Application of fluorocarbon nanoparticles of <SUP>131</SUP>I-fulvestrant as a targeted radiation drug for endocrine therapy on human breast cancer

作者全名："Zhi, Li; Cheng, Chen; Jing, Luo; Zhi-Ping, Peng; Lu, Yang; Yan, Tian; Zhi-Gang, Wang; Guo-Bing, Yin"

作者地址："[Zhi, Li; Cheng, Chen; Lu, Yang; Guo-Bing, Yin] Chongqing Med Univ, Affiliated Hosp 2, Dept Breast & Thyroid Surg, 74 Linjiang Rd, Chongqing 400010, Peoples R China; [Jing, Luo] Chongqing Med Univ, Affiliated Hosp 1, Dept Pathol, Chongqing 400010, Peoples R China; [Zhi-Ping, Peng] Chongqing Med Univ, Dept Nucl Med Lab, Chongqing 400010, Peoples R China; [Yan, Tian] Chongqing Med Univ, Affiliated Hosp 2, Dept Nucl Med, Chongqing 400010, Peoples R China; [Zhi-Gang, Wang] Chongqing Med Univ, Affiliated Hosp 2, Dept Ultrasound Res Inst, Chongqing 400010, Peoples R China"

通信作者："Guo-Bing, Y (通讯作者)，Chongqing Med Univ, Affiliated Hosp 2, Dept Breast & Thyroid Surg, 74 Linjiang Rd, Chongqing 400010, Peoples R China."

来源：JOURNAL OF NANOBIOTECHNOLOGY

ESI学科分类：BIOLOGY & BIOCHEMISTRY

WOS号：WOS:001183950800001

JCR分区：Q1

影响因子：10.6

年份：2024

卷号：22

期号：1

开始页：　

结束页：　

文献类型：Article

关键词：Breast cancer; Nanomedicine; Fulvestrant; Cerenkov radiation; Nuclear medicine; Photodynamic therapy

摘要："Background Breast cancer is the most prevalent malignant tumor among women, with hormone receptor-positive cases constituting 70%. Fulvestrant, an antagonist for these receptors, is utilized for advanced metastatic hormone receptor-positive breast cancer. Yet, its inhibitory effect on tumor cells is not strong, and it lacks direct cytotoxicity. Consequently, there's a significant challenge in preventing recurrence and metastasis once cancer cells develop resistance to fulvestrant. Method To address these challenges, we engineered tumor-targeting nanoparticles termed I-131-fulvestrant-ALA-PFP-FA-NPs. This involved labeling fulvestrant with I-131 to create I-131-fulvestrant. Subsequently, we incorporated the I-131-fulvestrant and 5-aminolevulinic acid (ALA) into fluorocarbon nanoparticles with folate as the targeting agent. This design facilitates a tri-modal therapeutic approach-endocrine therapy, radiotherapy, and PDT for estrogen receptor-positive breast cancer. Results Our in vivo and in vitro tests showed that the drug-laden nanoparticles effectively zeroed in on tumors. This targeting efficiency was corroborated using SPECT-CT imaging, confocal microscopy, and small animal fluorescence imaging. The I-131-fulvestrant-ALA-PFP-FA-NPs maintained stability and showcased potent antitumor capabilities due to the synergism of endocrine therapy, radiotherapy, and CR-PDT. Throughout the treatment duration, we detected no notable irregularities in hematological, biochemical, or histological evaluations. Conclusion We've pioneered a nanoparticle system loaded with radioactive isotope I-131, endocrine therapeutic agents, and a photosensitizer precursor. This system offers a combined modality of radiotherapy, endocrine treatment, and PDT for breast cancer."

基金机构："National Natural Science Foundation of China [82002615, 81972460]"

基金资助正文：This work was supported by the National Natural Science Foundation of China (No. 82002615 and No. 81972460).