Cancer remains a major global health concern, and thus, there is a growing demand for efficient and selective therapies with low systemic toxicity. Natural bioactive compounds have emerged as promising alternatives, and terpenoids have shown notable anticancer properties. They exert antiproliferative, proapoptotic, anti-invasive, and antimetastatic effects through the regulation of multiple molecular targets and signaling pathways, including modulation of apoptosis, suppression of angiogenesis, and inhibition of tumor-promoting inflammation. However, their clinical translation is constrained by poor aqueous solubility, low bioavailability, rapid systemic clearance, and inadequate tumor accumulation. Recent advances in nanotechnology offer strategies to overcome these limitations. Nanocarrier-based systems improve the solubility, stability, and pharmacokinetics of terpenoids, while enabling tumor-targeted delivery and controlled release. Various strategies, such as enhanced permeability and retention effect, ligand-mediated active targeting, and stimuli-responsive release have been used to achieve selective tumor accumulation and improved therapeutic outcomes. The purpose of this review is to provide a comprehensive evaluation of nanoformulated terpenoids in cancer with a special emphasis on their therapeutic applications and mechanisms of action. Preclinical studies demonstrate that nanocarrier-loaded terpenoids significantly increase bioavailability, enhance apoptosis, and suppress tumor angiogenesis compared with free terpenoids. The incorporation of artificial intelligence and machine learning further holds promise for the rational design of nanomedicines, accelerating their path toward clinical translation. Collectively, these developments position nanoformulated terpenoids as a powerful platform in precision oncology with strong potential for future application in cancer therapy.
癌症仍是全球主要的健康问题,因此对高效、选择性高且全身毒性低的治疗手段需求日益增长。天然生物活性化合物已成为有前景的替代选择,其中萜类化合物展现出显著的抗癌特性。它们通过调控多种分子靶点和信号通路——包括调节细胞凋亡、抑制血管生成及阻断肿瘤促进性炎症——发挥抗增殖、促凋亡、抗侵袭和抗转移作用。然而,其临床转化受限于水溶性差、生物利用度低、全身清除快及肿瘤蓄积不足等问题。纳米技术的最新进展为克服这些局限提供了策略。基于纳米载体的递送系统可改善萜类化合物的溶解性、稳定性和药代动力学特性,同时实现肿瘤靶向递送和可控释放。通过增强渗透与滞留效应、配体介导的主动靶向及刺激响应性释放等多种策略,可实现选择性肿瘤蓄积并提升治疗效果。本综述旨在全面评估纳米化萜类化合物在癌症治疗中的应用,重点关注其治疗作用机制。临床前研究表明,与游离萜类化合物相比,纳米载体负载的萜类化合物能显著提高生物利用度、增强细胞凋亡并抑制肿瘤血管生成。人工智能与机器学习技术的融合进一步为纳米药物的理性设计提供可能,加速其临床转化进程。总体而言,这些进展使纳米化萜类化合物成为精准肿瘤学中的重要平台,在癌症治疗领域具有广阔的应用前景。