Lipid-based colloidal carriers for peptide and protein delivery – liposomes versus lipid nanoparticles

Susana Martins¹, Bruno Sarmento¹, Domingos C Ferreira¹, Eliana B Souto^1,2

¹Department of Pharmaceutical Technology, Faculty of Pharmacy University of Porto, Porto, Portugal; ²Faculty of Health Sciences, Fernando Pessoa University, Porto, Portugal

Abstract: This paper highlights the importance of lipid-based colloidal carriers and their pharmaceutical implications in the delivery of peptides and proteins for oral and parenteral administration. There are several examples of biomacromolecules used nowadays in the therapeutics, which are promising candidates to be delivered by means of liposomes and lipid nanoparticles, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). Several production procedures can be applied to achieve a high association efficiency between the bioactives and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. Generally, this can lead to improved bioavailability, or in case of oral administration a more consistent temporal profile of absorption from the gastrointestinal tract. Advantages and drawbacks of such colloidal carriers are also pointed out. This article describes strategies used for formulation of peptides and proteins, methods used for assessment of association efficiency and practical considerations regarding the toxicological concerns.

Keywords: peptides, proteins, liposomes, solid lipid nanoparticles, SLN, nanostructured lipid carriers, NLC, oral, parenteral