摘要
紫杉醇作为一种高效的天然抗肿瘤药物,在治疗乳腺癌、卵巢癌和肺癌等多种癌症方面效果显著。传统的紫杉醇注射剂存在不良反应明显、患者治疗后生活质量低等问题,在给药途径优化、家庭化治疗模式支持等方面存在局限性。与注射给药相比,口服给药可以避免侵入性途径存在的感染风险,有利于提高患者依从性和生活质量,降低医疗成本,具有良好的应用前景。然而,紫杉醇的溶解性低、渗透性差,同时易受P-糖蛋白外排作用的影响,导致其口服制剂的开发存在巨大的挑战。新型药物递送技术不仅可以改善紫杉醇的溶解性,还具有控制释放药物的特点,有利于提高紫杉醇的口服吸收及疗效。该文梳理了紫杉醇口服制剂的发展历程,同时总结了聚合物胶束、纳米粒、纳米乳剂、纳米晶等递送技术,对各自的应用机制、优势与局限性及在不同癌症治疗中的适应性进行探讨。最后对紫杉醇口服制剂开发所面临的挑战进行总结,并提出未来的研究方向,为紫杉醇口服给药的发展提供新思路。
Paclitaxel,a highly effective natural antitumor drug,has been demonstrated to be efficacious in the treatment of a variety of cancers,including breast cancer,ovarian cancer,and lung cancer.The traditional paclitaxel injections have been observed to present certain issues,including overt adverse reactions and a decline in the quality of life of patients following treatment.This ultimately leads to an inability to meet the comprehensive needs of patients,thereby limiting the clinical applications of the drugs.Compared with injectable administration,the oral administration can avoid the risk of infection present in the invasive route,is conducive to improving patient compliance and quality of life,and reduces healthcare costs,and has a good application prospect.However,paclitaxel has low solubility,poor permeability,and is susceptible to the exocytosis of P-glycoprotein,which presents a significant challenge in the development of its oral preparations.Novel drug delivery technologies can enhance the solubility of paclitaxel and facilitate its controlled release,which is beneficial for the oral absorption and efficacy.The paper reviews the development history of oral preparations of paclitaxel,and summarizes the delivery technologies such as polymer micelles,nanoparticles,nanoemulsions and nanocrystals,and discusses the application mechanisms,advantages and limitations of these technologies and their adaptability in different cancer treatments.Finally,the challenges faced in the development of oral preparations of paclitaxel are summarized,and future research directions are proposed in order to provide new ideas for the development of oral delivery of paclitaxel.
作者
高洁
李师仰
郭静
李荣胜
玄振玉
GAO Jie;LI Shiyang;GUO Jing;LI Rongsheng;XUAN Zhenyu(School of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;School of Pharmacy,Soochow University,Suzhou 215123,China;Suzhou Youseen New Drug Research&Development Co.Ltd.,Suzhou 215125,China;Wuya College of Innovation,Shenyang Pharmaceutical University,Shenyang 110016,China)
出处
《中国实验方剂学杂志》
北大核心
2025年第11期322-330,共9页
Chinese Journal of Experimental Traditional Medical Formulae
基金
上海市科委“生物医药领域”科技支撑项目(21S21901000)。
关键词
紫杉醇
制剂
口服
药物递送系统
抗癌
生物利用度
研究进展
paclitaxel
preparation
oral administration
drug delivery system
anti-cancer
bioavailability
research progress
