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一种使用荧光光谱法监测血清中脂质体药物制剂阿霉素释放的简单易行方法。

A Simple and Easy Method of Monitoring Doxorubicin Release from a Liposomal Drug Formulation in the Serum Using Fluorescence Spectroscopy.

作者信息

Watanabe Ayako, Murayama Shuhei, Karasawa Koji, Yamamoto Eiichi, Morikawa Satoru, Takita Ryo, Murata Shigeo, Kato Masaru

机构信息

One-Stop Sharing Facility Center for Future Drug Discoveries, Graduate School of Pharmaceutical Sciences, The University of Tokyo.

Devision of Bioanalytical Chemistry, School of Pharmacy, Showa University.

出版信息

Chem Pharm Bull (Tokyo). 2019;67(4):367-371. doi: 10.1248/cpb.c18-00868.

Abstract

Formulation of a drug as liposomes facilitates its delivery to the disease target. Rightly, liposomes are gaining popularity in the medical field. In order for the drug to show efficacy, release of the encapsulated drug from the liposome at the target site is required. However, the release is affected by the permeability of the lipid bilayer of the liposome, and it is important to examine the effect of the surrounding environment on the permeability. In this study, we showed the usefulness of fluorescence analysis, especially fluorescence fingerprint, for a rapid and simple monitoring of release of an encapsulated anticancer drug (doxorubicin) from its liposomal formulation (DOXIL). Our result indicated that the release is accelerated by the existence of membrane permeable ions, such as tris(hydroxymethyl)aminomethane, and blood proteins like albumin. Hence, monitoring of doxorubicin release by fluorescence analysis is useful for the efficacy evaluation of DOXIL in a biomimetic environment.

摘要

将药物制成脂质体有助于将其递送至疾病靶点。脂质体在医学领域正日益受到欢迎,这是理所当然的。为使药物发挥疗效,需要将包封在脂质体中的药物在靶点部位释放出来。然而,这种释放受到脂质体脂质双层通透性的影响,研究周围环境对通透性的影响很重要。在本研究中,我们展示了荧光分析,尤其是荧光指纹图谱,对于快速、简单地监测包封的抗癌药物(阿霉素)从其脂质体制剂(多柔比星脂质体)中释放的有用性。我们的结果表明,膜可渗透离子(如三(羟甲基)氨基甲烷)和血液蛋白质(如白蛋白)的存在会加速释放。因此,通过荧光分析监测阿霉素释放对于在仿生环境中评估多柔比星脂质体的疗效很有用。

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