Characterization and Evaluation of BNIpdaoct-Loaded PLGA Nanoparticles for Visceral Leishmaniasis: In Vitro and In Vivo Studies

OBJECTIVE: To overcome the limitation of bisnaphthalimidopropyldiaaminooctane (BNIPDaoct) low physiological solubility and potentially increase its efficiency against visceral leishmaniasis (VL), a delivery system based on poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles was developed. MATERIALS & METHODS: BNIPDaoct-PLGA nanoparticles were prepared by nanoprecipitation and characterized. Anti-Leishmania activity was evaluated using in vitro and in vivo VL infection models. RESULTS: BNIPDaoct-PLGA nanoparticles were successfully produced and were sized at 156.0 ± 2.8 nm with an encapsulation efficiency of approximately 85%. The PLGA nanoparticles reduced BNIPDaoct cellular toxicity, retained its in vitro anti-leishmanial activity and led to a significant reduction (∼80%) in the parasite burden in the infected mice spleen when compared with the free drug or amphotericin B. In the liver the effect was less pronounced, with a 30-50% reduction observed between the nanoformulation and the BNIPDaoct per se or the amphotericin B, respectively. CONCLUSION: PLGA nanoparticles provide controlled and effective delivery of BNIPDaoct for treatment of VL.