Issue 2, 2024

Insight into the liposomal encapsulation of mono and bis-naphthalimides

Abstract

Mitonafide-loaded liposomes are a promising strategy to overcome the neurotoxicity observed in clinical trials for this drug. This study investigates the influence of loaded mitonafide or a dimer analogue on different liposomal formulations and their therapeutic efficacy in vitro. Physicochemical properties of the liposomes were manipulated using different loading methods (namely bilayer or core loading) and varying the rigidity of the bilayer using distinct phospholipid compositions. Our results demonstrated that the mitonafide dimer analogue had a comparable encapsulation efficiency (EE%) into the liposomes when loaded into rigid or flexible bilayers in contrast to the low mitonafide monomer EE%. A pH gradient core loading method resulted in a more efficient mechanism to load the monomer into the liposomes. DOSY NMR and spectrofluorometric studies revealed key differences in the structure of the vesicles and the arrangement of the monomer or the dimer in the bilayer or the core of the liposomes. The in vitro assessment of the formulations using MDA-MB-231 and RT-112 cells revealed that a flexible lipid bilayer allows a faster drug release, which correlated well with the spectroscopy studies. This study investigated for the first time that the characteristics of the lipid bilayer and the loading method influence the encapsulation efficacy, colloidal properties, photoactivity and stability of mono and bis-naphthalimides loaded in a liposomal carrier, essential factors that will impact the performance of the formulation in a biological scenario.

Graphical abstract: Insight into the liposomal encapsulation of mono and bis-naphthalimides

Supplementary files

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Article information

Article type
Paper
Submitted
01 Dec 2023
Accepted
25 Feb 2024
First published
08 Mar 2024
This article is Open Access
Creative Commons BY license

RSC Pharm., 2024,1, 272-282

Insight into the liposomal encapsulation of mono and bis-naphthalimides

A. M. Dauda, T. Swift, R. Telford, H. A. A. Abd El-wahab, C. C. Danta, K. Pors and A. Ruiz, RSC Pharm., 2024, 1, 272 DOI: 10.1039/D3PM00060E

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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