State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), and Shaanxi Key Laboratory of Chinese Medicine Fundamentals and New Drugs Research, and Shaanxi University of Chinese Medicine, Xi'an, 712046, People's Republic of China.
Int J Nanomedicine. 2024 Jul 18;19:7273-7305. doi: 10.2147/IJN.S469742. eCollection 2024.
Dried toad skin (TS) and toad venom (TV) are the dried skin of the and the , which remove the internal organs and the white secretions of the skin and retroauricular glands. Since 2005, cinobufacini preparations have been approved by the State Food and Drug Administration for use as adjuvant therapies in the treatment of various advanced cancers. Meanwhile, bufalenolides has been identified as the main component of TS/TV, exhibiting antitumor activity, inducing apoptosis of cancer cells and inhibiting cancer cell proliferation or metastasis through a variety of signaling pathways. However, clinical agents frequently face limitations such as inherent toxicity at high concentrations and insufficient tumor targeting. Additionally, the development and utilization of these active ingredients are hindered by poor water solubility, low bioavailability, and rapid clearance from the bloodstream. To address these challenges, the design of a targeted drug delivery system (TDDS) aims to enhance drug bioavailability, improve targeting within the body, increase drug efficacy, and reduce adverse reactions. This article reviews the TDDS for TS/TV, and their active components, including passive, active, and stimuli-responsive TDDS, to provide a reference for advancing their clinical development and use.
干蟾皮(TS)和蟾酥(TV)是蟾蜍科中华大蟾蜍或黑眶蟾蜍的干燥皮和耳后腺及皮肤腺的分泌物,经干燥而得。自 2005 年以来,华蟾素制剂已获国家食品药品监督管理局批准,作为各种晚期癌症的辅助治疗药物。同时,蟾毒内酯已被确定为 TS/TV 的主要成分,具有抗肿瘤活性,通过多种信号通路诱导癌细胞凋亡和抑制癌细胞增殖或转移。然而,临床制剂常常面临固有毒性在高浓度下和肿瘤靶向不足等限制。此外,这些活性成分的开发和利用受到水溶性差、生物利用度低和在血液中快速清除等因素的限制。为了解决这些挑战,靶向药物传递系统(TDDS)的设计旨在提高药物的生物利用度,改善体内靶向性,提高药物疗效,并减少不良反应。本文综述了 TS/TV 及其活性成分的 TDDS,包括被动、主动和刺激响应型 TDDS,为推进其临床开发和应用提供参考。