Liu Chenggong, Han Qiongmei, Liu Hua, Zhu Cuirong, Gui Wei, Yang Xiaodong, Li Wansen
Department of General Practice, Zhumadian City Central Hospital, Zhumadian, China.
Department of Endocrinology, Yankuang New Journey General Hospital, Jining, Shandong, China.
Drug Deliv. 2020 Dec;27(1):1063-1072. doi: 10.1080/10717544.2020.1790693.
GLOBOCAN estimates 36 types of cancers in 185 countries based on the incidence, mortality, and prevalence in the year 2019. Nowadays, chemotherapy is the most widely used cancer treatment among immune, radio, hormone, and gene therapies. Here, we describe a very simple yet cost-effective approach that synergistically combines drug reconstitution, supramolecular nano-assembly, and tumor-specific targeting to address the multiple challenges posed by the delivery of the chemotherapeutic Gemcitabine (GEM) drug. The GEM prodrugs were gifted to impulsively self-assemble into excellent steady nanoparticles size on covalent conjugation of linoleic acid hydrophobic through amide group with ∼100 nm. Newly synthesized GEM-NPs morphology was confirmed by various electron microscopic techniques. After successful synthesis, we have evaluated the anticancer property of GEM and GEM-NPs against B-CPAP (papillary thyroid carcinoma) and FTC-133 (human follicular thyroid carcinoma) cancer cell lines. Further studies such as AO-EB (acridine orange-ethidium bromide), nuclear staining and flow cytometry analyses on cell death mechanism signified that the cytotoxicity was associated with apoptosis in thyroid cancer cells. GEM-NPs show excellent biocompatibility compared to GEM. The present study explained that GEM-NPs as a safe and hopeful strategy for chemotherapeutics of thyroid cancer therapy and deserve for further clinical evaluations.
全球癌症观测站(GLOBOCAN)基于2019年的发病率、死亡率和患病率,对185个国家的36种癌症进行了估算。如今,在免疫疗法、放射疗法、激素疗法和基因疗法中,化疗是应用最广泛的癌症治疗方法。在此,我们描述了一种非常简单且具有成本效益的方法,该方法将药物重构、超分子纳米组装和肿瘤特异性靶向协同结合,以应对化疗药物吉西他滨(GEM)递送所带来的多重挑战。通过酰胺基团将亚油酸疏水基团共价偶联后,GEM前药能自发组装成尺寸约为100纳米的优良稳定纳米颗粒。通过各种电子显微镜技术确认了新合成的GEM纳米颗粒的形态。成功合成后,我们评估了GEM和GEM纳米颗粒对B-CPAP(甲状腺乳头状癌)和FTC-133(人甲状腺滤泡癌)癌细胞系的抗癌特性。进一步的研究,如吖啶橙-溴化乙锭(AO-EB)、细胞核染色和流式细胞术分析细胞死亡机制,表明细胞毒性与甲状腺癌细胞的凋亡有关。与GEM相比,GEM纳米颗粒表现出优异的生物相容性。本研究表明,GEM纳米颗粒是一种安全且有前景的甲状腺癌化疗策略,值得进一步进行临床评估。