Recent Advances in the Use of Phospholipids in Drug Delivery

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 (20 May 2023) | Viewed by 20730

Special Issue Editor


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Guest Editor
Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, 55 5230 Campusvej, Denmark
Interests: lipid-based colloidal formulations; physico-chemical characterization methods; drug release from colloidal carriers in physiologically relevant media; asymmetric flow field-flow fractionation; light scattering

Special Issue Information

Dear Colleagues,

Phospholipids are the major component of biological membranes and well-established, biocompatible pharmaceutical excipients. They are best known from liposomes, which have been intensively explored as drug carriers as well as model membrane systems since their discovery by Bangham and Horn in 1961. However, due to their unique properties, functionality, and structural diversity, the applicability of phospholipids in the pharmaceutical field goes far beyond liposomal formulations.

This Special Issue aims to summarize recent trends in the use of phospholipids in the field of drug delivery. In addition to recent research on liposomal and related nanoparticular formulations as intravenous drug carriers, the major aim of this Issue is to explore the utility of phospholipids in alternative formulations and administration routes, addressing major challenges in current drug development such as poor bioavailability (e.g., hydrophobic small molecules) as well as the formulation of large molecules (e.g., proteins and nucleic acids). In addition, the use of phospholipids in models for in vitro testing (e.g., permeability) and relevant characterization issues (e.g., drug release) will be addressed.

Dr. Judith Kuntsche
Guest Editor

Manuscript Submission Information

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Keywords

  • liposomes and lipid-based formulations
  • drug targeting
  • drug solubilization and bioavailability
  • oral drug delivery
  • injectables
  • (trans)dermal drug delivery
  • pulmonary drug delivery
  • in vitro models and characterization (drug permeability, drug release)

Published Papers (5 papers)

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Research

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16 pages, 3400 KiB  
Article
Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin
by Santosh Bashyal, Jo-Eun Seo, Taekwang Keum, Gyubin Noh, Shrawani Lamichhane and Sangkil Lee
Pharmaceutics 2021, 13(4), 565; https://doi.org/10.3390/pharmaceutics13040565 - 16 Apr 2021
Cited by 25 | Viewed by 3561
Abstract
Buccal drug delivery is a suitable alternative to invasive routes of drug administration. The buccal administration of insulin for the management of diabetes has received substantial attention worldwide. The main aim of this study was to develop and characterize elastic liposomes and assess [...] Read more.
Buccal drug delivery is a suitable alternative to invasive routes of drug administration. The buccal administration of insulin for the management of diabetes has received substantial attention worldwide. The main aim of this study was to develop and characterize elastic liposomes and assess their permeability across porcine buccal tissues. Sodium-cholate-incorporated elastic liposomes (SC-EL) and sodium-glycodeoxycholate-incorporated elastic liposomes (SGDC-EL) were prepared using the thin-film hydration method. The prepared liposomes were characterized and their ex vivo permeability attributes were investigated. The distribution of the SC-EL and SGDC-EL across porcine buccal tissues was evaluated using confocal laser scanning microscopy (CLSM). The SGDC-EL were the most superior nanocarriers since they significantly enhanced the permeation of insulin across porcine buccal tissues, displaying a 4.33-fold increase in the permeability coefficient compared with the insulin solution. Compared with the SC-EL, the SGDC-EL were better at facilitating insulin permeability, with a 3.70-fold increase in the permeability coefficient across porcine buccal tissue. These findings were further corroborated based on bioimaging analysis using CLSM. SGDC-ELs showed the greatest fluorescence intensity in buccal tissues, as evidenced by the greater shift of fluorescence intensity toward the inner buccal tissue over time. The fluorescence intensity ranked as follows: SGDC-EL > SC-EL > FITC–insulin solution. Conclusively, this study highlighted the potential nanocarriers for enhancing the buccal permeability of insulin. Full article
(This article belongs to the Special Issue Recent Advances in the Use of Phospholipids in Drug Delivery)
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19 pages, 3292 KiB  
Article
Phosphatidylinositol Stabilizes Fluid-Phase Liposomes Loaded with a Melphalan Lipophilic Prodrug
by Daria Tretiakova, Irina Le-Deigen, Natalia Onishchenko, Judith Kuntsche, Elena Kudryashova and Elena Vodovozova
Pharmaceutics 2021, 13(4), 473; https://doi.org/10.3390/pharmaceutics13040473 - 01 Apr 2021
Cited by 17 | Viewed by 2333
Abstract
Previously, a liposomal formulation of a chemotherapeutic agent melphalan (Mlph) incorporated in a fluid lipid bilayer of natural phospholipids in the form of dioleoylglyceride ester (MlphDG) was developed and the antitumor effect was confirmed in mouse models. The formulation composed of egg phosphatidylcholine [...] Read more.
Previously, a liposomal formulation of a chemotherapeutic agent melphalan (Mlph) incorporated in a fluid lipid bilayer of natural phospholipids in the form of dioleoylglyceride ester (MlphDG) was developed and the antitumor effect was confirmed in mouse models. The formulation composed of egg phosphatidylcholine (ePC), soybean phosphatidylinositol (PI), and MlphDG (8:1:1, by mol) showed stability in human serum for at least 4–5 h. On the contrary, replacing PI with pegylation of the liposomes, promoted fast dissociation of the components from the bilayer. In this work, interactions of MlphDG-liposomes with the most abundant plasma protein—albumin—in function of the presence of PI in the formulation were explored using Fourier transform infrared spectroscopy. The release of MlphDG from the liposomes was studied by asymmetrical flow field-flow fractionation (AF4) using micelles formed by a polyethylene glycol conjugate with phosphatidylethanolamine to mimic the physiological lipid sink like lipoproteins. Our results show that PI actually protects the membrane of MlphDG-liposomes from the protein penetration, presumably due to pairing between the positively charged MlphDG and negatively charged PI, which compensates for the heterogeneity of the lipid bilayer. The AF4 technique also evidences high stability of the formulation as a drug carrier. Full article
(This article belongs to the Special Issue Recent Advances in the Use of Phospholipids in Drug Delivery)
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16 pages, 3485 KiB  
Article
Changes in Skin Barrier Function after Repeated Exposition to Phospholipid-Based Surfactants and Sodium Dodecyl Sulfate In Vivo and Corneocyte Surface Analysis by Atomic Force Microscopy
by Claudia Vater, Alexandra Apanovic, Christoph Riethmüller, Brigitte Litschauer, Michael Wolzt, Claudia Valenta and Victoria Klang
Pharmaceutics 2021, 13(4), 436; https://doi.org/10.3390/pharmaceutics13040436 - 24 Mar 2021
Cited by 13 | Viewed by 3009
Abstract
(1) Background: The aim of the study was to evaluate the effect of pure lecithins in comparison to a conventional surfactant on skin in vivo. (2) Methods: Physiological skin parameters were evaluated at the beginning and the end of the study (day 1 [...] Read more.
(1) Background: The aim of the study was to evaluate the effect of pure lecithins in comparison to a conventional surfactant on skin in vivo. (2) Methods: Physiological skin parameters were evaluated at the beginning and the end of the study (day 1 and day 4) (n = 8, healthy forearm skin) with an Aquaflux®, skin-pH-Meter, Corneometer® and an Epsilon® sensor. Confocal Raman spectroscopy was employed to monitor natural moisturizing factor, urea and water content of the participants’ skin. Tape strips of treated skin sites were taken and the collected corneocytes were subjected to atomic force microscopy. Circular nano objects were counted, and dermal texture indices were determined. (3) Results: Transepidermal water loss was increased, and skin hydration was decreased after treatment with SDS and LPC80. Natural moisturizing factor and urea concentrations within the outermost 10 µm of the stratum corneum were lower than after treatment with S75 or water. Dermal texture indices of skin treated with SDS were higher than skin treated with water (control). (4) Conclusions: Results suggest very good (S75) or good (LPC80) skin-tolerability of lecithin-based surfactants in comparison to SDS and encourage further investigation. Full article
(This article belongs to the Special Issue Recent Advances in the Use of Phospholipids in Drug Delivery)
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16 pages, 3545 KiB  
Article
Towards the Development of Long Circulating Phosphatidylserine (PS)- and Phosphatidylglycerol (PG)-Enriched Anti-Inflammatory Liposomes: Is PEGylation Effective?
by Miriam E. Klein, Max Rieckmann, Daniel Sedding, Gerd Hause, Annette Meister, Karsten Mäder and Henrike Lucas
Pharmaceutics 2021, 13(2), 282; https://doi.org/10.3390/pharmaceutics13020282 - 19 Feb 2021
Cited by 9 | Viewed by 2999
Abstract
The anionic phospholipids (PLs) phosphatidylserine (PS) and phosphatidylglycerol (PG) are endogenous phospholipids with anti-inflammatory and immunomodulatory activity. A potential clinical use requires well-defined systems and for several applications, a long circulation time is desirable. Therefore, we aimed the development of long circulating liposomes [...] Read more.
The anionic phospholipids (PLs) phosphatidylserine (PS) and phosphatidylglycerol (PG) are endogenous phospholipids with anti-inflammatory and immunomodulatory activity. A potential clinical use requires well-defined systems and for several applications, a long circulation time is desirable. Therefore, we aimed the development of long circulating liposomes with intrinsic anti-inflammatory activity. Hence, PS- and PG-enriched liposomes were produced, whilst phosphatidylcholine (PC) liposomes served as control. Liposomes were either formulated as conventional or PEGylated formulations. They had diameters below 150 nm, narrow size distributions and composition-dependent surface charges. Pharmacokinetics were assessed non-invasively via in vivo fluorescence imaging (FI) and ex vivo in excised organs over 2 days. PC liposomes, conventionally formulated, were rapidly cleared from the circulation, while PEGylation resulted in prolongation of liposome circulation robustly distributing among most organs. In contrast, PS and PG liposomes, both as conventional or PEGylated formulations, were rapidly cleared. Non-PEGylated PS and PG liposomes did accumulate almost exclusively in the liver. In contrast, PEGylated PS and PG liposomes were observed mainly in liver and spleen. In summary, PEGylation of PS and PG liposomes was not effective to prolong the circulation time but caused a higher uptake in the spleen. Full article
(This article belongs to the Special Issue Recent Advances in the Use of Phospholipids in Drug Delivery)
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Review

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36 pages, 1457 KiB  
Review
The Phospholipid Research Center: Current Research in Phospholipids and Their Use in Drug Delivery
by Simon Drescher and Peter van Hoogevest
Pharmaceutics 2020, 12(12), 1235; https://doi.org/10.3390/pharmaceutics12121235 - 18 Dec 2020
Cited by 67 | Viewed by 7603
Abstract
This review summarizes the research on phospholipids and their use for drug delivery related to the Phospholipid Research Center Heidelberg (PRC). The focus is on projects that have been approved by the PRC since 2017 and are currently still ongoing or have recently [...] Read more.
This review summarizes the research on phospholipids and their use for drug delivery related to the Phospholipid Research Center Heidelberg (PRC). The focus is on projects that have been approved by the PRC since 2017 and are currently still ongoing or have recently been completed. The different projects cover all facets of phospholipid research, from basic to applied research, including the use of phospholipids in different administration forms such as liposomes, mixed micelles, emulsions, and extrudates, up to industrial application-oriented research. These projects also include all routes of administration, namely parenteral, oral, and topical. With this review we would like to highlight possible future research directions, including a short introduction into the world of phospholipids. Full article
(This article belongs to the Special Issue Recent Advances in the Use of Phospholipids in Drug Delivery)
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