Improved targeting of antimony to the bone marrow of dogs using liposomes of reduced size

Complement activation-related pseudoallergy in dogs following intravenous administration of a liposomal formulation of meglumine antimoniate

“…MA-containing liposomes with reduced size were prepared as described previously (Schettini et al 2006). Briefly, small unilamellar vesicles (SUVs) were obtained by ultrasonication of a suspension of multilamellar vesicles in de-ionized water, made from DSPC, CHOL and DCP (molar ratio of 5:4:1) at the final lipid concentration of 55 g/L.…”

“…The liposome pellet was then washed twice and finally resuspended in isotonic saline at a final antimony concentration of about 10 g/L. The concentration of encapsulated antimony and the phospholipid concentration were determined in the resulting liposome suspension, using previously described colorimetric assays (Schettini et al 2006). The mean hydrodynamic diameter of the vesicles was 400 nm, with a mean polydispersity factor of 0.3.…”

Advanced Drug Carriers Targeting Bone Marrow

“…Schettini and co-workers prepared a novel liposomal formulation of meglumine antimoniate, a drug used for treating leishmaniasis, to deliver the drug to the bone marrow (Schettini et al, 2006). The liposomes were produced from distearoylphosphatidylcholine (DSPC), cholesterol, and dicetylphosphate (molar ratio of 5:4:1).…”

“…This importance suggests that the phagocytic activity of bone marrow is a potent target of nanoparticle-based drug delivery. In fact, it has been demonstrated that nanoparticles modified with a specific molecule on their surface are distributed selectively into bone marrow tissues (Harris et al 2010;Mann et al, 2011;Moghimi, 1995;Porter et al, 1992;Schettini et al, 2006;Sou et al 2007Sou et al , 2010Sou et al , 2011a. These bone marrow-specific drug carrier systems are expected to improve diagnostic and therapeutic systems to treat hematopoietic disorders.…”

Antimonial drugs entrapped into phosphatidylserine liposomes: physicochemical evaluation and antileishmanial activity

“…Considering this limitation, an approach based on the improvement of existing drugs has been more successful than those based on designing new chemical entities (4) . Given that Leishmania parasites colonize macrophages, which are responsible for the clearance of liposomes, the use of liposomes has been studied for many years as an efficient strategy for the delivery of antileishmanial agents to Leishmania-infected tissues and reducing the parasite load (5) (6) . Liposome-encapsulated antimonials were found to be hundreds-fold more effective than the corresponding free drugs for treating experimental visceral leishmaniasis (7) , and could promote suppression of the parasite in the liver and/or spleen (8) .…”