Abstract

The aim of this work was the evaluation of the physico-chemical properties of a new type of liposomes that are composed of DPPC and bioconjugates of anisic acid with phosphatidylcholine. In particular, the impact of modified anisic acid phospholipids on the thermotropic parameters of liposomes was determined, which is crucial for using them as potential carriers of active substances in cancer therapies. Their properties were determined using three biophysical methods, namely differential scanning calorimetry (DSC), steady-state fluorimetry and attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR). Moreover, temperature studies of liposomes composed of DPPC and bioconjugates of anisic acid with phosphatidylcholine provided information about the phase transition, fluidity regarding chain order, hydration and dynamics. The DSC results show that the main phase transition peak for conjugates of anisic acid with phosphatidylcholine molecules was broadened and shifted to a lower temperature in a concentration- and structure-dependent manner. The ATR-FTIR results and the results of measurements conducted using fluorescent probes located at different regions in the lipid bilayer are in line with DSC. The results show that the new bioconjugates with phosphatidylcholine have a significant impact on the physico-chemical properties of a membrane and cause a decrease in the temperature of the main phase transition. The consequence of this is greater fluidity of the lipid bilayer.

Highlights

  • Liposomes have been extensively investigated as effective drug delivery systems (DDS) since 1965, when they were introduced for the first time by Alec Bangham et al [1]

  • differential scanning calorimetry (DSC) is a fundamental technique used for obtaining a precise determination of thermodynamic parameters during structural changes or phase transitions in lipid bilayers

  • In the spectrum of liposomes formed from DPPC and the conjugates of phosphatidylcholine with p-anisic acid, we considered a thermotropic behavior in characteristic regions, namely the hydrocarbon chains, the interface region and the head group

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Summary

Introduction

Liposomes have been extensively investigated as effective drug delivery systems (DDS) since 1965, when they were introduced for the first time by Alec Bangham et al [1] Their unique properties, including biocompatibility and biodegradability, as well as their physiochemical nature, make them excellent vesicles for both hydrophilic and hydrophobic molecules [2]. Research on liposome technology progressed during the following decades from conventional vesicles (“first-generation liposomes”) to “second-generation liposomes” which were obtained by modulating the lipid composition, size and charge of the vesicles. This strategy, based on the modification of a chemical surface of liposomes by incorporating specific molecules or macromolecules, Int. J.

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