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Lipid-Based Drug Carriers and Nanoparticles
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Lipid-Based Drug Carriers and Nanoparticles

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (31 May 2021) | Viewed by 25068

Special Issue Editors

Prof. Dr. Brian S. Cummings

E-Mail Website
Guest Editor
The University of Georgia, Athens, GA, USA
Interests: lipids; liposomes; lipidomics; phospholipases; prostate cancer
Dr. Robert D Arnold

E-Mail Website
Guest Editor
Auburn University, Auburn, AL, USA
Interests: cancer therapeutics; nanomedicine; pharmaceutics; drug delivery

Special Issue Information

Dear Colleagues,

Lipid-based delivery systems play critical roles in the delivery of therapeutic and diagnostic agents. Their popularity arises from their ability to improve drug delivery by improving drug stability and by altering pharmacokinetic parameters (ADME; absorption, distribution, metabolism and elimination). This allows lipid-based carriers to achieve exposure profiles not possible with free drugs. Further, the addition of diagnostic agents has allowed lipid-based carriers to assist in non-invasively tracking drug disposition and disease progression. Advances in molecular biology have identified targeting ligands that provide greater selectivity and improved cellular uptake. Despite these advances, several gaps in knowledge, as well as barriers, exist for lipid-based carriers. This includes knowledge of their biologic disposition, long-term toxicity, targeting specificity and issues with their large-scale production, stability, and their disposition in the environment. Further, while lipid-based carriers have enjoyed enhanced use in the laboratory, their use in the clinic is comparatively somewhat limited. This Special Issue on lipid-based delivery focuses on these issues, as well as on the diversity of platforms for generation of these carriers and their pharmaceutical and diagnostic applications.

Prof. Dr. Brian S. Cummings
Dr. Robert D Arnold
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • lipid
  • drug delivery
  • molecular imaging
  • nanomedicine
  • therapeutics
  • pharmaceutical

Published Papers (4 papers)

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Research

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25 pages, 9516 KiB  
Article
The Process of Binding and Releasing of Genetic Material from Lipoplexes Based on Trimeric Surfactants and Phospholipids
by Żaneta Polańska, Zuzanna Pietralik-Molińska, Daria Wojciechowska, Augustyn Moliński, Marek Weiss, Andrzej Skrzypczak and Maciej Kozak
Int. J. Mol. Sci. 2021, 22(14), 7744; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22147744 - 20 Jul 2021
Cited by 1 | Viewed by 1989
Abstract
Nonviral vectors for gene therapy such as lipoplexes are characterized by low toxicity, high biocompatibility, and good transfection efficiency. Specifically, lipoplexes based on polymeric surfactants and phospholipids have great potential as gene carriers due to the increased ability to bind genetic material (multiplied [...] Read more.
Nonviral vectors for gene therapy such as lipoplexes are characterized by low toxicity, high biocompatibility, and good transfection efficiency. Specifically, lipoplexes based on polymeric surfactants and phospholipids have great potential as gene carriers due to the increased ability to bind genetic material (multiplied positive electric charge) while lowering undesirable effects (the presence of lipids makes the system more like natural membranes). This study aimed to test the ability to bind and release genetic material by lipoplexes based on trimeric surfactants and lipid formulations of different compositions and to characterize formed complexes by circular dichroism (CD) spectroscopy and atomic force microscopy (AFM). The cytotoxicity of studied lipoplexes was tested on HeLa cells by the MTT cell viability assay and the dye exclusion test (trypan blue). The presence of lipids in the system lowered the surfactant concentration required for complexation (higher efficiency) and reduced the cytotoxicity of lipoplexes. Surfactant/lipids/DNA complexes were more stable than surfactant/DNA complexes. Surfactant molecules induced the genetic material condensation, but the presence of lipids significantly intensified this process. Systems based on trimeric surfactants and lipid formulations, particularly TRI_N and TRI_IMI systems, could be used as delivery carrier, and have proven to be highly effective, nontoxic, and universal for DNA of various lengths. Full article
(This article belongs to the Special Issue Lipid-Based Drug Carriers and Nanoparticles)
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15 pages, 2484 KiB  
Article
Liposomes Targeting P21 Activated Kinase-1 (PAK-1) and Selective for Secretory Phospholipase A2 (sPLA2) Decrease Cell Viability and Induce Apoptosis in Metastatic Triple-Negative Breast Cancer Cells
by Wided Najahi-Missaoui, Nhat D. Quach, Payaningal R. Somanath and Brian S. Cummings
Int. J. Mol. Sci. 2020, 21(24), 9396; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21249396 - 10 Dec 2020
Cited by 9 | Viewed by 2075
Abstract
P21 activated kinases (or group I PAKs) are serine/threonine kinases whose expression is altered in prostate and breast cancers. PAK-1 activity is inhibited by the small molecule “Inhibitor targeting PAK-1 activation-3” (IPA-3), which has selectivity for PAK-1 but is metabolically unstable. Secretory Group [...] Read more.
P21 activated kinases (or group I PAKs) are serine/threonine kinases whose expression is altered in prostate and breast cancers. PAK-1 activity is inhibited by the small molecule “Inhibitor targeting PAK-1 activation-3” (IPA-3), which has selectivity for PAK-1 but is metabolically unstable. Secretory Group IIA phospholipase A2 (sPLA2) expression correlates to increased metastasis and decreased survival in many cancers. We previously designed novel liposomal formulations targeting both PAK-1 and sPLA2, called Secretory Phospholipase Responsive liposomes or SPRL-IPA-3, and demonstrated their ability to alter prostate cancer growth. The efficacy of SPRL against other types of cancers is not well understood. We addressed this limitation by determining the ability of SPRL to induce cell death in a diverse panel of cells representing different stages of breast cancer, including the invasive but non-metastatic MCF-7 cells, and metastatic triple-negative breast cancer (TNBC) cells such as MDA-MB-231, MDA-MB-468, and MDA-MB-435. We investigated the role of sPLA2 in the disposition of these liposomes by comparing the efficacy of SPRL-IPA-3 to IPA-3 encapsulated in sterically stabilized liposomes (SSL-IPA-3), a formulation shown to be less sensitive to sPLA2. Both SSL-IPA-3 and SPRL-IPA-3 induced time- and dose-dependent decreases in MTT staining in all cell lines tested, but SPRL-IPA-3-induced effects in metastatic TNBC cell lines were superior over SSL-IPA-3. The reduction in MTT staining induced by SPRL-IPA-3 correlated to the expression of Group IIA sPLA2. sPLA2 expression also correlated to increased induction of apoptosis in TNBC cell lines by SPRL-IPA-3. These data suggest that SPRL-IPA-3 is selective for metastatic TNBC cells and that the efficacy of SPRL-IPA-3 is mediated, in part, by the expression of Group IIA sPLA2. Full article
(This article belongs to the Special Issue Lipid-Based Drug Carriers and Nanoparticles)
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Review

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21 pages, 2608 KiB  
Review
Safe Nanoparticles: Are We There Yet?
by Wided Najahi-Missaoui, Robert D. Arnold and Brian S. Cummings
Int. J. Mol. Sci. 2021, 22(1), 385; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22010385 - 31 Dec 2020
Cited by 195 | Viewed by 15730
Abstract
The field of nanotechnology has grown over the last two decades and made the transition from the benchtop to applied technologies. Nanoscale-sized particles, or nanoparticles, have emerged as promising tools with broad applications in drug delivery, diagnostics, cosmetics and several other biological and [...] Read more.
The field of nanotechnology has grown over the last two decades and made the transition from the benchtop to applied technologies. Nanoscale-sized particles, or nanoparticles, have emerged as promising tools with broad applications in drug delivery, diagnostics, cosmetics and several other biological and non-biological areas. These advances lead to questions about nanoparticle safety. Despite considerable efforts to understand the toxicity and safety of these nanoparticles, many of these questions are not yet fully answered. Nevertheless, these efforts have identified several approaches to minimize and prevent nanoparticle toxicity to promote safer nanotechnology. This review summarizes our current knowledge on nanoparticles, their toxic effects, their interactions with mammalian cells and finally current approaches to minimizing their toxicity. Full article
(This article belongs to the Special Issue Lipid-Based Drug Carriers and Nanoparticles)
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23 pages, 28809 KiB  
Review
Building Blocks to Design Liposomal Delivery Systems
by Katarzyna Juszkiewicz, Aleksander F. Sikorski and Aleksander Czogalla
Int. J. Mol. Sci. 2020, 21(24), 9559; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21249559 - 15 Dec 2020
Cited by 23 | Viewed by 4678
Abstract
The flexibility of liposomal carriers does not just simply rely on their capability to encapsulate various types of therapeutic substances, but also on the large array of components used for designing liposome-based nanoformulations. Each of their components plays a very specific role in [...] Read more.
The flexibility of liposomal carriers does not just simply rely on their capability to encapsulate various types of therapeutic substances, but also on the large array of components used for designing liposome-based nanoformulations. Each of their components plays a very specific role in the formulation and can be easily replaced whenever a different therapeutic effect is desired. It is tempting to describe this by an analogy to Lego blocks, since a whole set of structures, differing in their features, can be designed using a certain pool of blocks. In this review, we focus on different design strategies, where a broad variety of liposomal components facilitates the attainment of straightforward control over targeting and drug release, which leads to the design of the most promising systems for drug delivery. The key aspects of this block-based architecture became evident after its implementation in our recent works on liposomal carriers of antisense oligonucleotides and statins, which are described in the last chapter of this review. Full article
(This article belongs to the Special Issue Lipid-Based Drug Carriers and Nanoparticles)
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