Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity. (15th December 2021)

• Record Type: Journal Article
• Authors: Higuita-Castro, Jorge; Vélez, Iván D.; Escobar, Diana M.; Murillo, Javier; Pineda, Tatiana; Ospina, Victoria; Robledo, Sara M.
• Is Part Of: Materials & design. Volume 212(2021)
• Publication Date: 2021-12-15
• Subjects: SS Extract from Sapindus saponaria L -- TC2 Compound benzoic acid 2-(2, 3-dihydro-4H-1-benzopyran-4-ylidene) hydrazide -- CQ Soft capsule of chitosan with TC2 and SS (1:1) -- CL Cutaneous Leishmaniasis -- SAP Saponins -- ASOG Acyclic sesquiterpene oligoglycosides; Cutaneous leishmaniasis -- Plant extracts -- Leishmanicidal activity -- Drug release kinetics -- In vitro assays -- In vivo studies; Materials -- Periodicals; Engineering design -- Periodicals; Matériaux -- Périodiques; Conception technique -- Périodiques; Electronic journals; 620.11
• DOI: 10.1016/j.matdes.2021.110232
• Languages: English
• ISSNs: 0264-1275

Abstract

Graphical abstract: Highlights: Chitosan softgels containing two leishmanicidal compounds were manufactured by drip. Chitosan softgels release leishmanicidal compounds in a controlled manner. Chitosan softgels with leishmanicidal compounds were effective in the in vivo model. 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.