Liposomal aggregates sustain the release of rapamycin and protect cartilage from friction.

Bordon, Gregor; Ramakrishna, Shivaprakash N; Edalat, Sam G; Eugster, Remo; Arcifa, Andrea; Vermathen, Martina; Aleandri, Simone; Bertoncelj, Mojca Frank; Furrer, Julien; Vermathen, Peter; Isa, Lucio; Crockett, Rowena; Distler, Oliver; Luciani, Paola (2023). Liposomal aggregates sustain the release of rapamycin and protect cartilage from friction. Journal of Colloid and Interface Science, 650(Pt B), pp. 1659-1670. Elsevier 10.1016/j.jcis.2023.07.087

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Liposomes show promise as biolubricants for damaged cartilage, but their small size results in low joint and cartilage retention. We developed a zinc ion-based liposomal drug delivery system for local osteoarthritis therapy, focusing on sustained release and tribological protection from phospholipid lubrication properties. Our strategy involved inducing aggregation of negatively charged liposomes with zinc ions to extend rapamycin (RAPA) release and improve cartilage lubrication. Liposomal aggregation occurred within 10 min and was irreversible, facilitating excess cation removal. The aggregates extended RAPA release beyond free liposomes and displayed irregular morphology influenced by RAPA. At nearly 100 µm, the aggregates were large enough to exceed the previously reported size threshold for increased joint retention. Tribological assessment on silicon surfaces and ex vivo porcine cartilage revealed the system's excellent protective ability against friction at both nano- and macro-scales. Moreover, RAPA was shown to attenuate the fibrotic response in human OA synovial fibroblasts. Our findings suggest the zinc ion-based liposomal drug delivery system has potential to enhance OA therapy through extended release and cartilage tribological protection, while also illustrating the impact of a hydrophobic drug like RAPA on liposome aggregation and morphology.

Item Type:

Journal Article (Original Article)


08 Faculty of Science > Department of Chemistry, Biochemistry and Pharmaceutical Sciences (DCBP)
04 Faculty of Medicine > Department of Radiology, Neuroradiology and Nuclear Medicine (DRNN) > Institute of Diagnostic, Interventional and Paediatric Radiology

UniBE Contributor:

Bordon, Gregor, Eugster, Remo, Vermathen, Martina, Aleandri, Simone, Furrer, Julien, Vermathen, Peter, Luciani, Paola


500 Science > 570 Life sciences; biology
500 Science > 540 Chemistry
600 Technology > 610 Medicine & health








Pubmed Import

Date Deposited:

27 Jul 2023 14:20

Last Modified:

17 Aug 2023 00:16

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PubMed ID:


Uncontrolled Keywords:

Aggregation kinetics Cartilage lubrication Liposomal aggregates Liposomal morphology Osteoarthritis Rapamycin Sustained release Synovial fibroblasts




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