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小角X射线和中子散射:研究载药脂质体结构的强大工具。

Small Angle X-ray and Neutron Scattering: Powerful Tools for Studying the Structure of Drug-Loaded Liposomes.

作者信息

Di Cola Emanuela, Grillo Isabelle, Ristori Sandra

机构信息

Laboratoire Interdisciplinaire de Physique (LIPhy), Université Grenoble-Alpes, CNRS-UMR 5588, 140 rue de la Physique, 38402 Saint-Martin-d'Hères, France.

Institut Laue-Langevin (ILL) DS/LSS, CS 20156-38042 Grenoble Cedex 9, France.

出版信息

Pharmaceutics. 2016 Mar 28;8(2):10. doi: 10.3390/pharmaceutics8020010.

Abstract

Nanovectors, such as liposomes, micelles and lipid nanoparticles, are recognized as efficient platforms for delivering therapeutic agents, especially those with low solubility in water. Besides being safe and non-toxic, drug carriers with improved performance should meet the requirements of (i) appropriate size and shape and (ii) cargo upload/release with unmodified properties. Structural issues are of primary importance to control the mechanism of action of loaded vectors. Overall properties, such as mean diameter and surface charge, can be obtained using bench instruments (Dynamic Light Scattering and Zeta potential). However, techniques with higher space and time resolution are needed for in-depth structural characterization. Small-angle X-ray (SAXS) and neutron (SANS) scattering techniques provide information at the nanoscale and have therefore been largely used to investigate nanovectors loaded with drugs or other biologically relevant molecules. Here we revise recent applications of these complementary scattering techniques in the field of drug delivery in pharmaceutics and medicine with a focus to liposomal carriers. In particular, we highlight those aspects that can be more commonly accessed by the interested users.

摘要

纳米载体,如脂质体、胶束和脂质纳米颗粒,被认为是递送治疗剂的有效平台,尤其是那些在水中溶解度低的治疗剂。除了安全无毒外,性能改进的药物载体应满足以下要求:(i)合适的尺寸和形状;(ii)货物装载/释放时性质不变。结构问题对于控制负载载体的作用机制至关重要。可以使用台式仪器(动态光散射和zeta电位)获得诸如平均直径和表面电荷等整体性质。然而,需要具有更高空间和时间分辨率的技术来进行深入的结构表征。小角X射线(SAXS)和中子(SANS)散射技术可在纳米尺度上提供信息,因此已被广泛用于研究负载药物或其他生物相关分子的纳米载体。在此,我们回顾了这些互补散射技术在制药和医学领域药物递送中的最新应用,重点是脂质体载体。特别是,我们强调了感兴趣的用户更常能了解到的那些方面。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7eb1/4932473/0b68b65de379/pharmaceutics-08-00010-g001.jpg

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