Abstract

Advanced theranostic nanomedicine is a multifunctional approach which combines the diagnosis and effective therapy of diseased tissues. Here, we investigated the preparation, characterization and in vitro evaluation of theranostic liposomes. As is known, liposome–quantum dot (L–QD) hybrid vesicles are promising nanoconstructs for cell imaging and liposomal-topotecan (L-TPT) enhances the efficiency of TPT by providing protection against systemic clearance and allowing extended time for it to accumulate in tumors. In the present study, hydrophobic CdSe/ZnS QD and TPT were located in the bilayer membrane and inner core of liposomes, respectively. Dynamic light scattering (DLS), zeta potential (ζ) measurements and fluorescence/absorption spectroscopy were performed to determine the vesicle size, charge and spectroscopic properties of the liposomes. Moreover, drug release was studied under neutral and acidic pH conditions. Fluorescence microscopy and flow cytometry analysis were used to examine the cellular uptake and intracellular distribution of the TPT-loaded L–QD formulation. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was utilized to investigate the in vitro cytotoxicity of the formulations on HeLa cells. According to the results, the TPT-loaded L–QD hybrid has adequate physicochemical properties and is a promising multifunctional delivery vehicle which is capable of a simultaneous co-delivery of therapeutic and diagnostic agents.

Highlights

  • Nanomedicine is an innovative field with enormous potential for treatment by a combination of smart nanoparticles with small molecules carrying a wide range of functions [1]

  • Liposome–quantum dot (L–Quantum dots (QDs)) hybrid vesicles are promising nanoconstructs for cell imaging and liposomal-topotecan (L-TPT) enhances the efficiency of TPT by providing protection against systemic clearance and allowing extended time for it to accumulate in tumors

  • Apomorphine and QDs were integrated into multifunctional liposomes for brain targeting and bioimaging and the results showed that these liposomes can be accumulated to a large extent in the brain [18]

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Summary

Introduction

Nanomedicine is an innovative field with enormous potential for treatment by a combination of smart nanoparticles with small molecules carrying a wide range of functions [1]. Quantum dots (QDs) are one of the promising nanoparticles with excellent fluorescence properties, including broad absorption spectra, narrow emission spectra, high quantum yields, resistance to photobleaching, and high photochemical stability [2,3,4] Due to these characteristics, they have been explored as fluorescent probes for biomedical applications and are useful in particular for in vivo cell labeling and imaging [5,6,7,8]. The aim was to develop multifunctional theranostic liposomes which contain both the model drug TPT and QDs for cell therapy and imaging For this purpose, L–QD hybrids were synthesized by the incorporation of hydrophobic QD within the lipid bilayer. TPT therapeutic activity and QD optical properties could be successfully integrated into one nanocarrier

Synthesis and Characterization of TPT-Loaded Liposomal Formulations
Encapsulation Efficiency
Characterization
In Vitro Drug Release
Cell Culture
Cytotoxicity
Cellular Uptake and Internalization
Conclusions
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