Abstract (EN):
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 (similar to 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 BNIIPDaoct per se or the amphotericin B, respectively. Conclusion: PLGA nanoparticles provide controlled and effective delivery of BNIPDaoct for treatment of VL. Original submitted 23 December 2012; Revised submitted 5 April 2012; Published online 20 July 2012
Language:
English
Type (Professor's evaluation):
Scientific
No. of pages:
11