Samanta Siddhartha, Pramanik Nilkamal, Singh Nitesh, Maity Sanhita, Pradhan Anirban
Department of Chemistry, Birla Institute of Technology (BIT)─Mesra, Ranchi, Jharkhand 835215, India.
Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, Nebraska 68198, United States.
ACS Appl Bio Mater. 2025 Aug 18;8(8):7139-7144. doi: 10.1021/acsabm.5c00891. Epub 2025 Aug 4.
The high surface area to volume ratio of covalent organic frameworks (COFs) provides higher surface energy, which makes them fascinating for studying the rapid adsorption of biomolecules followed by their sustained cellular delivery. Besides their many scopes of application, the therapeutic efficacy of these materials has been less explored. These hurdles are overcome herein by the surface modification of perylene-porphyrin based COF (P) with hydrophilic hyaluronic acid (HA) as confirmed by the UV, FTIR spectra, and fluorescence microscopy analyses. The resulting HA modification is shown to increase the cellular uptake of nanoparticles into CD44 expressing MDA MB231 breast cancer lines with minimum inherent toxic effects. Further, the chemotherapeutic agent doxorubicin loaded HA-P nanoparticles showed significant antitumor activity in killing the MDA MB-231 breast cancer lines at higher drug concentration (more than 80% cell death at 5 μM Dox) and even at lower ranges of Dox concentration as compared to P compound and free Dox. In summary, the developed fluorescence active multifunctional drug delivery system demonstrated superior cellular internalization with a maximum antitumor activity.
共价有机框架材料（COFs）的高比表面积提供了更高的表面能，这使得它们在研究生物分子的快速吸附及其持续的细胞递送方面具有吸引力。除了其众多的应用范围外，这些材料的治疗效果尚未得到充分探索。本文通过用亲水性透明质酸（HA）对基于苝-卟啉的COF（P）进行表面改性克服了这些障碍，紫外、傅里叶变换红外光谱和荧光显微镜分析证实了这一点。结果表明，HA修饰增加了纳米颗粒对表达CD44的MDA MB231乳腺癌细胞系的细胞摄取，且固有毒性最小。此外，负载化疗药物阿霉素的HA-P纳米颗粒在较高药物浓度（5 μM阿霉素时细胞死亡率超过80%）下以及与P化合物和游离阿霉素相比在较低阿霉素浓度范围内对MDA MB-231乳腺癌细胞系均显示出显著的抗肿瘤活性。总之，所开发的具有荧光活性的多功能药物递送系统表现出优异的细胞内化能力和最大抗肿瘤活性。
