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使用光物理探针评估脂质体内的药物包封情况。

Assessment of drug entrapment within liposomes using photophysical probes.

作者信息

Oliverio Filomena, Nuin Edurne, Andreu Inmaculada, Ragno Gaetano, Miranda Miguel A

机构信息

Instituto de Tecnología Química (UPV-CSIC), Universitat Politècnica de València, Consejo Superior de Investigaciones Científicas, Valencia, Spain; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende, Italy.

Instituto de Tecnología Química (UPV-CSIC), Universitat Politècnica de València, Consejo Superior de Investigaciones Científicas, Valencia, Spain.

出版信息

Eur J Pharm Biopharm. 2014 Oct;88(2):551-5. doi: 10.1016/j.ejpb.2014.06.013. Epub 2014 Jun 26.

DOI:10.1016/j.ejpb.2014.06.013
PMID:24973632
Abstract

The photophysical and photochemical behavior of (R)-cinacalcet (CIN) and (S)-naproxen (NPX) entrapped within liposomes has been studied. For this purpose, liposome encapsulated drugs have been prepared through thin layer evaporation and characterized by transmission electron microscopy, cryoscopy scanning electron microscopy and dynamic light scattering. Steady state and time-resolved fluorescence experiments showed similar spectra, emission quantum yields, singlet energies and lifetimes for the selected drugs, outside and inside liposomes. By contrast, laser flash photolysis experiments revealed an important enhancement of the triplet lifetimes for entrapped drugs inside liposomes, indicating the spatial confinement existing in the microenvironment prevailing in these biomimetic entities. Thus, this photophysical property shows potential as a non-invasive, direct and valuable tool to monitor encapsulation of photoactive drugs and to probe the intraliposome environment. In addition, it provides a new quantitative indicator of the capability of liposomes to act as drug carriers.

摘要

研究了包裹在脂质体内的(R)-西那卡塞(CIN)和(S)-萘普生(NPX)的光物理和光化学行为。为此,通过薄膜蒸发法制备了脂质体包封药物,并通过透射电子显微镜、冰点降低扫描电子显微镜和动态光散射对其进行了表征。稳态和时间分辨荧光实验表明,所选药物在脂质体外部和内部的光谱、发射量子产率、单线态能量和寿命相似。相比之下,激光闪光光解实验表明,脂质体内包裹药物的三重态寿命显著延长,这表明这些仿生实体中普遍存在的微环境存在空间限制。因此,这种光物理性质有望成为一种非侵入性、直接且有价值的工具,用于监测光活性药物的包封情况并探测脂质体内环境。此外,它为脂质体作为药物载体的能力提供了一个新的定量指标。

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