active targeting while PEG functionalized CHI (mPEG-CHI) NPs are fabricated for passive targeting. The size of twist1-siRNA-loaded NPs is below 70 nm and the zeta potential is near neutral for both types of NPs. Based on gel retardation assay, complete encapsulation of twist1-siRNA is achieved in both NP systems. The ALD-PEG-CHI-siRNA and mPEG-CHI-siRNA NPs display serum protection for 6 and 4 h, respectively, compared to the immediate degradation of naked twist1-siRNA. The NPs can knockdown twist1 in 4T1 cells as demonstrated through protein expression as well as by phenotypic change in directional cell migration by wound healing assay. Overall, these in vitro results illustrate the potential of the NPs as an effective therapeutic system for bone metastasized breast cancer.
骨转移性乳腺癌会降低生活质量并缩短中位生存期。使用纳米颗粒(NPs)靶向递送twist1-siRNA是克服当前治疗此类转移性乳腺癌局限性的一种有前景的策略。本研究评估了两种基于壳聚糖(CHI)的纳米颗粒用于递送twist1-siRNA的效果。开发了阿仑膦酸盐共轭聚乙二醇功能化壳聚糖(ALD-PEG-CHI)纳米颗粒用于主动靶向,而制备了聚乙二醇功能化壳聚糖(mPEG-CHI)纳米颗粒用于被动靶向。两种类型的纳米颗粒中,负载twist1-siRNA的纳米颗粒尺寸均低于70nm,且zeta电位接近中性。基于凝胶阻滞试验,在两种纳米颗粒系统中均实现了twist1-siRNA的完全包封。与裸twist1-siRNA立即降解相比,ALD-PEG-CHI-siRNA和mPEG-CHI-siRNA纳米颗粒分别显示出6小时和4小时的血清保护作用。通过蛋白质表达以及伤口愈合试验中细胞定向迁移的表型变化证明,这些纳米颗粒可以在4T1细胞中敲低twist1。总体而言,这些体外结果说明了纳米颗粒作为骨转移性乳腺癌有效治疗系统的潜力。