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  2. Navigating the challenges of lipid nanoparticle formulation: the role of unpegylated lipid surfactants in enhancing drug loading and stability

Navigating the challenges of lipid nanoparticle formulation: the role of unpegylated lipid surfactants in enhancing drug loading and stability

  • Nanoscale Adv. 2023 Dec 18;6(2):669-679. doi: 10.1039/d3na00484h.
Cameron Hogarth 1 Keith Arnold 2 Steve Wright 1 Heba Elkateb 1 Steve Rannard 1 2 Tom O McDonald 1 3 4
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Liverpool Crown Street Liverpool L69 7ZD UK.
  • 2 Material Innovation Factory, University of Liverpool Liverpool L7 3NY UK.
  • 3 Department of Materials, The University of Manchester Oxford Road Manchester M13 9PL UK Thomas.mcdonald@manchester.ac.uk.
  • 4 Henry Royce Institute, The University of Manchester Oxford Road Manchester UK.
Abstract

Lipid nanoparticles have proved an attractive approach for drug delivery; however, the challenges of optimising formulation stability and increasing drug loading have limited progression. In this work, we investigate the role of unpegylated lipid Surfactants (helper lipids) in nanoparticle formation and the effect of blending helper lipids with pegylated lipid Surfactants on the formation and stability of lipid-based nanoparticles by nanoprecipitation. Furthermore, blends of unpegylated/pegylated lipid Surfactants were examined for ability to accommodate higher drug loading formulations by means of a higher weight percentage (wt%) of drug relative to total mass of formulation components (i.e. drug, Surfactants and lipids). Characterisation included evaluation of particle diameter, size distribution, drug loading and nanoformulation stability. Our findings demonstrate that the addition of unpegylated lipid surfactant (Lipoid S100) to pegylated lipid surfactant (Brij S20) enhances stability, particularly at higher weight percentages of the core material. This blending approach enables drug loading capacities exceeding 10% in the lipid nanoparticles. Notably, Lipoid S100 exhibited nucleating properties that aided in the formation and stabilisation of the nanoparticles. Furthermore, we examined the incorporation of a model drug into the lipid nanoparticle formulations. Blending the model drug with the core material disrupted the crystallinity of the core, offering additional potential benefits in terms of drug release and stability. This comprehensive investigation provides valuable insights into the interplay between surfactant properties, core material composition, and nanoparticle behaviour. The study enhances our understanding of lipid Materials and offers guidance for the design and optimisation of lipid nanoparticle formulations.

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