Abstract

Lipid liposomes are promising drug delivery systems because they have superior curative effects owing to their high adaptability to a living body. Lipid liposomes encapsulating proteins were constructed and the structures examined using synchrotron radiation small- and wide-angle X-ray scattering (SR-SWAXS). The liposomes were prepared by a sequential combination of natural swelling, ultrasonic dispersion, freeze-throw, extrusion and spin-filtration. The liposomes were composed of acidic glycosphingolipid (ganglioside), cholesterol and phospholipids. By using shell-modeling methods, the asymmetric bilayer structure of the liposome and the encapsulation efficiency of proteins were determined. As well as other analytical techniques, SR-SWAXS and shell-modeling methods are shown to be a powerful tool for characterizing in situ structures of lipid liposomes as an important candidate of drug delivery systems.

Highlights

  • Liposomes are closed bilayer lipid systems and afford a very useful tool in various scientific fields including biology and theoretical physics, biophysics, chemistry, colloid science and so on

  • In spite of the addition of proteins with different concentrations, all scattering curves after spin-filtration agree with the scattering curve of large unilamellar vesicle (LUV) without the addition of proteins in the whole q range, indicating that un-entrapped proteins were removed from the solution without affecting the LUV structure and its dispersity

  • By the combination of different types of liposome preparation methods, proteins were effectively encapsulated within the water pool of LUV composed of glycosphingolipid, cholesterol and phospholipid

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Summary

Introduction

Liposomes are closed bilayer lipid systems and afford a very useful tool in various scientific fields including biology and theoretical physics, biophysics, chemistry, colloid science and so on. During the past 30 years, liposomes have received a lot of attention as effective drug delivery systems (DDS) because they can reduce drug toxicity due to biodegradability and biocompatibility, and offer promising carriers of anti-cancer, anti-fungal and anti-biotic drugs, gene medicines and anesthetics and anti-inflammatory drugs, compared with other delivery systems (Kaneda, 2000; Rahimpour & Hamishehkar, 2012; Allen & Cullis, 2013) Liposome studies and those clinical trials have progressed from the use of conventional liposomes to that of ‘secondgeneration liposomes’ that are developed by modulating the lipid composition, size and modified surface of liposome (Torchilin, 2005). It can be assumed that gangliosides are promising reagents of liposome due to those intrinsic properties

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