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.

Highlights

  • Small-angle X-ray and neutron scattering (SAXS and Small-angle X-ray (SAXS) and neutron (SANS), respectively) measurements are conceptually very simple and the basic principles are similar to those of light scattering, which is routinely used in biological and pharmaceutical labs to estimate the size distribution of formulations with particles in the submicron domain [1]

  • In this paper we mainly focus on the recent applications of SAXS and SANS for the characterization of lipidic self-assembled soft nano-structures

  • Schilt et al have reported a throughout investigation, based on SAXS and WAXS, on a series of PEGylated liposomes loaded with doxorubicin, a system that has already been approved for clinical applications [14]

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Summary

Introduction

Small-angle X-ray and neutron scattering (SAXS and SANS, respectively) measurements are conceptually very simple and the basic principles are similar to those of light scattering, which is routinely used in biological and pharmaceutical labs to estimate the size distribution of formulations with particles in the submicron domain [1]. In the case of X-rays, the scattering originates from electrons, and it is nearly independent of the incident wavelength, except in the close vicinity of the absorption edge of the constituent elements The beamstop is often equipped with intensity monitors to record transmission simultaneously with the scattering the with the the scattering pattern. X-raythe scattering can give information over a wideX-ray rangescattering of scattering qa wide provides theoflength scales probed byultralow the experiment. Reviews of experimental aspects of the technique and descriptions ofexperimental the different types of space dimensions from the μm down to the nm range

Layout
Calculated
Studies under Equilibrium Conditions
Localisation of Guest Molecules in Drug Loaded Liposomes
Studies under Non-Equilibrium Conditions
Pure Liposome
Effect of External Stimuli on the Liposome Structure
Drug-Loaded Liposome
Findings
Conclusions and Perspectives
Full Text
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