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Pharmaceutics
Special Issues
Preclinical Evaluation of Lipid-Based Nanosystems (Volume II)
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Preclinical Evaluation of Lipid-Based Nanosystems (Volume II)

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (10 June 2022) | Viewed by 8102

Special Issue Editors

Dr. Ana Catarina Silva

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Guest Editor
1. UCIBIO/REQUIMTE, MEDTECH, Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
2. FP-I3ID (Instituto de Investigação, Inovação e Desenvolvimento), FP-BHS (Biomedical and Health Sciences Research Unit), Faculty of Health Sciences, University Fernando Pessoa, 4249-004 Porto, Portugal
Interests: lipid nanoparticles; nose-to-brain delivery; cutaneous delivery; drug delivery systems; biopharmaceutics; biological medicines; biosimilars
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. José Manuel Sousa Lobo

E-Mail Website1 Website2
Guest Editor
UCIBIO, REQUIMTE, Laboratory of Pharmaceutical Technology, Centre of Research in Pharmaceutical Sciences, Faculty of Pharmacy, University of Porto, Porto, Portugal
Interests: pharmaceutical technology; biopharmacy; pharmacokinetics; pharmaceutical nanotechnology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues,

The use of lipid-based nanosystems, including lipid nanoparticles (solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)), nanoemulsions, and liposomes, is widespread. Several researchers have described the advantages of the different applications of these nanosystems. For instance, they can increase the targeting and bioavailability of drugs, improving their therapeutic effect. Their use in the cosmetic field is also promising, owing to the moisturizing properties and ability to protect labile cosmetic actives. Thus, it is surprising that only few lipid-based nanosystems have reached the market. This can be explained by the strict regulatory requirements of medicines and the occurrence of unexpected in vivo failure, which highlights the need to conduct more preclinical studies.

Current research is focused on testing the in vitro, ex vivo, and in vivo efficacy of lipid-based nanosystems to predict their clinical performance. However, there is a lack of method validation, which compromises comparison between different studies.

This special issue brings together the latest research and reviews that report preclinical studies in vitro, ex vivo, and in vivo using lipid-based nanosystems. Readers will find up-to-date information on the most common experiments that have been carried out to predict the clinical behavior of lipid-based nanosystems.

Dr. Ana Catarina Silva
Prof. Dr. José Manuel Sousa Lobo
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

  • solid lipid nanoparticles
  • nanostructured lipid carriers
  • nanoemulsions
  • liposomes
  • in vitro studies
  • ex vivo studies
  • in vivo studies

Related Special Issue

Published Papers (3 papers)

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Research

20 pages, 13826 KiB  
Article
Theranostic Microbubbles with Homogeneous Ligand Distribution for Higher Binding Efficacy
by Simone A. G. Langeveld, Bram Meijlink, Inés Beekers, Mark Olthof, Antonius F. W. van der Steen, Nico de Jong and Klazina Kooiman
Pharmaceutics 2022, 14(2), 311; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14020311 - 28 Jan 2022
Cited by 4 | Viewed by 2161
Abstract
Phospholipid-coated targeted microbubbles are used for ultrasound molecular imaging and locally enhanced drug delivery, with the binding efficacy being an important trait. The use of organic solvent in microbubble production makes the difference between a heterogeneous or homogeneous ligand distribution. This study demonstrates [...] Read more.
Phospholipid-coated targeted microbubbles are used for ultrasound molecular imaging and locally enhanced drug delivery, with the binding efficacy being an important trait. The use of organic solvent in microbubble production makes the difference between a heterogeneous or homogeneous ligand distribution. This study demonstrates the effect of ligand distribution on the binding efficacy of phospholipid-coated ανβ3-targeted microbubbles in vitro using a monolayer of human umbilical-vein endothelial cells and in vivo using chicken embryos. Microbubbles with a homogeneous ligand distribution had a higher binding efficacy than those with a heterogeneous ligand distribution both in vitro and in vivo. In vitro, 1.55× more microbubbles with a homogeneous ligand distribution bound under static conditions, while this was 1.49× more under flow with 1.25 dyn/cm2, 1.56× more under flow with 2.22 dyn/cm2, and 1.25× more in vivo. The in vitro dissociation rate of bound microbubbles with homogeneous ligand distribution was lower at low shear stresses (1–5 dyn/cm2). The internalized depth of bound microbubbles was influenced by microbubble size, not by ligand distribution. In conclusion, for optimal binding the use of organic solvent in targeted microbubble production is preferable over directly dispersing phospholipids in aqueous medium. Full article
(This article belongs to the Special Issue Preclinical Evaluation of Lipid-Based Nanosystems (Volume II))
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17 pages, 3987 KiB  
Article
Vine Cane Compounds to Prevent Skin Cells Aging through Solid Lipid Nanoparticles
by Adriana Pereira, Maria João Ramalho, Renata Silva, Vera Silva, Rita Marques-Oliveira, Ana Catarina Silva, Maria Carmo Pereira and Joana A. Loureiro
Pharmaceutics 2022, 14(2), 240; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14020240 - 20 Jan 2022
Cited by 5 | Viewed by 2436
Abstract
The long lifespan of the world’s population has been raising interest in the research for new solutions to delay the aging process. With the aim of skin aging prevention, solid lipid nanoparticles (SLNs) were developed in this work for the encapsulation of three [...] Read more.
The long lifespan of the world’s population has been raising interest in the research for new solutions to delay the aging process. With the aim of skin aging prevention, solid lipid nanoparticles (SLNs) were developed in this work for the encapsulation of three lipophilic natural compounds extracted from vine cane—epigallocatechin gallate (EGCG), resveratrol and myricetin. The developed loaded-SLNs proved to be stable, maintaining their adequate physicochemical characteristics for 30 days. In addition, the loaded-SLNs formulations exhibited high encapsulation efficiencies and loading capacities and high intracellular antioxidant activity. The mixture of EGCG-loaded SLNs with resveratrol-loaded SLNs proved to have the highest protection against induced oxidative stress. The in vitro cytotoxicity of the loaded SLNs was also evaluated, showing that the developed formulations are biocompatible for concentrations up to 50 µg/mL and could be safe for use in cosmetics. The encapsulation of EGCG, resveratrol and myricetin in SLNs seems to be a suitable strategy for the delivery of these antioxidants to the skin, improving their bioavailability. Full article
(This article belongs to the Special Issue Preclinical Evaluation of Lipid-Based Nanosystems (Volume II))
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21 pages, 3711 KiB  
Article
Celecoxib-Loaded Solid Lipid Nanoparticles for Colon Delivery: Formulation Optimization and In Vitro Assessment of Anti-Cancer Activity
by Hamdan N. Alajami, Ehab A. Fouad, Abdelkader E. Ashour, Ashok Kumar and Alaa Eldeen B. Yassin
Pharmaceutics 2022, 14(1), 131; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14010131 - 05 Jan 2022
Cited by 21 | Viewed by 2710
Abstract
This work aimed to optimize a celecoxib (CXB)-loaded solid lipid nanoparticles (SLN) colon delivery system for the enhancement of anticancer activity. An ultrasonic melt-emulsification method was employed in this work for the preparation of SLN. The physical attributes were characterized for their particle [...] Read more.
This work aimed to optimize a celecoxib (CXB)-loaded solid lipid nanoparticles (SLN) colon delivery system for the enhancement of anticancer activity. An ultrasonic melt-emulsification method was employed in this work for the preparation of SLN. The physical attributes were characterized for their particle sizes, charges, morphology, and entrapment efficiency (%EE), in addition to DSC and FTIR. The in vitro drug release profiles were evaluated, and the anticancer activity was examined utilizing an MTT assay in three cancer cell lines: the colon cancer HT29, medulloblastoma Daoy, and hepatocellular carcinoma HepG2 cells. All of the prepared SLN formulations had nanoscale particle sizes ranging from 238 nm to 757 nm. High zeta-potential values (mv) within −30 s mv were reported. The %EE was in the range 86.76–96.6%. The amorphous nature of the SLN-entrapped CXB was confirmed from SLN DSC thermograms. The in vitro release profile revealed a slow constant rate of release with no burst release, which is unusual for SLN. Both the F9 and F14 demonstrated almost complete CXB release within 24 h, with only 25% completed within the first 5 h. F9 caused a significant percentage of cell death in the three cancer cell lines tested after 24 h of incubation and maintained this effect for 72 h. The prepared CXB-loaded SLN exhibited unique properties such as slow release with no burst and a high %EE. The anticancer activity of one formulation was extremely significant in all tested cancer cell lines at all incubation times, which is very promising. Full article
(This article belongs to the Special Issue Preclinical Evaluation of Lipid-Based Nanosystems (Volume II))
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