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Biomedicines
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Lipid-Based Nanocarriers
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Lipid-Based Nanocarriers

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Drug Discovery, Development and Delivery".

Deadline for manuscript submissions: closed (30 June 2022) | Viewed by 16117

Special Issue Editor

Dr. Chin-Tin Chen

E-Mail Website
Guest Editor
Department of Biochemical Science and Technology, National Taiwan University, No. 1, Sec. 4, Roosevelt Road, Taipei 10617, Taiwan
Interests: photodynamic therapy; drug delivery system; cell biology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Lipid-based nanocarriers (LN) effectively deliver active pharmaceutical ingredients (API) to modify the bioavailability and performance of drugs. Patients benefit from these nanocarrier formulations by altered pharmacokinetic properties, tissue distribution, higher therapeutic efficacy, and reduced side effects. These lipid-based nanocarriers include liposomes, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and lipid nanoparticles (LNP) for delivering small molecule drugs as well as biologics. Recently, the application of lipid-based nanocarriers in oncology, infectious diseases, and other metabolic disorders have shown impressive efficacy. A typical example is the success of COVID-19 vaccines developed by Moderna and BioNTech/Pfizer.

This Special Issue welcomes manuscripts related to lipid-based nanocarriers,  encapsulating with small molecules, peptides/proteins, and nucleic acids. The manuscript can be at various stages, from the development of lipid-based nanocarrier formulations to their translational applications for treating diseases, in the form of original articles as well as reviews.

Dr. Chin-Tin Chen
Guest Editor

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. Biomedicines 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 2600 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

  • liposomes
  • solid lipid nanoparticles (SLN)
  • nanostructured lipid carriers (NLC)
  • lipid nanoparticle (LNP)

Published Papers (7 papers)

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Editorial

Jump to: Research, Review

2 pages, 165 KiB  
Editorial
Editorial for the Specific Issue: “Lipid-Based Nanocarriers”
by Chin-Tin Chen
Biomedicines 2022, 10(7), 1734; https://doi.org/10.3390/biomedicines10071734 - 19 Jul 2022
Viewed by 909
Abstract
Small molecules and biologics are the two major categories of active pharmaceutical ingredients (APIs) commonly used for disease management [...] Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)

Research

Jump to: Editorial, Review

19 pages, 3815 KiB  
Article
Fabrication of Doxorubicin-Loaded Lipid-Based Nanocarriers by Microfluidic Rapid Mixing
by Chia-Ying Lee, Tsuimin Tsai, Po-Chun Peng and Chin-Tin Chen
Biomedicines 2022, 10(6), 1259; https://doi.org/10.3390/biomedicines10061259 - 27 May 2022
Cited by 6 | Viewed by 2152
Abstract
Doxorubicin (Dox) is a widely known chemotherapeutic drug that has been encapsulated into liposomes for clinical use, such as Doxil® and Myocet®. Both of these are prepared via remote loading methods, which require multistep procedures. Additionally, their antitumor efficacy is [...] Read more.
Doxorubicin (Dox) is a widely known chemotherapeutic drug that has been encapsulated into liposomes for clinical use, such as Doxil® and Myocet®. Both of these are prepared via remote loading methods, which require multistep procedures. Additionally, their antitumor efficacy is hindered due to the poor drug release from PEGylated liposomes in the tumor microenvironment. In this study, we aimed to develop doxorubicin-loaded lipid-based nanocarriers (LNC-Dox) based on electrostatic interaction using microfluidic technology. The resulting LNC-Dox showed high loading capacity, with a drug-to-lipid ratio (D/L ratio) greater than 0.2, and high efficacy of drug release in an acidic environment. Different lipid compositions were selected based on critical packing parameters and further studied to outline their effects on the physicochemical characteristics of LNC-Dox. Design of experiments was implemented for formulation optimization. The optimized LNC-Dox showed preferred release in acidic environments and better therapeutic efficacy compared to PEGylated liposomal Dox in vivo. Thus, this study provides a feasible approach to efficiently encapsulate doxorubicin into lipid-based nanocarriers fabricated by microfluidic rapid mixing. Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)
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18 pages, 7442 KiB  
Article
Synthesis and Characterization of Fatty Acid Grafted Chitosan Polymeric Micelles for Improved Gene Delivery of VGF to the Brain through Intranasal Route
by Richard Nii Lante Lamptey, Avinash Gothwal, Riddhi Trivedi, Sanjay Arora and Jagdish Singh
Biomedicines 2022, 10(2), 493; https://doi.org/10.3390/biomedicines10020493 - 19 Feb 2022
Cited by 15 | Viewed by 2676
Abstract
Multifunctional fatty acid grafted polymeric micelles are an effective and promising approach for drug and gene delivery to the brain. An alternative approach to bypass the blood–brain barrier is administration through intranasal route. Multifunctional fatty acid grafted polymeric micelles were prepared and characterized [...] Read more.
Multifunctional fatty acid grafted polymeric micelles are an effective and promising approach for drug and gene delivery to the brain. An alternative approach to bypass the blood–brain barrier is administration through intranasal route. Multifunctional fatty acid grafted polymeric micelles were prepared and characterized for pVGF delivery to the brain. In vitro pVGF expression was analyzed in bEnd.3 cells, primary astrocytes, and neurons. Comparative in-vivo pVGF expression was analyzed to evaluate the effective route of administration between intranasal and intravenous. Biocompatible, multifunctional polymeric micelles were prepared, having an average size of 200 nm, and cationic zeta potential. Modified polymers were found to be hemo- and cyto-compatible. When transfected with the different modified chitosan formulations, significantly (p < 0.05) higher VGF expression was observed in primary astrocytes and neurons using the mannose, Tat peptide, and oleic acid grafted chitosan polymer. Compared to intravenous administration, intranasal administration of pVGF in polyplex formulation led to significantly (p < 0.05) higher pVGF expression. Developed multifunctional polymeric micelles were an effective pVGF delivery platform to the brain. Mannose and Tat ligand tagging improved the pVGF delivery to the brain. Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)
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15 pages, 23294 KiB  
Article
Utilizing Sphingomyelinase Sensitizing Liposomes in Imaging Intestinal Inflammation in Dextran Sulfate Sodium-Induced Murine Colitis
by Tuula Penate Medina, Jie Pan, Christabel Damoah, Jana Humbert, Anna-Lena Köpnick, Olga Will, Susanne Sebens and Oula Penate Medina
Biomedicines 2022, 10(2), 413; https://doi.org/10.3390/biomedicines10020413 - 09 Feb 2022
Cited by 5 | Viewed by 1812
Abstract
Inflammatory bowel disease (IBD) is characterized by chronic inflammation in the gastrointestinal tract, resulting in severe symptoms. At the moment, the goal of medical treatments is to reduce inflammation. IBD is treated with systemic anti-inflammatory compounds, but they have serious side effects. The [...] Read more.
Inflammatory bowel disease (IBD) is characterized by chronic inflammation in the gastrointestinal tract, resulting in severe symptoms. At the moment, the goal of medical treatments is to reduce inflammation. IBD is treated with systemic anti-inflammatory compounds, but they have serious side effects. The treatment that is most efficient and causes the fewest side effects would be the delivery of the drugs on the disease site. This study aimed to investigate the suitability of sphingomyelin (SM) containing liposomes to specifically target areas of inflammation in dextran sulfate sodium-induced murine colitis. Sphingomyelin is a substrate to the sphingomyelinase enzyme, which is only present outside cells in cell stress, like inflammation. When sphingomyelin consisting of liposomes is predisposed to the enzyme, it causes the weakening of the membrane structure. We demonstrated that SM-liposomes are efficiently taken up in intestinal macrophages, indicating their delivery potential. Furthermore, our studies showed that sphingomyelinase activity and release are increased in a dextran sulfate sodium-induced IBD mouse model. The enzyme appearance in IBD disease was also traced in intestine samples of the dextran sulfate sodium-treated mice and human tissue samples. The results from the IBD diseased animals, treated with fluorescently labeled SM-liposomes, demonstrated that the liposomes were taken up preferentially in the inflamed colon. This uptake efficiency correlated with sphingomyelinase activity. Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)
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13 pages, 2410 KiB  
Article
Antimicrobial, Immunomodulatory and Anti-Inflammatory Potential of Liposomal Thymoquinone: Implications in the Treatment of Bacterial Pneumonia in Immunocompromised Mice
by Khaled S. Allemailem, Ahmad Almatroudi, Faris Alrumaihi, Aseel Aljaghwani, Abdullah M. Alnuqaydan, Habibullah Khalilullah, Hina Younus, Asmaa M. El-Kady, Fahad M. Aldakheel, Amjad Ali Khan, Arif Khan and Masood Alam Khan
Biomedicines 2021, 9(11), 1673; https://doi.org/10.3390/biomedicines9111673 - 12 Nov 2021
Cited by 8 | Viewed by 1832
Abstract
Acinetobacter baumannii has recently been increasing as an aggressive pathogen in immunocompromised persons. In the present study, we determined the in vitro antibacterial and anti-biofilm activity of thymoquinone (TQ) against A. baumannii. A liposomal formulation of TQ (Lip-TQ) was prepared and its [...] Read more.
Acinetobacter baumannii has recently been increasing as an aggressive pathogen in immunocompromised persons. In the present study, we determined the in vitro antibacterial and anti-biofilm activity of thymoquinone (TQ) against A. baumannii. A liposomal formulation of TQ (Lip-TQ) was prepared and its therapeutic potential was investigated in the treatment of A. baumannii infection in immunocompromised mice. Leukopenia was induced in mice by injecting cyclophosphamide (CYP) at a dose of 200 mg/kg and the leukopenic mice were infected with 1 × 106 CFUs of A. baumannii. The effectiveness of free TQ or Lip-TQ against A. baumannii infection was assessed by analyzing the survival rate and bacterial burden. Moreover, the efficacy of Lip-TQ was also studied by examining the systemic inflammatory markers and the histological changes in the lung tissues. The results showed that the mice in the group treated with Lip-TQ at a dose of 10 mg/kg exhibited a 60% survival rate on day 40 post-infection, whereas all the mice treated with free TQ at the same dose died within this duration. Likewise, the lowest bacterial burden was found in the lung tissue of mice treated with Lip-TQ (10 mg/kg). Besides, Lip-TQ treatment remarkably alleviated the infection-associated inflammation, oxidative stress, and histological changes in the lung tissues. Based on the findings of the present study, we recommend considering Lip-TQ as a valuable therapeutic formulation in the treatment of A. baumannii-associated pneumonia in immunocompromised subjects. Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)
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Review

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13 pages, 722 KiB  
Review
Lipid-Based Nanocarriers in Renal RNA Therapy
by Chi-Ting Su, Daniel H. W. See and Jenq-Wen Huang
Biomedicines 2022, 10(2), 283; https://doi.org/10.3390/biomedicines10020283 - 26 Jan 2022
Cited by 9 | Viewed by 2947
Abstract
Kidney disease is a multifactorial problem, with a growing prevalence and an increasing global burden. With the latest worldwide data suggesting that chronic kidney disease (CKD) is the 12th leading cause of death, it is no surprise that CKD remains a public health [...] Read more.
Kidney disease is a multifactorial problem, with a growing prevalence and an increasing global burden. With the latest worldwide data suggesting that chronic kidney disease (CKD) is the 12th leading cause of death, it is no surprise that CKD remains a public health problem that requires urgent attention. Multiple factors contribute to kidney disease, each with its own pathophysiology and pathogenesis. Furthermore, microRNAs (miRNAs) have been linked to several types of kidney diseases. As dysregulation of miRNAs is often seen in some diseases, there is potential in the exploitation of this for therapeutic applications. In addition, uptake of interference RNA has been shown to be rapid in kidneys making them a good candidate for RNA therapy. The latest advancements in RNA therapy and lipid-based nanocarriers have enhanced the effectiveness and efficiency of RNA-related drugs, thereby making RNA therapy a viable treatment option for renal disease. This is especially useful for renal diseases, for which a suitable treatment is not yet available. Moreover, the high adaptability of RNA therapy combined with the low risk of lipid-based nanocarriers make for an attractive treatment choice. Currently, there are only a small number of RNA-based drugs related to renal parenchymal disease, most of which are in different stages of clinical trials. We propose the use of miRNAs or short interfering RNAs coupled with a lipid-based nanocarrier as a delivery vehicle for managing renal disease. Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)
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22 pages, 373 KiB  
Review
Recent Advances in RNA Therapy and Its Carriers to Treat the Single-Gene Neurological Disorders
by Ming-Jen Lee, Inyoul Lee and Kai Wang
Biomedicines 2022, 10(1), 158; https://doi.org/10.3390/biomedicines10010158 - 12 Jan 2022
Cited by 9 | Viewed by 2892
Abstract
The development of new sequencing technologies in the post-genomic era has accelerated the identification of causative mutations of several single gene disorders. Advances in cell and animal models provide insights into the underlining pathogenesis, which facilitates the development and maturation of new treatment [...] Read more.
The development of new sequencing technologies in the post-genomic era has accelerated the identification of causative mutations of several single gene disorders. Advances in cell and animal models provide insights into the underlining pathogenesis, which facilitates the development and maturation of new treatment strategies. The progress in biochemistry and molecular biology has established a new class of therapeutics—the short RNAs and expressible long RNAs. The sequences of therapeutic RNAs can be optimized to enhance their stability and translatability with reduced immunogenicity. The chemically-modified RNAs can also increase their stability during intracellular trafficking. In addition, the development of safe and high efficiency carriers that preserves the integrity of therapeutic RNA molecules also accelerates the transition of RNA therapeutics into the clinic. For example, for diseases that are caused by genetic defects in a specific protein, an effective approach termed “protein replacement therapy” can provide treatment through the delivery of modified translatable mRNAs. Short interference RNAs can also be used to treat diseases caused by gain of function mutations or restore the splicing aberration defects. Here we review the applications of newly developed RNA-based therapeutics and its delivery and discuss the clinical evidence supporting the potential of RNA-based therapy in single-gene neurological disorders. Full article
(This article belongs to the Special Issue Lipid-Based Nanocarriers)
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