Phosphatidylserine (PS) and phosphatidylglycerol (PG) enriched mixed micelles (MM): A new nano-drug delivery system with anti-inflammatory potential?

Klein, Miriam Elisabeth; Rieckmann, Max; Lucas, Henrike; Meister, Annette; Loppnow, Harald

doi:10.1016/j.ejps.2020.105451

Cited by 14 publications

(13 citation statements)

References 63 publications

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“…The interaction between the phospholipid and SPI can be achieved in a variety of ways, including hydrophobic and electrostatic interactions [20] . Phosphatidylserine (PS) is a natural phospholipid with an irreplaceable role in biological cell membranes, showing great physicochemical properties and biological activity, and has been used in the preparation of mixed micelles [21] , nanodispersions [22] , and liposomes [23] . PS has a negatively charged head.…”

Section: Introductionmentioning

confidence: 99%

Effect of ultrasound on the structural characteristics and oxidative stability of walnut oil oleogel coated with soy protein isolate-phosphatidylserine

Wang

Gong

et al. 2022

Ultrasonics Sonochemistry

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Section: Introductionmentioning

confidence: 99%

Effect of ultrasound on the structural characteristics and oxidative stability of walnut oil oleogel coated with soy protein isolate-phosphatidylserine

Wang

Gong

et al. 2022

Ultrasonics Sonochemistry

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“…This can be explained by different phagocytosis rates and mechanisms, as PS can be engulfed by cells of the MPS and others, e.g., by hepatocytes [56] or fibroblasts, whereas PG is only phagocytized by monocytes and macrophages [56]. Furthermore, we previously observed PS being more potently engulfed than PG in vitro [42]. The variation in their phagocytosis activities may also explain the differences between the in vivo biodistribution profiles of PS and PG.…”

Section: Discussionmentioning

confidence: 90%

“…Liposomes were prepared as previously described [40,42]. Briefly, stock solutions of PLs were prepared in chloroform:methanol (4:1, v/v).…”

Section: Liposome Preparationmentioning

confidence: 99%

Towards the Development of Long Circulating Phosphatidylserine (PS)- and Phosphatidylglycerol (PG)-Enriched Anti-Inflammatory Liposomes: Is PEGylation Effective?

et al. 2021

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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.

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“…PS delivered in a micelle formulation was recently shown to stimulate the polarization of macrophages from the pro-inflammatory to anti-inflammatory phenotype ( Klein et al ., 2020 ). This was consistent with previous reports associating PS treatment with down-regulation of pro-inflammatory cytokines (e.g., TNF-α and IL-6) and increased secretion of anti-inflammatory mediators (e.g., IL-10 and TGF-β) ( Szondy et al ., 2017 ).…”

Section: Glycerophospholipidsmentioning

confidence: 99%

“…This was consistent with previous reports associating PS treatment with down-regulation of pro-inflammatory cytokines (e.g., TNF-α and IL-6) and increased secretion of anti-inflammatory mediators (e.g., IL-10 and TGF-β) ( Szondy et al ., 2017 ). Indeed, micelles enriched with 1,2-dioleoyl-sn-glycero-3-phospho-L-serine (DOPS) significantly reduced the release of TNF-α by LPS-activated macrophages, indicating an anti-inflammatory effect ( Klein et al ., 2020 ).…”

Section: Glycerophospholipidsmentioning

confidence: 99%

Bioactive Lipids and Their Derivatives in Biomedical Applications

Park

Choi

Kim

et al. 2021

Biomolecules & Therapeutics

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Lipids, which along with carbohydrates and proteins are among the most important nutrients for the living organism, have a variety of biological functions that can be applied widely in biomedicine. A fatty acid, the most fundamental biological lipid, may be classified by length of its aliphatic chain, and the short-, medium-, and long-chain fatty acids and each have distinct biological activities with therapeutic relevance. For example, short-chain fatty acids have immune regulatory activities and could be useful against autoimmune disease; medium-chain fatty acids generate ketogenic metabolites and may be used to control seizure; and some metabolites oxidized from long-chain fatty acids could be used to treat metabolic disorders. Glycerolipids play important roles in pathological environments, such as those of cancers or metabolic disorders, and thus are regarded as a potential therapeutic target. Phospholipids represent the main building unit of the plasma membrane of cells, and play key roles in cellular signaling. Due to their physical properties, glycerophospholipids are frequently used as pharmaceutical ingredients, in addition to being potential novel drug targets for treating disease. Sphingolipids, which comprise another component of the plasma membrane, have their own distinct biological functions and have been investigated in nanotechnological applications such as drug delivery systems. Saccharolipids, which are derived from bacteria, have endotoxin effects that stimulate the immune system. Chemically modified saccharolipids might be useful for cancer immunotherapy or as vaccine adjuvants. This review will address the important biological function of several key lipids and offer critical insights into their potential therapeutic applications.

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Phosphatidylserine (PS) and phosphatidylglycerol (PG) enriched mixed micelles (MM): A new nano-drug delivery system with anti-inflammatory potential?

Cited by 14 publications

References 63 publications

Effect of ultrasound on the structural characteristics and oxidative stability of walnut oil oleogel coated with soy protein isolate-phosphatidylserine

Effect of ultrasound on the structural characteristics and oxidative stability of walnut oil oleogel coated with soy protein isolate-phosphatidylserine

Towards the Development of Long Circulating Phosphatidylserine (PS)- and Phosphatidylglycerol (PG)-Enriched Anti-Inflammatory Liposomes: Is PEGylation Effective?

Bioactive Lipids and Their Derivatives in Biomedical Applications

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