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AAPS PharmSciTech

, Volume 19, Issue 7, pp 2971–2989 | Cite as

Development and Evaluation of Stimuli-Responsive Chimeric Nanostructures

  • Nikolaos Naziris
  • Natassa Pippa
  • Dimitris Stellas
  • Varvara Chrysostomou
  • Stergios Pispas
  • Costas Demetzos
  • Marcin Libera
  • Barbara Trzebicka
Research Article
  • 63 Downloads

Abstract

Chimeric/mixed stimuli-responsive nanocarriers are promising agents for therapeutic and diagnostic applications, as well as in the combinatorial field of theranostics. Herein, we designed chimeric nanosystems, composed of natural phospholipid and pH-sensitive amphiphilic diblock copolymer, in different molar ratios and assessed the polymer lyotropic effect on their properties. Initially, polymer-grafted bilayers were evaluated for their thermotropic behavior by thermal analysis. Chimeric liposomes were prepared through thin-film hydration and the obtained vesicles were studied by light scattering techniques, to measure their physicochemical characteristics and colloidal stability, as well as by imaging techniques, to elucidate their global and membrane morphology. Finally, in vitro screening of the systems’ toxicity was held. The copolymer effect on the membrane phase transition strongly depended on the pH of the surrounding environment. Chimeric nanoparticles were around and above 100 nm, while electron microscopy revealed occasional morphology diversity, probably affecting the toxicity of the systems. The latter was assessed to be tolerable, while dependent on the nanosystems’ material concentration, polymer concentration, and polymer composition. All experiments suggested that the thermodynamic and biophysical properties of the nanosystems are copolymer-composition- and concentration-dependent, since different amounts of incorporated polymer would produce divergent effects on the lyotropic liquid crystal membrane. Certain chimeric systems can be exploited as advanced drug delivery nanosystems, based on their overall promising profiles.

KEY WORDS

chimeric nanosystems amphiphilic biomaterials lyotropism pH-responsive biophysics 

Notes

Funding Information

This research has been financially supported by the General Secretariat for Research and Technology (GSRT) and the Hellenic Foundation for Research and Innovation (HFRI) (Scholarship Code: 392).

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

Supplementary material

12249_2018_1112_MOESM1_ESM.docx (202 kb)
ESM 1 The stability evaluation of polydispersity, as well as diameters and wall dimensions extracted by cryo-TEM for the prepared chimeric nanosystems are provided in the supplementary material section. (DOCX 201 kb)

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Nikolaos Naziris
    • 1
  • Natassa Pippa
    • 1
    • 2
  • Dimitris Stellas
    • 3
    • 4
  • Varvara Chrysostomou
    • 2
  • Stergios Pispas
    • 2
  • Costas Demetzos
    • 1
  • Marcin Libera
    • 5
  • Barbara Trzebicka
    • 5
  1. 1.Section of Pharmaceutical Technology, Department of Pharmacy, School of Health SciencesNational and Kapodistrian University of AthensAthensGreece
  2. 2.Theoretical and Physical Chemistry InstituteNational Hellenic Research FoundationAthensGreece
  3. 3.Biomedical Research FoundationAcademy of AthensAthensGreece
  4. 4.Vaccine Branch, Center for Cancer Research, National Cancer InstituteNational Institutes of HealthFrederickUSA
  5. 5.Centre of Polymer and Carbon MaterialsPolish Academy of SciencesZabrzePoland

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