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Special Issue "Liposomal and Lipid-Based Drug Delivery Systems and Vaccines"

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (28 February 2023) | Viewed by 6239

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Special Issue Editor

Dr. Elena L. Vodovozova

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Guest Editor

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, Moscow, Russia
Interests: liposomes; lipid-based formulations; drug delivery; lipid chemistry; synthesis; lipophilic prodrugs; vaccines; immunotherapy

Special Issue Information

Dear Colleagues,

After the discovery of liposomes by Bangham in the early 1960s, they have been explored extensively, both as vehicles for drug delivery and as adjuvant carriers in vaccinology, starting from the first works by Gregoriadis, Ryman, and Allison in the 1970s. The advantage of liposomal and related lipid-based formulations lies in their flexibility, high biocompatibility, and multifunctionality. Nowadays, along with significant successes in the production and clinical implementation of traditional small molecule drugs in liposomal formulations for the treatment of oncological diseases, the first lipid-based formulations for gene therapy are being introduced in clinics. Finally, against the background of pandemic challenges, it is noteworthy to cite Gregory Gregoriadis, “that it took fifty or so years for the two technologies, mRNA and lipid vesicles, to come together at more or less the same time of their need” (https://doi.org/10.1016/j.medidd.2021.100104).

This Special Issue is addressed to those authors who are currently engaged in research on the use of liposomes, lipid nanoparticles (non-vesicular supramolecular systems, as opposed to classical liposomes), and other lipid-based formulations for the development of drug delivery systems and vaccines. The issue is aimed at considering a wide variety of the aspects surrounding the creation and characterization of lipid-based formulations (structural and functional), including delivery systems for small molecule drugs, peptides, oligonucleotides, aptamers, proteins, antibodies, and nucleic acid molecules. Systems for the targeted delivery of therapeutic agents, both to organs and tissues and to intracellular organelles, will also be considered in the scope. The undesirable effects mediated by the immune system in response to the introduction of lipid-based formulations (such as hypersensitivity reactions and others) and the mechanisms of their emergence will also be addressed.

Dr. Elena L. Vodovozova
Guest Editor

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Keywords

liposomes
lipid nanoparticles
lipid-based formulations
drug delivery
gene delivery
mRNA and saRNA
vaccines
immunotherapy
nanomedicine

Published Papers (7 papers)

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Research

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Open AccessArticle

Multicomponent Lipid Nanoparticles for RNA Transfection

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Pharmaceutics 2023, 15(4), 1289; https://doi.org/10.3390/pharmaceutics15041289 - 20 Apr 2023

Viewed by 618

Abstract

Despite the wide variety of available cationic lipid platforms for the delivery of nucleic acids into cells, the optimization of their composition has not lost its relevance. The purpose of this work was to develop multi-component cationic lipid nanoparticles (LNPs) with or without a hydrophobic core from natural lipids in order to evaluate the efficiency of LNPs with the widely used cationic lipoid DOTAP (1,2-dioleoyloxy-3-[trimethylammonium]-propane) and the previously unstudied oleoylcholine (Ol-Ch), as well as the ability of LNPs containing GM3 gangliosides to transfect cells with mRNA and siRNA. LNPs containing cationic lipids, phospholipids and cholesterol, and surfactants were prepared according to a three-stage procedure. The average size of the resulting LNPs was 176 nm (PDI 0.18). LNPs with DOTAP mesylate were more effective than those with Ol-Ch. Core LNPs demonstrated low transfection activity compared with bilayer LNPs. The type of phospholipid in LNPs was significant for the transfection of MDA-MB-231 and SW 620 cancer cells but not HEK 293T cells. LNPs with GM3 gangliosides were the most efficient for the delivery of mRNA to MDA-MB-231 cells and siRNA to SW620 cells. Thus, we developed a new lipid platform for the efficient delivery of RNA of various sizes to mammalian cells. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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Open AccessArticle

HER2/neu Oncogene Silencing in a Breast Cancer Cell Model Using Cationic Lipid-Based Delivery Systems

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Pharmaceutics 2023, 15(4), 1190; https://doi.org/10.3390/pharmaceutics15041190 - 08 Apr 2023

Viewed by 684

Abstract

The overexpression of the human epidermal growth factor 2 (HER2/neu) oncogene is predictive of adverse breast cancer prognosis. Silencing the HER2/neu overexpression using siRNA may be an effective treatment strategy. Major requirements for siRNA-based therapy are safe, stable, and efficient delivery systems to channel siRNA into target cells. This study assessed the efficacy of cationic lipid-based systems for the delivery of siRNA. Cationic liposomes were formulated with equimolar ratios of the respective cholesteryl cytofectins, 3β-N-(N′, N′-dimethylaminopropyl)-carbamoyl cholesterol (Chol-T) or N, N-dimethylaminopropylaminylsuccinylcholesterylformylhydrazide (MS09), with the neutral helper lipid, dioleoylphosphatidylethanolamine (DOPE), with and without a polyethylene glycol stabilizer. All cationic liposomes efficiently bound, compacted, and protected the therapeutic siRNA against nuclease degradation. Liposomes and siRNA lipoplexes were spherical, <200 nm in size, with moderate particle size distributions (PDI < 0.4). The siRNA lipoplexes exhibited minimal dose-dependent cytotoxicity and effective HER2/neu siRNA transfection in the HER2/neu overexpressing SKBR-3 cells. The non-PEGylated Chol-T-siRNA lipoplexes induced the highest HER2/neu silencing at the mRNA (10000-fold decrease) and protein levels (>111.6-fold decrease), surpassing that of commercially available Lipofectamine 3000 (4.1-fold reduction in mRNA expression). These cationic liposomes are suitable carriers of HER2/neu siRNA for gene silencing in breast cancer. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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Open AccessArticle

Efficient mRNA Delivery with mRNA Lipoplexes Prepared Using a Modified Ethanol Injection Method

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Pharmaceutics 2023, 15(4), 1141; https://doi.org/10.3390/pharmaceutics15041141 - 04 Apr 2023

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Abstract

Messenger RNA (mRNA)-based therapies are a novel class of therapeutics used in vaccination and protein replacement therapies for monogenic diseases. Previously, we developed a modified ethanol injection (MEI) method for small interfering RNA (siRNA) transfection, in which cationic liposome/siRNA complexes (siRNA lipoplexes) were prepared by mixing a lipid-ethanol solution with a siRNA solution. In this study, we applied the MEI method to prepare mRNA lipoplexes and evaluated the in vitro and in vivo protein expression efficiencies. We selected six cationic lipids and three neutral helper lipids to generate 18 mRNA lipoplexes. These were composed of cationic lipids, neutral helper lipids, and polyethylene glycol-cholesteryl ether (PEG-Chol). Among them, mRNA lipoplexes containing N-hexadecyl-N,N-dimethylhexadecan-1-aminium bromide (DC-1-16) or 11-((1,3-bis(dodecanoyloxy)-2-((dodecanoyloxy)methyl) propan-2-yl) amino)-N,N,N-trimethyl-11-oxoundecan-1-aminium bromide (TC-1-12) with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) and PEG-Chol exhibited high protein expression in cells. Furthermore, mRNA lipoplexes composed of DC-1-16, DOPE, and PEG-Chol exhibited high protein expression in the lungs and spleen of mice after systemic injection and induced high antigen-specific IgG1 levels upon immunization. These results suggest that the MEI method can potentially increase the efficiency of mRNA transfection, both in vitro and in vivo. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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Open AccessArticle

Liposomal Forms of Fluoroquinolones and Antifibrotics Decorated with Mannosylated Chitosan for Inhalation Drug Delivery

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Pharmaceutics 2023, 15(4), 1101; https://doi.org/10.3390/pharmaceutics15041101 - 29 Mar 2023

Viewed by 548

Abstract

The severe course of COVID-19 leads to the long-terming pulmonary diseases, such as bacterial pneumonia and post-COVID-19 pulmonary fibrosis. Thus, the essential task of biomedicine is a design of new effective drug formulations, including those for inhalation administration. In this work, we propose an approach to the creation of lipid–polymer delivery systems for fluoroquinolones and pirfenidone based on liposomes of various compositions decorated with mucoadhesive mannosylated chitosan. A generalizing study on the physicochemical patterns of the interactions of drugs with bilayers of various compositions was carried out, and the main binding sites were identified. The role of the polymer shell in the stabilization of vesicles and the delayed release of the contents has been demonstrated. For the liquid–polymer formulation of moxifloxacin, a prolonged accumulation of the drug in lung tissues was found after a single endotracheal administration to mice, significantly exceeding the control intravenous and endotracheal administration of the drug. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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Open AccessArticle

Influence of Lipid Composition of Cationic Liposomes 2X3-DOPE on mRNA Delivery into Eukaryotic Cells

Vera Vysochinskaya

Sergey Shishlyannikov

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Pharmaceutics 2023, 15(1), 8; https://doi.org/10.3390/pharmaceutics15010008 - 20 Dec 2022

Viewed by 1377

Abstract

The design of cationic liposomes for efficient mRNA delivery can significantly improve mRNA-based therapies. Lipoplexes based on polycationic lipid 1,26-bis(cholest-5-en-3β-yloxycarbonylamino)-7,11,16,20-tetraazahexacosane tetrahydrochloride (2X3) and helper lipid 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) were formulated in different molar ratios (1:1, 1:2, 1:3) to efficiently deliver model mRNAs to BHK-21 and A549. The objective of this study was to examine the effect of 2X3-DOPE composition as well as lipid-to-mRNA ratio (amino-to-phosphate group ratio, N/P) on mRNA transfection. We found that lipoplex-mediated transfection efficiency depends on both liposome composition and the N/P ratio. Lipoplexes with an N/P ratio of 10/1 showed nanometric hydrodynamic size, positive ζ potential, maximum loading, and transfection efficiency. Liposomes 2X3-DOPE (1:3) provided the superior delivery of both mRNA coding firefly luciferase and mRNA-eGFP into BHK-21 cells and A549 cells, compared with commercial Lipofectamine MessengerMax. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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Open AccessArticle

Oxime Therapy for Brain AChE Reactivation and Neuroprotection after Organophosphate Poisoning

Alexandra D. Voloshina

Konstantin A. Petrov

Lucia Y. Zakharova

and

Oleg G. Sinyashin

Pharmaceutics 2022, 14(9), 1950; https://doi.org/10.3390/pharmaceutics14091950 - 15 Sep 2022

Cited by 4 | Viewed by 1158

Abstract

One of the main problems in the treatment of poisoning with organophosphorus (OPs) inhibitors of acetylcholinesterase (AChE) is low ability of existing reactivators of AChE that are used as antidotes to cross the blood-brain barrier (BBB). In this work, modified cationic liposomes were developed that can penetrate through the BBB and deliver the reactivator of AChE pralidoxime chloride (2-PAM) into the brain. Liposomes were obtained on the basis of phosphatidylcholine and imidazolium surfactants. To obtain the composition optimized in terms of charge, stability, and toxicity, the molar ratio of surfactant/lipid was varied. For the systems, physicochemical parameters, release profiles of the substrates (rhodamine B, 2-PAM), hemolytic activity and ability to cause hemagglutination were evaluated. Screening of liposome penetration through the BBB, analysis of 2-PAM pharmacokinetics, and in vivo AChE reactivation showed that modified liposomes readily pass into the brain and reactivate brain AChE in rats poisoned with paraoxon (POX) by 25%. For the first time, an assessment was made of the ability of imidazolium liposomes loaded with 2-PAM to reduce the death of neurons in the brains of mice. It was shown that intravenous administration of liposomal 2-PAM can significantly reduce POX-induced neuronal death in the hippocampus. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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Review

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Open AccessReview

Design of Folate-Containing Liposomal Nucleic Acid Delivery Systems for Antitumor Therapy

Elena V. Shmendel

Pavel A. Puchkov

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Michael A. Maslov

Pharmaceutics 2023, 15(5), 1400; https://doi.org/10.3390/pharmaceutics15051400 - 03 May 2023

Viewed by 603

Abstract

The delivery of therapeutic nucleic acids is a prospective method for the treatment of both inherited and acquired diseases including cancer. To achieve maximal delivery efficiency and selectivity, nucleic acids should be targeted to the cells of interest. In the case of cancer, such targeting may be provided through folate receptors overexpressed in many tumor cells. For this purpose, folic acid and its lipoconjugates are used. Compared to other targeting ligands, folic acid provides low immunogenicity, rapid tumor penetration, high affinity to a wide range of tumors, chemical stability, and easy production. Different delivery systems can utilize targeting by folate ligand including liposomal forms of anticancer drugs, viruses, and lipid and polymer nanoparticles. This review focuses on the liposomal gene delivery systems that provide targeted nucleic acid transport into tumor cells due to folate lipoconjugates. Moreover, important development step, such as rational design of lipoconjugates, folic acid content, size, and ζ-potential of lipoplexes are discussed. Full article

(This article belongs to the Special Issue Liposomal and Lipid-Based Drug Delivery Systems and Vaccines)

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