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紫杉醇非注射给药制剂的最新研究进展。

Current development in the formulations of non-injection administration of paclitaxel.

机构信息

Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.

Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.

出版信息

Int J Pharm. 2018 May 5;542(1-2):242-252. doi: 10.1016/j.ijpharm.2018.03.030. Epub 2018 Mar 16.

Abstract

Paclitaxel (PTX) belongs to a class of taxane anti-tumor drug used for the clinic treatment of breast cancer, ovarian cancer, non-small-cell lung cancer, and so on. PTX has poor water solubility and oral bioavailability. It is generally administered via intravenous (i.v.) infusion. Traditional PTX injectable preparations contain Cremophor-EL and ethanol to improve its solubility, which would result in adverse reactions like severe hypersensitivity, neutropenia, etc. Adverse reactions can be reduced only by complicated pretreatment with glucocorticoid and antihistamines drugs and followed by PTX slow infusion for three hours, which has brought significant inconvenience to the patients. Though, a new-generation PTX formulation, Abraxane, free of Cremophor-EL and ethanol, is still being administrated by frequent i.v. infusions and extremely expensive. Therefore, non-injection administration of PTX is urgently needed to avoid the side effects as well as reduce inconvenience to the patients. Recently, a variety of non-injection drug delivery systems (DDSs) of PTX have been developed. This review aims to discuss the progress of non-injectable administration systems of PTX, including oral administration systems, vaginal administration systems, implantable DDSs, transdermal DDSs and intranasal administration for the future study and clinical applications.

摘要

紫杉醇(PTX)属于紫杉烷类抗肿瘤药物,用于临床治疗乳腺癌、卵巢癌、非小细胞肺癌等。PTX 水溶性差,口服生物利用度低。一般通过静脉(i.v.)输注给药。传统的 PTX 注射制剂含有 Cremophor-EL 和乙醇以提高其溶解度,但会导致严重过敏反应、中性粒细胞减少症等不良反应。只有通过复杂的糖皮质激素和抗组胺药物预处理,并进行三小时的 PTX 缓慢输注,才能减少不良反应,但这给患者带来了很大的不便。尽管新一代的紫杉醇制剂 Abraxane 不含 Cremophor-EL 和乙醇,但仍需频繁静脉输注,且价格昂贵。因此,急需非注射途径给药以避免副作用并减少患者的不便。最近,已经开发了多种紫杉醇的非注射给药系统(DDS)。本综述旨在讨论 PTX 的非注射给药系统的进展,包括口服给药系统、阴道给药系统、植入式 DDS、透皮 DDS 和鼻内给药,为未来的研究和临床应用提供参考。

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