Liposomes: From the bench to the bed
Liposomes: From the bench to the bed
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DOI：
10.1081/lpr-120017488
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发表时间：
2003-01-01
影响因子：
4.4
通讯作者：
Storm, G
中科院分区：
文献类型：
--
作者：
Crommelin, DJA;Storm, G
几种脂质体制剂已经成功地开发出来并推向市场。例如阿霉素、柔红霉素和含有两性霉素的脂质体。一些其他脂质体产品目前正在开发中，既可用于非肠道外，也可用于非肠道内使用。所有这些配方都必须符合药品定义的高质量标准。为了确保适当的脂质体性能，必须建立脂质体分散体的批次到批次的重复性和稳定性。这需要定义脂质体分散体在制剂前阶段、临床试验阶段和最终生产阶段的特性。Barenholz和Crommelin(1)列出了脂质体制剂的质量控制分析(表1)。本清单是一份综合性清单，相关检测方法的选择取决于脂质体产品的开发阶段。有趣的是，FDA目前正在制定脂质体产品的指南，并将讨论这些指南中提出的一些问题。当翻阅表1时，很明显脂质体的物理和化学特征是复杂的。特别是，在这些分散体中，物理性质，如脂质体大小和片层性质通常是不均匀的，很难用一个参数来掌握。另一个有争议的问题是为脂质体配方设定规格。在化合物和产品相关的杂质方面，什么是可接受的？
Several liposomal formulations have been successfully developed and reached the market place. Examples are doxorubicin, daunorubicin, and amphothericin containing liposomes. A number of other liposomal products are presently under development both for parenteral and non-parenteral use. All these formulations have to meet the high quality criteria as defined for pharmaceutical products. To ensure proper liposome performance, batch to batch reproducibility, and stability of the liposome dispersions has to be established. This requires definition of the charactistics of liposome dispersions in the preformulation stage, clinical test stage, and final production stage.Barenholz and Crommelin (1) listed quality control assays for liposomal preparation (Table 1). This list is a comprehensive list and the selection of relevant assays depends on the stage of development of the liposome product. Interestingly, the FDA is presently working on guidelines for liposome products and some issues brought up in these guidelines will be discussed. When one goes through Table 1, it is clear that the physical and chemical characterization of liposomes is complex. In particular, in these dispersions physical properties such as liposome size and lamellarity are often heterogeneous in nature and difficult to grasp in one parameter. Another issue of debate is setting the specifications for the liposomes formulations. What is acceptable in terms of compound and product related impurities?