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“纳米紫杉醇”:释放潜能,重新定义癌症化疗

"Nano-Paclitaxel" Unlocking Potential and Redefining Cancer Chemotherapy.

作者信息

Muley Anuja, Navale Aniket, Gupta Rachna, Tekade Rakesh Kumar

机构信息

An Institute of National Importance, Government of India, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad Palaj, Opp. Air force station, Gandhinagar, Gujarat 382355, India.

出版信息

ACS Omega. 2025 Jun 27;10(27):28670-28690. doi: 10.1021/acsomega.5c02916. eCollection 2025 Jul 15.

Abstract

Paclitaxel (PTX) has emerged as one of the first-line drug candidates in cancer therapy due to its potency and profound anticancer potential. Derived from a rich natural source, it stands out as a beacon of hope in the battle against various forms of cancer, such as breast, lung, ovarian, head, and neck tumors. PTX presents significant challenges in its pharmaceutical application, including low aqueous solubility (10-20 mg/L), limited oral bioavailability (approximately 10%), and nonlinear pharmacokinetics, particularly with short infusion times. Furthermore, its highly lipophilic nature necessitates formulation in the challenging vehicle Cremophor EL, contributing to hypersensitivity reactions and hyperlipidemia. The primary concerns in PTX delivery encompass its availability and the incidence of adverse drug events, emphasizing the critical necessity of innovative drug delivery strategies. Nanoformulations of PTX herald a new dawn in cancer treatment, leaving behind harmful vehicles and offering targeted delivery of the drug. Numerous nanoformulations have been proposed, such as nanoparticles, liposomes, micelles, nanoemulsions, and others. These ground-breaking formulations not only mitigate organ toxicities and hypersensitivity reactions but also pave the way for a regime of lower risk, fueling hope in the fight against cancer. This review article is evidence of the enduring legacy of PTX, offering profound insights into its journey from discovery to the present day and chronicling the remarkable advancements and progress in its nanocarrier-mediated delivery.

摘要

紫杉醇(PTX)因其强大的效力和巨大的抗癌潜力,已成为癌症治疗的一线候选药物之一。它源自丰富的天然来源,在对抗各种癌症(如乳腺癌、肺癌、卵巢癌、头颈肿瘤)的战斗中脱颖而出,成为希望的灯塔。PTX在其药物应用中面临重大挑战,包括低水溶性(10 - 20毫克/升)、口服生物利用度有限(约10%)以及非线性药代动力学,尤其是在输注时间较短时。此外,其高度亲脂性使得必须在具有挑战性的载体聚氧乙烯蓖麻油(Cremophor EL)中进行制剂,这会导致过敏反应和高脂血症。PTX递送中的主要问题包括其可用性和药物不良事件的发生率,强调了创新药物递送策略的迫切必要性。PTX的纳米制剂预示着癌症治疗的新曙光,摒弃了有害载体并实现了药物的靶向递送。已经提出了许多纳米制剂,如纳米颗粒、脂质体、胶束、纳米乳液等。这些开创性的制剂不仅减轻了器官毒性和过敏反应,还为低风险治疗方案铺平了道路,为抗癌斗争注入了希望。这篇综述文章证明了PTX的持久影响力,深入洞察了其从发现到如今的历程,并记录了其纳米载体介导递送方面的显著进展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d9c2/12268397/38235d633033/ao5c02916_0001.jpg

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