The Interplay between Liposomal Composition, Stability and Biological Properties

Authors

  • Marina Zoupa Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupolis Zografou, 15771 Athens, Greece
  • Nikolaos Naziris Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupolis Zografou, 15771 Athens, Greece and Department of General Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143, 90-236 Lodz, Poland
  • Clotilde Lauro Department of Physiology and Pharmacology, Laboratory Affiliated to Istituto Pasteur Italia, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy
  • Cristina Limatola Department of Physiology and Pharmacology, Laboratory Affiliated to Istituto Pasteur Italia, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy and IRCCS Neuromed, Via Atinense 18, 86077 Pozzilli, Italy
  • Costas Demetzos Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupolis Zografou, 15771 Athens, Greece

DOI:

https://doi.org/10.31437/2309-4435.2021.09.2

Keywords:

Liposomes, Composition, Physicochemical properties, Stability, Lyophilization, Protein interactions, Cytotoxicity

Abstract

Liposomes are nanoparticles that belong to the class of drug delivery systems. They are widely utilized in medicine for the controlled and targeted delivery of therapeutic and diagnostic molecules. In the present study, our aim was to develop different types of liposomal nanoparticles, evaluate their physicochemical properties, stability, interaction with serum proteins and assess their cytotoxic effect on GL261 glioma cells. Conventional, anionic, cationic and PEGylated liposomes were developed, by using L-?-phosphatidylcholine, hydrogenated (Soy) (HSPC), cholesterol (CHOL), 1,2-dipalmitoyl-sn-glycero-3-phospho-(1’-rac-glycerol) (DPPG) (for anionic particles), 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) (for cationic particles) and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-5000] (DPPE-mPEG5000 particles) (for PEGylated particles). Physicochemical studies revealed the interplay between the liposomal composition and their resultant properties and stability, while all formulations were stable during and after lyophilization. Concerning protein interactions, positively charged liposomes were particularly susceptible to those, as it was evident from the alteration in their physicochemical properties. Finally, in vitro toxicity on cells was dependent on the type and concentration of the liposomes utilized, with cationic nanoparticles being the most toxic. The herein presented studies and results can be a roadmap to the development of liposomal nanosystems that will be efficient, stable and biocompatible nanocarriers for the delivery of drug molecules or other therapeutics.

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Published

2021-11-22

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