Phosphatidylserine (PS) and phosphatidylglycerol (PG) nanodispersions as potential anti-inflammatory therapeutics: Comparison of in vitro activity and impact of pegylation

Klein, Miriam Elisabeth; Mauch, Simone; Rieckmann, Max; Martínez, Dailén García; Hause, Gerd; Noutsias, Michel; Hofmann, Ulrich; Lucas, Henrike; Meister, Annette; Ramos, Gustavo; Loppnow, Harald

doi:10.1016/j.nano.2019.102096

Cited by 22 publications

(24 citation statements)

References 55 publications

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“…A previous study reported that palmitoyl-oleoyl-PG inhibits eicosanoid production in macrophages stimulated by Mycoplasma pneumoniae, insofar as saturated PG and saturated and unsaturated phosphatidylcholines did not have a significant effect on M. pneumoniae-induced arachidonic acid (ARA) release [10]. It has been demonstrated as well that PG-liposome decreases TNF-α production of lipopolysaccharide-stimulated macrophages in vitro [11]. On the other hand, we reported the preparation of n-3 PUFA-PG from salmon roe PL through phospholipase D (PLD)-mediated transphosphatidylation [12,13].…”

Section: Introductionmentioning

confidence: 99%

The Effect of n-3 PUFA Binding Phosphatidylglycerol on Metabolic Syndrome-Related Parameters and n-3 PUFA Accretion in Diabetic/Obese KK-Ay Mice

et al. 2019

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n-3 Polyunsaturated fatty acid binding phospholipids (n-3 PUFA-PLs) are known to be potent carriers of n-3 PUFAs and provide health benefits. We previously prepared n-3 PUFA binding phosphatidylglycerol (n-3 PUFA-PG) by phospholipase D-mediated transphosphatidylation. Because PG has excellent emulsifiability, n-3 PUFA-PG is expected to work as a functional molecule with properties of both PG and n-3 PUFAs. In the present study, the health benefits and tissue accretion of dietary n-3 PUFA-PG were examined in diabetic/obese KK-Ay mice. After a feeding duration over 30 days, n-3 PUFA-PG significantly reduced the total and non-HDL cholesterols in the serum of diabetic/obese KK-Ay mice. In the mice fed n-3 PUFA-PG, but not n-3 PUFA-TAG, hepatic lipid content was markedly alleviated depending on the neutral lipid reduction compared with the SoyPC-fed mice. Further, the n-3 PUFA-PG diet increased eicosapentaenoic acid and docosahexaenoic acid (DHA) and reduced arachidonic acid in the small intestine, liver, perirenal white adipose tissue, and brain, and the ratio of the n-6 PUFAs to n-3 PUFAs in those tissues became lower compared to the SoyPC-fed mice. Especially, the DHA level was more significantly elevated in the brains of n-3 PUFA-PG-fed mice compared to the SoyPC-fed mice, whereas n-3 PUFA-TAG did not significantly alter DHA in the brain. The present results indicate that n-3 PUFA-PG is a functional lipid for reducing serum and liver lipids and is able to supply n-3 PUFAs to KK-Ay mice.

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Section: Introductionmentioning

confidence: 99%

The Effect of n-3 PUFA Binding Phosphatidylglycerol on Metabolic Syndrome-Related Parameters and n-3 PUFA Accretion in Diabetic/Obese KK-Ay Mice

et al. 2019

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“…In a similar context, the project of Karsten Mäder and Annette Meister (Martin Luther University Halle-Wittenberg, Halle/Saale, Germany) is about to develop and characterize anti-inflammatory phospholipid depot formulations including PS-and PG-enriched extrudates and nanofibers, respectively, for the local therapy in brain, ear, and eye. The project is based on the encouraging results [138] obtained with PC extrudates for controlled release [139] and the biological activity of PS and PG-containing phospholipid nanodispersions. PS [140]-as well as PG [141,142]-containing phospholipid depot systems have high potential for the local treatment of inflammation.…”

Section: Ongoingmentioning

confidence: 99%

The Phospholipid Research Center: Current Research in Phospholipids and Their Use in Drug Delivery

Drescher

Hoogevest

2020

Pharmaceutics

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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.

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“…[ 15 ] PG‐based liposomes have shown anti‐inflammatory activities in a recent in vitro study with decreased TNFα‐production of lipopolysaccharide‐stimulated mouse peritoneal macrophages. [ 16 ] Other headgroups, such as phosphatic acid (PA), with a crucial role in vesicle trafficking and endocytosis, [ 17 ] have been shown to be taken up by alveolar macrophages upon administration of PA‐based liposomal aerosols in vivo. Finally, given the high expression of mannose receptors (MRs) in most tissue‐resident macrophages and certain MdMs, mannosylated liposomes have also demonstrated efficient macrophage targeting, both in vitro and in vivo.…”

Section: Introductionmentioning

confidence: 99%

Beyond Trial and Error: A Systematic Development of Liposomes Targeting Primary Macrophages

Weber

Ivan

Proulx

et al. 2021

Advanced NanoBiomed Research

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Monocytes/macrophages are phagocytic innate immune cells playing a pivotal role in tissue homeostasis, inflammation, and antitumor immunity in a microenvironment‐dependent manner. By expressing pattern recognition and scavenger receptors on their surface, macrophages selectively take up pathogens, cellular debris, and often—undesirably—drug delivery systems. On the other hand, the propensity of phagocytic cells to internalize particulate drug carriers is used to load them with a cargo of choice, turning the monocytes/macrophages into a diagnostic or therapeutic Trojan horse. Identifying the ideal physicochemical properties of particulate carriers such as liposomes to achieve the most efficient macrophage‐mediated drug delivery has been object of extensive research in the past, but the studies reported so far rely solely on trial‐and‐error approaches. Herein, a design of experiment (DoE) strategy to identify the optimal liposomal formulation is proposed, fully characterized in terms of size, surface charge, and membrane fluidity, to maximize macrophage targeting. The findings are validated using mouse bone marrow‐derived macrophages, a primary preparation modeling in vivo monocyte‐derived macrophages, thus confirming the robustness and versatility of the systematic and iterative approach and suggesting the promising potential of the DoE approach for the design of cell‐targeting delivery systems.

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Phosphatidylserine (PS) and phosphatidylglycerol (PG) nanodispersions as potential anti-inflammatory therapeutics: Comparison of in vitro activity and impact of pegylation

Cited by 22 publications

References 55 publications

The Effect of n-3 PUFA Binding Phosphatidylglycerol on Metabolic Syndrome-Related Parameters and n-3 PUFA Accretion in Diabetic/Obese KK-Ay Mice

The Effect of n-3 PUFA Binding Phosphatidylglycerol on Metabolic Syndrome-Related Parameters and n-3 PUFA Accretion in Diabetic/Obese KK-Ay Mice

The Phospholipid Research Center: Current Research in Phospholipids and Their Use in Drug Delivery

Beyond Trial and Error: A Systematic Development of Liposomes Targeting Primary Macrophages

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