Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity

Abstract

Leishmaniasis is a tropical disease caused by parasites of the genus Leishmania spp; it presents different clinical manifestations, of which cutaneous leishmaniasis is the most common form, and it is endemic in more than 70 countries worldwide. Only four drugs are registered for the treatment of the disease, all associated with high toxicity. Recently, the in vitro and in vivo leishmanicidal activity of a mixture of the benzoic acid 2-(2,3-dihydro-4H-1-benzopyran-4-ylidene) hydrazide (TC2) and the compounds present in the plant extract Sapindus saponaria L (SS) were reported. In the present study were prepared soft capsules of chitosan incorporating TC2 and SS in 1:1 (CQ) ratio showed low cytotoxicity in U937 macrophages but moderate cytotoxicity in Detroit 551 fibroblast and had high antileishmanial activity against intracellular L. braziliensis amastigotes. The kinetics of TC2 release from CQ was fitted to the Korsmeyer-Peppas model. Finally, CQ was effective in treating experimental cutaneous leishmaniasis induced in the hamster model. In conclusion, the CQ are biocompatible and can help treat cutaneous leishmaniasis.

Keywords

• Cutaneous leishmaniasis
• Plant extracts
• Leishmanicidal activity
• Drug release kinetics
• In vitro assays
• In vivo studies