Application of solid lipid nanoparticles as a long-term drug delivery platform for intramuscular and subcutaneous administration: In vitro and in vivo evaluation

Kimberley Elbrink, Sofie Van Hees, Ronnie Chamanza, Dirk Roelant, Tine Loomans, René Holm, Filip Kiekens*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

The purpose of this work was to evaluate solid lipid nanoparticles (SLNs) as a long acting injectable drug delivery platform for intramuscular and subcutaneous administration. SLNs were developed with a low (unsaturated) and high (supersaturated) drug concentration at equivalent lipid doses. The impact of the drug loading as well as the administration route for the SLNs using two model compounds with different physicochemical properties were explored for their in vitro and in vivo performance. Results revealed that drug concentration had an influence on the particle size and entrapment efficiency of the SLNs and, therefore, indirectly an influence on the Cmax/dose and AUC/dose after administration to rats. Furthermore, the in vitro drug release was compound specific, and linked to the affinity of the drug compounds towards the lipid matrix and release medium. The pharmacokinetic parameters resulted in an increased tmax, t1/2 and mean residence time (MRT) for all formulations after intramuscular and subcutaneous dosing, when compared to intravenous administration. Whereas, the subcutaneous injections performed better for those parameters than the intramuscular injections, because of the higher blood perfusion in the muscles compared with the subcutaneous tissues. In conclusion, SLNs extend drug release, need to be optimized for each drug, and are appropriate carriers for the delivery of drugs that require a short-term sustained release in a timely manner.

Original languageEnglish
JournalEuropean journal of pharmaceutics and biopharmaceutics
Volume163
Pages (from-to)158-170
Number of pages13
ISSN0939-6411
DOIs
Publication statusPublished - Jun 2021
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2021 Elsevier B.V.

Keywords

  • Bedaquiline
  • Celecoxib
  • Intramuscular and subcutaneous administration
  • Pharmacokinetic behavior
  • Solid lipid nanoparticles
  • Sustained release

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