化学疗法是一种重要且有效的治疗策略,通常用于治疗癌症。基于小分子前药的纳米组装体(SMPDNAs)将前药和纳米药物的益处结合到具有高载药量的单个纳米组装体中,增加稳定性,改善了生物相容性。
■在这项研究中,合理设计了二硫键插入的7-乙基-10-羟基喜树碱(SN38)前药,然后用于制备纳米组装体(SNSSNAs),这些纳米组装体在肿瘤部位被丰富的谷胱甘肽(GSH)选择性激活。进行了SNSSNAs的表征以及它们对胰腺癌模型的抗肿瘤作用的体外和体内评估。
■体外研究结果表明,SNSSNA表现出GSH诱导的SN38释放和细胞毒性。SNSSNAs已经证明了对肿瘤组织的被动靶向作用,与伊立替康(CPT-11)相比,具有更好的抗肿瘤作用,双剂量治疗和令人满意的生物相容性。
■本研究中开发的SNSSNA为制备具有改善的抗肿瘤效果和生物安全性的基于SN38的纳米递送系统提供了新方法。
UNASSIGNED: Chemotherapy is a significant and effective therapeutic strategy that is frequently utilized in the treatment of cancer. Small molecular prodrug-based nanoassemblies (SMPDNAs) combine the benefits of both prodrugs and nanomedicine into a single nanoassembly with high drug loading, increased stability, and improved biocompatibility.
UNASSIGNED: In this study, a disulfide bond inserted 7-ethyl-10-hydroxycamptothecin (SN38) prodrug was rationally designed and then used to prepare nanoassemblies (SNSS NAs) that were selectively activated by rich glutathione (GSH) in the tumor site. The characterization of SNSS NAs and the in vitro and in vivo evaluation of their antitumor effect on a pancreatic cancer model were performed.
UNASSIGNED: In vitro findings demonstrated that SNSS NAs exhibited GSH-induced SN38 release and cytotoxicity. SNSS NAs have demonstrated a passive targeting effect on tumor tissues, a superior antitumor effect compared to irinotecan (CPT-11), and satisfactory biocompatibility with double dosage treatment.
UNASSIGNED: The SNSS NAs developed in this study provide a new method for the preparation of SN38-based nano-delivery systems with improved antitumor effect and biosafety.