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多西他赛非注射制剂的研究进展。

Advances in the formulations of non-injection administration of docetaxel.

机构信息

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

出版信息

J Drug Target. 2014 Feb;22(2):87-94. doi: 10.3109/1061186X.2013.839686. Epub 2013 Oct 7.

Abstract

Docetaxel is one of the most important anti-tumor drugs and has shown powerful therapeutic activity against breast cancer, non-small cell lung cancer, prostate cancer and so on. Owing to its poor water solubility and the efflux by P-glycoprotein (P-gp) and metabolism by CYP3A4 enzymes, it is generally administered as an injection form, the only manner for the current clinical application. However, the injection bearing polysorbate 80 and ethanol may cause adverse events such as severe hypersensitivity reactions, neutropenia, neurotoxicity, musculoskeletal toxicity and cumulative fluid retention, these adverse events limit clinical application and commercialization of docetaxel. Recently, various kinds of non-injection delivery systems for docetaxel have been developed to eliminate the polysorbate 80-based vehicle and increase the drug solubility. In this review, the non-injection delivery formulations of docetaxel for oral route, transdermal delivery, lung and rectal administration were discussed for future study and clinical application.

摘要

多西紫杉醇是最重要的抗肿瘤药物之一,对乳腺癌、非小细胞肺癌、前列腺癌等具有强大的治疗活性。由于其水溶性差,且由 P 糖蛋白(P-gp)外排和 CYP3A4 酶代谢,因此通常以注射剂的形式给药,这是目前临床应用的唯一方式。然而,含有聚山梨酯 80 和乙醇的注射剂可能会引起严重的过敏反应、中性粒细胞减少、神经毒性、肌肉骨骼毒性和累积性液体潴留等不良反应,这些不良反应限制了多西紫杉醇的临床应用和商业化。最近,已经开发了各种非注射递药系统来递送多西紫杉醇,以消除基于聚山梨酯 80 的载体并增加药物溶解度。本文综述了多西紫杉醇的口服、透皮、肺部和直肠给药的非注射递药制剂,以期为未来的研究和临床应用提供参考。

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