{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,11,3]],"date-time":"2026-11-03T11:31:43Z","timestamp":1793705503655,"version":"4.5.1"},"reference-count":35,"publisher":"Cambridge University Press (CUP)","issue":"9","license":[{"start":{"date-parts":[[2020,5,4]],"date-time":"2020-05-04T00:00:00Z","timestamp":1588550400000},"content-version":"unspecified","delay-in-days":0,"URL":"https:\/\/www.cambridge.org\/core\/terms"}],"content-domain":{"domain":["cambridge.org"],"crossmark-restriction":true},"short-container-title":["Parasitology"],"published-print":{"date-parts":[[2020,8]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Cutaneous leishmaniasis (CL) is a major health problem in many countries and its current treatment involves multiple parenteral injections with toxic drugs and requires intensive health services. Previously, the efficacy of a single subcutaneous injection with a slow-release formulation consisting of poly(lactide-co-glycolide) (PLGA) microparticles loaded with an antileishmanial 3-nitro-2-hydroxy-4,6-dimethoxychalcone (CH8) was demonstrated in mice model. In the search for more easily synthesized active chalcone derivatives, and improved microparticle loading, CH8 analogues were synthesized and tested for antileishmanial activity<jats:italic>in vitro<\/jats:italic>and<jats:italic>in vivo<\/jats:italic>. The 3-nitro-2\u2032,4\u2032,6\u2032-trimethoxychalcone (NAT22) analogue was chosen for its higher selectivity against intracellular amastigotes (selectivity index = 1489, as compared with 317 for CH8) and more efficient synthesis (89% yield, as compared with 18% for CH8). NAT22 was loaded into PLGA \/ polyvinylpyrrolidone (PVP) polymeric blend microspheres (NAT22-PLGAk) with average diameter of 1.9<jats:italic>\u03bc<\/jats:italic>m. Although NAT22-PLGAk showed similar activity to free NAT22 in killing intracellular parasites<jats:italic>in vitro<\/jats:italic>(IC<jats:sub>50<\/jats:sub>~ 0.2<jats:italic>\u03bc<\/jats:italic><jats:sc>m<\/jats:sc>),<jats:italic>in vivo<\/jats:italic>studies in<jats:italic>Leishmania amazonensis<\/jats:italic>\u2013 infected mice demonstrated the significant superior efficacy of NAT22-PLGAk to reduce the parasite load. A single intralesional injection with NAT22-PLGAk was more effective than eight injections with free NAT22. Together, these results show that NAT22-PLGAk is a promising alternative for single-dose localized treatment of CL.<\/jats:p>","DOI":"10.1017\/s0031182020000712","type":"journal-article","created":{"date-parts":[[2020,5,4]],"date-time":"2020-05-04T09:56:55Z","timestamp":1588586215000},"page":"1032-1037","update-policy":"https:\/\/doi.org\/10.1017\/policypage","source":"Crossref","is-referenced-by-count":14,"title":["Single-dose treatment for cutaneous leishmaniasis with an easily synthesized chalcone entrapped in polymeric microparticles"],"prefix":"10.1017","volume":"147","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1642-6669","authenticated-orcid":false,"given":"Ariane J.","family":"Sousa-Batista","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Natalia","family":"Arruda-Costa","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Douglas 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