Macrophage apoptosis using alendronate in targeted nanoarchaeosomes

Nanoarchaeosomes are non-hydrolysable nanovesicles made of archaeolipids, naturally functionalised with ligand for scavenger receptor class 1. We hypothesized that nitrogenate bisphosphonate alendronate (ALN) loaded nanoarchaeosomes (nanoarchaeosomes(ALN)) may constitute more efficient macrophage targeted apoptotic inducers than ALN nanoliposomes (nanoliposomes (ALN)). To aim, was in cholesterol containing (nanoARC-chol(ALN)) or not (nanoARC(ALN)) nanoarchaeosomes. Nanoarchaeosomes(ALN) (220–320 nm sized, ~ −40 mV ξ potential, 38–50 μg ALN/mg lipid ratio) displayed higher structural stability nanoliposomes(ALN) matching size and retaining most against a 1/200 folds dilution. The cytotoxicity nanoARC(ALN) on J774A.1 cells, resulted > 30 free reduced by nanoARC-chol(ALN). Devoid ALN, nanoARC-chol non-cytotoxic, exhibited pronounced anti-inflammatory activity J774.1 strongly reducing reactive oxygen species (ROS) IL-6 induced LPS. bilayer extensively interacted serum proteins but refractory to phospholipases. Upon cells uptake, cytoplasmic acid vesicles, the mitochondrial membrane potential 20–40 % without consuming ATP neither damaging lysosomes increasing pERK. Refractory chemoenzymatic attacks, either void drug loaded, anti-inflammation macrophages apoptosis, constituting promising multiple therapeutic purposes.