Design of lipid-based formulations for oral delivery of a BASP1 peptide targeting MYC-dependent gastrointestinal cancer cells

Abstract

Conclusion

Myr-NT can be efficiently delivered into intestinal tumor cells using orally administered lipid-based formulations.

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Materials

Fluorescently-labelled Myr-NT (myristoyl-GGKLSKKKKGK-TAMRA-COOH, Mr = 1780.6) and the unlabelled Myr-NT peptide (myristoyl-GGKLSKKKKG-OH, Mr = 1240.3) were commercially synthesized by the company PANATecs (Heilbronn, Germany). Lumogen Yellow (LGY) was a gift from BASF (Ludwigshafen, Germany). Lyso-Phosphatidylcholin was a gift from Lipoid GmbH (Ludwigshafen, Germany). Glyceryl monocaprylate (trade name: Capmul MCM C8) was provided as a free sample from Abitec Corporation (Columbus, OH, USA). Propylene glycol monocaprylate (trade name: Capryol 90) was a free sample from Gattefossé SAS (Lyon, France). Propylene glycol dicaprylate/dicaprate (trade name: Miglyol 840) was kindly donated by IOI Oleo GmbH (Hamburg, Germany).

Human erythrocyte concentrate was kindly provided by Tirol Kliniken GmbH (Innsbruck, Austria). Docusate sodium (DS) and soybean oil were purchased from Alfa Aesar (Kandel, Germany). Opti-MEM was obtained from Thermo Fisher Scientific (Vienna, Austria). Hoechst 33528 was purchased from Santa Cruz Biotechnology (Dallas, TX, USA). Acetonitrile (ACN), calcium chloride (CaCl2), dimethyl sulfoxide (DMSO), glucose anhydrous, 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), isopropylmyristate, methanol, octanol, PEG (20) – sorbitan monooleate (trade name: Tween 80), PEG (35) – castor oil (trade name: Kolliphor EL), potassium chloride (KCl), sodium chloride (NaCl), sodium dodecyl sulfate (SDS), sodium dodecyl benzene sulfonate (SDBS), trifluoroacetic acid (TFA), tris(hydroxymethyl)aminomethane (TRIS), trypsin from porcine pancreas (0.1 mg/mL) and Triton X-100 were purchased from Sigma-Aldrich (Vienna, Austria).

DPBS and the cell culture media DMEM, RPMI, and Leibovitz’s L-15 medium were purchased from PAN-Biotech (Aidenbach, Germany). Trypsin-EDTA (0.25 %) and glutamine were purchased from Life Technologies (Carlsbad, CA, USA), and Eximus Fetal Bovine Serum (FBS) from Catus Biotech (Tutzing, Germany). Glutaraldehyde was obtained from Merck (Darmstadt, Germany), and acrylamide (Rotiphorese) from Carl Roth (Karlsruhe, Germany).

Dennis To, Christian Steinbring, Leonie I. Weber, Fabrizio Ricci, Ilaria Polidori, Annika Postina, Markus Hartl, Andreas Bernkop-Schnürch, Design of lipid-based formulations for oral delivery of a BASP1 peptide targeting MYC-dependent gastrointestinal cancer cells, Journal of Controlled Release, Volume 382, 2025, 113677, ISSN 0168-3659, https://doi.org/10.1016/j.jconrel.2025.113677.

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