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Pharmaceutics
Special Issues
Lipid-Based Drug Delivery Systems: The Key Ingredient for Future Medicine
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Lipid-Based Drug Delivery Systems: The Key Ingredient for Future Medicine

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 (31 January 2023) | Viewed by 11705

Special Issue Editors

Dr. Simone Aleandri

E-Mail Website
Guest Editor
Department of Chemistry, Biochemistry and pharmaceutical science, University of Bern, 3030 Bern, Switzerland
Interests: lipidic mesophases; liposomes; lipid-based drug delivery systems; new lipidic–depot systems; controlled drug release; active targeting
Special Issues, Collections and Topics in MDPI journals
Dr. Wye-Khay Fong

E-Mail Website
Guest Editor
School of Environmental and Life Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia
Interests: lipid self-assembly; soft matter; lipid-based drug delivery systems; stimuli-responsive drug release; synchrotron science; microplastics
Dr. Livia Salvati Manni

E-Mail Website
Guest Editor
1. School of Chemistry, University of Sydney, Sydney, NSW, Australia
2. School of Environmental and Life Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia
Interests: lipid self-assembly; lipid behavior; synthetic lipids; lipid-based drug delivery; ionic liquids

Special Issue Information

Dear Colleagues,

Lipid-based matrices are state-of-the-art tools employed to envelop and protect a vast range of therapeutics from degradation and to deliver them safely to the site of action. Due to their unique ability to compartmentalise hydrophilic and hydrophobic components, they have been utilized to achieve targeted and/or controlled drug release. Whilst a plethora of lipidic drug carriers have been reported in the last few decades, with many lipid-based products already on the market or undergoing clinical trials, there is still a pressing need for new formulations tailored to target different sites of action and to incorporated novel drugs. Moreover, several aspects of their in vivo behaviour in the complex biological environment are not fully elucidated. Research into the innovative use of lipidic platforms in pharmaceutics is vital for their application as a mean to modify or control the release of drugs in vitro and in vivo. This Special Issue aims to highlight research on the encapsulation of pharmaceuticals and bio-pharmaceuticals in lipidic systems, their behaviour in biological environments, controlled release kinetics, and organ-specific bioavailability (e.g., through a targeting strategy). Reviews or original articles on these topics are welcome.

We look forward to receiving your contributions.

Dr. Simone Aleandri
Dr. Wye-Khay Fong
Dr. Livia Salvati Manni
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. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). 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 nanoparticles
  • controlled release
  • targeting strategies
  • biopharmaceuticals
  • drug delivery
  • nanocarriers

Published Papers (4 papers)

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Research

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21 pages, 3905 KiB  
Article
Tailoring the Lamellarity of Liposomes Prepared by Dual Centrifugation
by Jonas K. Koehler, Lars Gedda, Leonie Wurster, Johannes Schnur, Katarina Edwards, Heiko Heerklotz and Ulrich Massing
Pharmaceutics 2023, 15(2), 706; https://doi.org/10.3390/pharmaceutics15020706 - 20 Feb 2023
Cited by 4 | Viewed by 2515
Abstract
Dual centrifugation (DC) is a new and versatile technique for the preparation of liposomes by in-vial homogenization of lipid-water mixtures. Size, size distribution, and entrapping efficiencies are strongly dependent on the lipid concentration during DC-homogenization. In this study, we investigated the detailed structure [...] Read more.
Dual centrifugation (DC) is a new and versatile technique for the preparation of liposomes by in-vial homogenization of lipid-water mixtures. Size, size distribution, and entrapping efficiencies are strongly dependent on the lipid concentration during DC-homogenization. In this study, we investigated the detailed structure of DC-made liposomes. To do so, an assay to determine the ratio of inner to total membrane surfaces of liposomes (inaccessible surface) was developed based on either time-resolved or steady-state fluorescence spectroscopy. In addition, cryogenic electron microscopy (cryo-EM) was used to confirm the lamellarity results and learn more about liposome morphology. One striking result leads to the possibility of producing a novel type of liposome—small multilamellar vesicles (SMVs) with low PDI, sizes of the order of 100 nm, and almost completely filled with bilayers. A second particularly important finding is that VPGs can be prepared to contain open bilayer structures that will close spontaneously when, after storage, more aqueous phase is added and liposomes are formed. Through this process, a drug can effectively be entrapped immediately before application. In addition, dual centrifugation at lower lipid concentrations is found to produce predominantly unilamellar vesicles. Full article
(This article belongs to the Special Issue Lipid-Based Drug Delivery Systems: The Key Ingredient for Future Medicine)
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20 pages, 4249 KiB  
Article
Interplay of Hydropathy and Heterogeneous Diffusion in the Molecular Transport within Lamellar Lipid Mesophases
by Antonio M. Bosch and Salvatore Assenza
Pharmaceutics 2023, 15(2), 573; https://doi.org/10.3390/pharmaceutics15020573 - 08 Feb 2023
Cited by 1 | Viewed by 1384
Abstract
Lipid mesophases are being intensively studied as potential candidates for drug-delivery purposes. Extensive experimental characterization has unveiled a wide palette of release features depending on the nature of the host lipids and of the guest molecule, as well as on the environmental conditions. [...] Read more.
Lipid mesophases are being intensively studied as potential candidates for drug-delivery purposes. Extensive experimental characterization has unveiled a wide palette of release features depending on the nature of the host lipids and of the guest molecule, as well as on the environmental conditions. However, only a few simulation works have addressed the matter, which hampers a solid rationalization of the richness of outcomes observed in experiments. Particularly, to date, there are no theoretical works addressing the impact of hydropathy on the transport of a molecule within lipid mesophases, despite the significant fraction of hydrophobic molecules among currently-available drugs. Similarly, the high heterogeneity of water mobility in the nanoscopic channels within lipid mesophases has also been neglected. To fill this gap, we introduce here a minimal model to account for these features in a lamellar geometry, and systematically study the role played by hydropathy and water–mobility heterogeneity by Brownian-dynamics simulations. We unveil a fine interplay between the presence of free-energy barriers, the affinity of the drug for the lipids, and the reduced mobility of water in determining the net molecular transport. More in general, our work is an instance of how multiscale simulations can be fruitfully employed to assist experiments in release systems based on lipid mesophases. Full article
(This article belongs to the Special Issue Lipid-Based Drug Delivery Systems: The Key Ingredient for Future Medicine)
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17 pages, 2063 KiB  
Article
Preliminary Assessment of Intramuscular Depot of Lipid-Based Decoquinate Formulation for Long-Term Chemoprophylaxis of Malaria
by Yinzhou Fan, Li Qin, Zhenping Huang, Shuanghong Liang, Xiaoyi Huang, Sumei Zeng, Yucheng Liu and Hongxing Wang
Pharmaceutics 2022, 14(12), 2813; https://doi.org/10.3390/pharmaceutics14122813 - 15 Dec 2022
Cited by 2 | Viewed by 1426
Abstract
Sustained-release formulations of decoquinate were evaluated for the long-term prophylaxis of malaria. In the initial experiment, mice were protected from liver-stage Plasmodium infection by intramuscular administration of a lipids-based formulation at a dose of decoquinate 200 mg/kg. The mice that were inoculated with [...] Read more.
Sustained-release formulations of decoquinate were evaluated for the long-term prophylaxis of malaria. In the initial experiment, mice were protected from liver-stage Plasmodium infection by intramuscular administration of a lipids-based formulation at a dose of decoquinate 200 mg/kg. The mice that were inoculated with Plasmodium berghei sporozoites 34 days after the administration of a one-time drug dose were continuously monitored for 60 days and shown to be free of Plasmodium parasites. The optimized formulation for the sustained release of decoquinate was prepared by hot melt extrusion, constructed by lipids including cholesterol and mono or diglycerides, and had a drug load of 20 to 40% and particle size of 30 to 50 μm. Decoquinate of the lipids-based formulation was slowly released in vitro at a constant rate for the duration of two months, and was examined and continuously exposed at a therapeutic level in the blood for as long as 4 to 6 months. Further evaluation showed that the lipids-based formulation at doses of decoquinate 100 to 150 mg/kg could protect mice from Plasmodium infection for a period of 120 days. It is the first time that cholesterol has been used for a controlled drug delivery system of decoquinate. The results may provide useful information, not only for preparing a formulation of long-acting decoquinate but also in general for developing a controlled drug release system. The one-time administration of pharmaceutical agents in such a slow-release system may serve patients with no concerns about compliance. Full article
(This article belongs to the Special Issue Lipid-Based Drug Delivery Systems: The Key Ingredient for Future Medicine)
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Review

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22 pages, 3917 KiB  
Review
Recent Progress of Lipid Nanoparticles-Based Lipophilic Drug Delivery: Focus on Surface Modifications
by Yoseph Seo, Hayeon Lim, Hyunjun Park, Jiyun Yu, Jeongyun An, Hah Young Yoo and Taek Lee
Pharmaceutics 2023, 15(3), 772; https://doi.org/10.3390/pharmaceutics15030772 - 26 Feb 2023
Cited by 17 | Viewed by 5415
Abstract
Numerous drugs have emerged to treat various diseases, such as COVID-19, cancer, and protect human health. Approximately 40% of them are lipophilic and are used for treating diseases through various delivery routes, including skin absorption, oral administration, and injection. However, as lipophilic drugs [...] Read more.
Numerous drugs have emerged to treat various diseases, such as COVID-19, cancer, and protect human health. Approximately 40% of them are lipophilic and are used for treating diseases through various delivery routes, including skin absorption, oral administration, and injection. However, as lipophilic drugs have a low solubility in the human body, drug delivery systems (DDSs) are being actively developed to increase drug bioavailability. Liposomes, micro-sponges, and polymer-based nanoparticles have been proposed as DDS carriers for lipophilic drugs. However, their instability, cytotoxicity, and lack of targeting ability limit their commercialization. Lipid nanoparticles (LNPs) have fewer side effects, excellent biocompatibility, and high physical stability. LNPs are considered efficient vehicles of lipophilic drugs owing to their lipid-based internal structure. In addition, recent LNP studies suggest that the bioavailability of LNP can be increased through surface modifications, such as PEGylation, chitosan, and surfactant protein coating. Thus, their combinations have an abundant utilization potential in the fields of DDSs for carrying lipophilic drugs. In this review, the functions and efficiencies of various types of LNPs and surface modifications developed to optimize lipophilic drug delivery are discussed. Full article
(This article belongs to the Special Issue Lipid-Based Drug Delivery Systems: The Key Ingredient for Future Medicine)
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