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脂质体,铂类衍生物临床应用的一种有前途的策略。

Liposomes, a promising strategy for clinical application of platinum derivatives.

机构信息

University of Navarra, Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Irunlarrea, 1. 31008-Pamplona, Spain.

出版信息

Expert Opin Drug Deliv. 2013 Jun;10(6):829-44. doi: 10.1517/17425247.2013.778240. Epub 2013 Mar 8.

DOI:10.1517/17425247.2013.778240
PMID:23470129
Abstract

INTRODUCTION

Liposomes represent a versatile system for drug delivery in various pathologies. Platinum derivatives have been demonstrated to have therapeutic efficacy against several solid tumors. But their use is limited due to their side effects. Since liposomal formulations are known to reduce the toxicity of some conventional chemotherapeutic drugs, the encapsulation of platinum derivatives in these systems may be useful in reducing toxicity and maintaining an adequate therapeutic response.

AREAS COVERED

This review describes the strategies applied to platinum derivatives in order to improve their therapeutic activity, while reducing the incidence of side effects. It also reviews the results found in the literature for the different platinum-drugs liposomal formulations and their current status.

EXPERT OPINION

The design of liposomes to achieve effectiveness in antitumor treatment is a goal for platinum derivatives. Liposomes can change the pharmacokinetic parameters of these encapsulated drugs, reducing their side effects. However, few liposomal formulations have demonstrated a significant advantage in therapeutic terms. Lipoplatin, a cisplatin formulation in Phase III, combines a reduction in the toxicity associated with an antitumor activity similar to the free drug. Thermosensitive or targeted liposomes for tumor therapy are also included in this review. Few articles about this strategy applied to platinum drugs can be found in the literature.

摘要

简介

脂质体是一种在各种病理中用于药物传递的多功能系统。已经证明铂衍生物对几种实体瘤具有治疗功效。但由于其副作用,其应用受到限制。由于已知脂质体制剂可以降低一些常规化疗药物的毒性,因此将铂衍生物封装在这些系统中可能有助于降低毒性并保持足够的治疗反应。

涵盖领域

本文综述了用于改善铂衍生物治疗活性,同时降低副作用发生率的策略。还回顾了不同铂药物脂质体制剂的文献中发现的结果及其现状。

专家意见

设计脂质体以实现抗肿瘤治疗的效果是铂衍生物的目标。脂质体可以改变这些包裹药物的药代动力学参数,降低其副作用。然而,很少有脂质体制剂在治疗方面表现出显著优势。Lipoplatin(顺铂的一种脂质体制剂)结合了降低与抗肿瘤活性相关的毒性,与游离药物相似。用于肿瘤治疗的热敏或靶向脂质体也包括在本综述中。关于将这种策略应用于铂类药物的文献很少。

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