pH-responsive chimeric liposomes : from nanotechnology to biological assessment

The utilization of liposomes in biomedical applications has greatly benefited the diagnosis and treatment of various diseases. These biomimetic nano-entities have been very useful in the clinical practice as drug delivery systems in their conventional form, comprising lipids as structural components. However, the scientific efforts have recently shifted towards the development of more sophisticated nanotechnological platforms, which apply functional biomaterials, such as stimuli-responsive polymers, in order to aid the drug molecule targeting concept. These nanosystems are defined as chimeric/mixed, because they combine more than one different in nature biomaterials and their development requires intensive study through biophysical and thermodynamic approaches before they may reach in vivo application. Herein, we designed and developed chimeric liposomes, composed of a phospholipid and pH-responsive amphiphilic diblock copolymers and studied their morphology and their behavior based on crucial formulation parameters, including biomaterial concentration, dispersion medium pH and polymer composition. Additionally, their interactions with biological components, pH-responsiveness and membrane thermodynamics were also assessed. Finally, preliminary in vivo toxicity experiments of the developed nanosystems were carried out, in order to establish a future protocol for full in vivo evaluation. The results have been correlated with the properties of the chimeric nanosystems and highlight the importance of such approaches for designing and developing effective nanocarriers for biomedical applications.