Design and characterization of Squalene-Gusperimus nanoparticles for modulation of innate immunity

In Vitro Studies of Squalene‐Gusperimus Nanoparticles in Islet‐Containing Alginate Microcapsules to Regulate the Immune Response in the Immediate Posttransplant Period

“…To facilitate sustained release of gusperimus, we previously encapsulated gusperimus by binding it to squalene to form Sq-GusNPs after nanoprecipitation. [21] By this, we avoid the stability issues associated with the free drug under physiological conditions, which cause loss of its immunosuppressive activity. [21][22][23] The Sq-GusNPs were then incorporated into alginate microcapsules by suspending them in an alginate solution followed by gelation in 100 mM CaCl 2 to immobilize the NPs.…”

“…[21] By this, we avoid the stability issues associated with the free drug under physiological conditions, which cause loss of its immunosuppressive activity. [21][22][23] The Sq-GusNPs were then incorporated into alginate microcapsules by suspending them in an alginate solution followed by gelation in 100 mM CaCl 2 to immobilize the NPs. Subsequently, the immunomodulatory effects were determined by studying cytokine release from LPS-stimulated U-937 macrophages when cultured with alginate microcapsules or Sq-GusNP-containing alginate microcapsules.…”

“…This may be done with gusperimus, a proven potent inhibitor of macrophages, which are the driving force behind the foreign body responses. [20] Recently we developed a controlled release system in which gusperimus was nanoencapsulated as squalene-gusperimus nanoparticles (Sq-GusNPs) [21] to avoid stability issues and loss of activity associated with free gusperimus. [21][22][23] These nanoparticles (NPs) are shown to be stable, have a high drug-loading capacity, high uptake, and lack of toxicity, and exert an enhanced anti-inflammatory activity over time compared with free gusperimus.…”

“…[20] Recently we developed a controlled release system in which gusperimus was nanoencapsulated as squalene-gusperimus nanoparticles (Sq-GusNPs) [21] to avoid stability issues and loss of activity associated with free gusperimus. [21][22][23] These nanoparticles (NPs) are shown to be stable, have a high drug-loading capacity, high uptake, and lack of toxicity, and exert an enhanced anti-inflammatory activity over time compared with free gusperimus. [21] Here we applied and tested this system when loaded into alginate microcapsules, which could be transplanted together with encapsulated islets to reduce immune responses in the immediate posttransplant period.…”

“…[21][22][23] These nanoparticles (NPs) are shown to be stable, have a high drug-loading capacity, high uptake, and lack of toxicity, and exert an enhanced anti-inflammatory activity over time compared with free gusperimus. [21] Here we applied and tested this system when loaded into alginate microcapsules, which could be transplanted together with encapsulated islets to reduce immune responses in the immediate posttransplant period. We studied the effect of Sq-GusNPs on pancreatic islets and immune cells after their incorporation into alginate microcapsules and we determined the anti-inflammatory effect after triggering a proinflammatory response in macrophages in vitro.…”