注射用紫杉醇在剂型和递送技术方面的进展

doi:10.5246/jcps.2015.08.063

中国药学(英文版) ›› 2015, Vol. 24 ›› Issue (8): 487-500.DOI: 10.5246/jcps.2015.08.063

• 【综述】 • 下一篇

注射用紫杉醇在剂型和递送技术方面的进展

孙静, 代文兵, 梁哲, 王兆扬, 黄昌盛, 何冰, 张华, 王学清, 张强^*

北京大学医学部药学院天然药物及仿生药物国家重点实验室, 北京 100191

收稿日期:2015-03-09 修回日期:2015-03-20 出版日期:2015-08-22 发布日期:2015-04-10
通讯作者: Tel.: 86-10-82802791, E-mail: zqdodo@bjmu.edu.cn
基金资助:
Key Project from the Ministry of Science and Technology (Grant No. 2014ZX09507001-010) and Innovation Team of Ministry of Education (Grant No. BMU20110263).

Advances in the formulation and delivery technology of paclitaxel for injection

Jing Sun, Wenbing Dai, Zhe Liang, Zhaoyang Wang, Changsheng Huang, Bing He, Hua Zhang, Xueqing Wang, Qiang Zhang^*

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2015-03-09 Revised:2015-03-20 Online:2015-08-22 Published:2015-04-10
Contact: Tel.: 86-10-82802791, E-mail: zqdodo@bjmu.edu.cn
Supported by:
Key Project from the Ministry of Science and Technology (Grant No. 2014ZX09507001-010) and Innovation Team of Ministry of Education (Grant No. BMU20110263).

摘要/Abstract

摘要：

紫杉醇用于治疗人体各种实体瘤比如卵巢癌, 乳腺癌, 头颈部癌和黑色素瘤, 是一个很有前景的抗癌药物。由于它的疏水性, 紫杉醇的第一个给药剂型泰素是以非水浓缩液的形式存在, 成分主要含有聚氧乙烯蓖麻油和乙醇, 它在长时间的输注前必须用合适的水溶液稀释。基于它的成分和用法, 泰素存在严重的不良反应并造成临床应用的不便。为了解决以上问题, 科学家们开始致力于开发低毒、较好耐受性、不含聚氧乙烯蓖麻油的紫杉醇新剂型。最近几年, 新的药物递送系统如白蛋白纳米粒、胶束、脂质体等已经处于研究中。在这篇综述中, 我们提出了注射用紫杉醇的一些新剂型及递送技术, 并且重点研究已经上市的或处于临床研究阶段的几个制剂的部分临床前和临床研究成果。最后, 阐述纳米技术优势的几个原因及紫杉醇给药系统现存的挑战和展望。

关键词: 紫杉醇, 泰素, 临床前和临床研究, 新型药物给药系统

Abstract:

Paclitaxel is a promising antineoplastic agent against a variety of human solid tumors, such as ovary, breast, lung, head and neck tumors, and melanoma. Owing to its poor solubility, the first available formulation of paclitaxel (Taxol^®) exists as a non-aqueous concentrate composed of Cremophor EL (polyethoxylated castor oil) and ethanol. It must be diluted to a suitable aqueous solution prior to long time intravenous infusion. Based on the components and usage, Taxol^® has serious adverse effects and is inconvenient for clinical use. To address these problems, the development of a less-toxic, better-tolerated, Cremophor EL-free formulation of paclitaxel has been attempted. In recent years, new drug delivery systems (DDS) including albumin-based nanoparticles, micelles, liposomes, etc. have been investigated. In this review, we present the formulations and delivery technologies of paclitaxel for injection and focus on some of preclinical and clinical experience on the formulations which are already on the market or under clinical stages. Finally, possible nanotechnology advantages, existing challenges and future perspectives of paclitaxel delivery are highlighted.

Key words: Paclitaxel, Taxol®, Preclinical and clinical studies, New drug delivery system

中图分类号:

R943

Supporting:

孙静, 代文兵, 梁哲, 王兆扬, 黄昌盛, 何冰, 张华, 王学清, 张强. 注射用紫杉醇在剂型和递送技术方面的进展[J]. 中国药学(英文版), 2015, 24(8): 487-500.

Jing Sun, Wenbing Dai, Zhe Liang, Zhaoyang Wang, Changsheng Huang, Bing He, Hua Zhang, Xueqing Wang, Qiang Zhang. Advances in the formulation and delivery technology of paclitaxel for injection[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(8): 487-500.

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注射用紫杉醇在剂型和递送技术方面的进展

Advances in the formulation and delivery technology of paclitaxel for injection

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