Santos A C, Matos C M, Oliveiros B, Almeida T, Gano L, Neves M, Ferreira N
Biophysics/Biomathematics Institute, Medical School, Coimbra University, Azinhaga de Sta Comba, Celas, 3000-548 Coimbra, Portugal.
Curr Radiopharm. 2012 Apr;5(2):166-74.
Liposomes, usually assembled from organic/synthetic lipidic compounds, are biocompatible, biodegradable, non-toxic, and do not induce immune response. Due to their structural versatility in terms of size, composition, surface charge, bilayer fluidity and ability to encapsulate drugs regardless of their solubility, liposomes enable the production of a vast number and type of formulations with potential clinical use. They can be administered through several routes of administration (e.g. i.v., i.m., oral, nasal, etc.). The use of liposomes enables the variation and control retention of drugs in biologic fluids, enhancing blood circulation and specific compartments residence. They can be tailored to target specific tissues and cells. They can play a very important role for imaging diagnosis and/or therapy. After an extensive literature review of the subject, we selected a particular area of potential clinical application: pulmonary ɶdema. This clinical entity has a variety of possible etiologies, conducing to two main types of edema: cardiogenic and non-cardiogenic. At the moment a dedicated technique for the early diagnosis/therapy of this pathology is lacking. We propose a new methodology using a specially designed GUV formulation, encapsulating chosen radiotracers labeled with 99mTc. The aim of the work has been successfully achieved in an experimental animal model of cardiogenic pulmonary oedema. Experiments using an animal model of non-cardiogenic pulmonary oedema are in course (simultaneous study with two different drugs), using the same GUV methodology. Preliminary results are very promising.
脂质体通常由有机/合成脂质化合物组装而成,具有生物相容性、可生物降解、无毒且不引发免疫反应。由于其在大小、组成、表面电荷、双层流动性以及无论药物溶解性如何都能包封药物的结构多功能性,脂质体能够生产大量具有潜在临床用途的制剂类型。它们可以通过多种给药途径(如静脉内、肌肉内、口服、鼻腔等)给药。脂质体的使用能够改变和控制药物在生物流体中的保留,增强血液循环并延长在特定隔室中的停留时间。它们可以进行定制以靶向特定组织和细胞。它们在成像诊断和/或治疗中可以发挥非常重要的作用。在对该主题进行广泛的文献综述之后,我们选择了一个潜在临床应用的特定领域:肺水肿。这种临床病症有多种可能的病因,导致两种主要类型的水肿:心源性和非心源性。目前缺乏针对这种病症的早期诊断/治疗的专用技术。我们提出了一种使用特殊设计的巨型单层囊泡(GUV)制剂的新方法,包封用99mTc标记的选定放射性示踪剂。该工作的目标已在实验性心源性肺水肿动物模型中成功实现。使用非心源性肺水肿动物模型的实验正在进行中(同时研究两种不同药物),采用相同的GUV方法。初步结果非常有前景。