2022
DOI: 10.1039/d1tb02346b
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Poly-phosphocholination of liposomes leads to highly-extended retention time in mice joints

Abstract: Surface-attached layers of phosphatidylcholine (PC) lipid vesicles (liposomes) may reduce the friction coefficient μ (= force-to-slide/load) between the sliding surfaces down to μ ≈ 10-3 – 10-4 up to tens...

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Cited by 25 publications
(15 citation statements)
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“…For example, Lipotalon® (Merckle, Germany) is the first used liposome formulation in Germany to clinically treat OA by IA delivery, 43 containing dexamethasone palmitate as active ingredient, preferentially taken up by synovial macrophages after IA injection and transformed to its active form by intracellular esterases, thus preventing the side effects of free dexamethasone (synovitis and tissue irritation). 99 , 100 …”
Section: Different Drug-delivery Systems For Intra-articular Injectio...mentioning
confidence: 99%
“…For example, Lipotalon® (Merckle, Germany) is the first used liposome formulation in Germany to clinically treat OA by IA delivery, 43 containing dexamethasone palmitate as active ingredient, preferentially taken up by synovial macrophages after IA injection and transformed to its active form by intracellular esterases, thus preventing the side effects of free dexamethasone (synovitis and tissue irritation). 99 , 100 …”
Section: Different Drug-delivery Systems For Intra-articular Injectio...mentioning
confidence: 99%
“…Although liposomes offer several advantages over other carrier systems, such as the ability to carry both hydrophobic and hydrophilic compounds, high encapsulation efficiency, biocompatibility, and transport ability through cell membranes, they are thermodynamically unstable systems prone to aggregation, fusion, degradation, or hydrolyzation, resulting in leakage of the entrapped compounds. The main limitations of liposome application in drug delivery systems are their physical and chemical instability [ 20 , 21 ] and their retention time after both systemic and local application [ 22 ]. Hydrophobic interactions are responsible for their physical instability, while degradative lipid oxidation determines their chemical instability.…”
Section: Introductionmentioning
confidence: 99%
“…It was also found that such PMPCylated liposomes intra-articularly (IA) injected into mice joints showed a significant increase in retention half-life compared with PEGylated liposomes. [44] In order to reduce friction between surfaces, the liposomes must adsorb on the substrate to form boundary layers. Non-functionalized PC liposomes adsorb on negatively charged surfaces via dipole-charge interactions between the phosphocholine zwitterions and the negative surface charges.…”
Section: Introductionmentioning
confidence: 99%