Enhanced Liposomal Drug Delivery Via Membrane Fusion Triggered by Dimeric Coiled-Coil Peptides.

cell-liposome membrane fusion coiled-coil peptide drug delivery membranes peptide-membrane interactions

Journal

Small (Weinheim an der Bergstrasse, Germany)
ISSN: 1613-6829
Titre abrégé: Small
Pays: Germany
ID NLM: 101235338

Informations de publication

Date de publication:
09 2023
Historique:
revised: 06 04 2023
received: 08 02 2023
medline: 14 9 2023
pubmed: 18 5 2023
entrez: 18 5 2023
Statut: ppublish

Résumé

An ideal nanomedicine system improves the therapeutic efficacy of drugs. However, most nanomedicines enter cells via endosomal/lysosomal pathways and only a small fraction of the cargo enters the cytosol inducing therapeutic effects. To circumvent this inefficiency, alternative approaches are desired. Inspired by fusion machinery found in nature, synthetic lipidated peptide pair E4/K4 is used to induce membrane fusion previously. Peptide K4 interacts specifically with E4, and it has a lipid membrane affinity and resulting in membrane remodeling. To design efficient fusogens with multiple interactions, dimeric K4 variants are synthesized to improve fusion with E4-modified liposomes and cells. The secondary structure and self-assembly of dimers are studied; the parallel PK4 dimer forms temperature-dependent higher-order assemblies, while linear K4 dimers form tetramer-like homodimers. The structures and membrane interactions of PK4 are supported by molecular dynamics simulations. Upon addition of E4, PK4 induced the strongest coiled-coil interaction resulting in a higher liposomal delivery compared to linear dimers and monomer. Using a wide spectrum of endocytosis inhibitors, membrane fusion is found to be the main cellular uptake pathway. Doxorubicin delivery results in efficient cellular uptake and concomitant antitumor efficacy. These findings aid the development of efficient delivery systems of drugs into cells using liposome-cell fusion strategies.

Identifiants

pubmed: 37199140
doi: 10.1002/smll.202301133
doi:

Substances chimiques

Liposomes 0
Peptides 0
Polymers 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e2301133

Informations de copyright

© 2023 The Authors. Small published by Wiley-VCH GmbH.

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Auteurs

Ye Zeng (Y)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

Mengjie Shen (M)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

Ankush Singhal (A)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

Geert Jan Agur Sevink (GJA)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

Niek Crone (N)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

Aimee L Boyle (AL)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

Alexander Kros (A)

Dept. Supramolecular & Biomaterials Chemistry, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.

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