Development of a microemulsion loaded with epoxy-?-lapachone against Leishmania (Leishmania) amazonensis murine infection

被引：8

作者：

Peixoto, Juliana Figueiredo ^{[1
]}

Goncalves-Oliveira, Luiz Filipe ^{[1
]}

Souza-Silva, Franklin ^{[1
,2
]}

Cortes, Luzia Monteiro de Castro ^{[1
]}

Dias-Lopes, Geovane ^{[1
]}

Cardoso, Flavia de Oliveira ^{[3
]}

Santos, Rafael de Oliveira ^{[4
,5
]}

Patricio, Beatriz Ferreira de Carvalho ^{[6
,7
]}

Nicoletti, Caroline Deckmann ^{[8
]}

Lima, Carolina Guimaraes de Souza ^{[8
]}

Calabrese, Katia da Silva ^{[3
]}

Moreira, Davyson de Lima ^{[4
,5
]}

Rocha, Helvecio Vinicius Antunes ^{[6
]}

da Silva, Fernando de Carvalho ^{[8
]}

Ferreira, Vitor Francisco ^{[8
,9
]}

Alves, Carlos Roberto ^{[1
]}

机构：

[1] Fundacao Oswaldo Cruz, Lab Biol Mol & Doencas Endem, Inst Oswaldo Cruz, Ave Brasil 4365, BR-21040900 Rio De Janeiro, RJ, Brazil

[2] Univ Iguacu, Ave Abilio Augusto Tavora 2134, BR-26260045 Nova Iguacu, RJ, Brazil

[3] Fundacao Oswaldo Cruz, Lab Imunomodulacao & Protozool, Inst Oswaldo Cruz, Ave Brasil 4365, BR-21040900 Rio De Janeiro, RJ, Brazil

[4] Fundacao Oswaldo Cruz, Dept Prod Nat, Inst Tecnol Farmacos, Farmanguinhos, Sizenando Nabuco 100, BR-21041250 Rio De Janeiro, RJ, Brazil

[5] Inst Pesquisas Jardim Bot Rio de Janeiro, Lab Prod Nat, Jardim Bot, Rua Pacheco Leao 15, BR-22460030 Rio De Janeiro, RJ, Brazil

[6] Fundacao Oswaldo Cruz, Lab Micro & Nanotecnol, Farmanguinhos, Ave Brasil 4036, BR-21040361 Rio De Janeiro, RJ, Brazil

[7] Univ Fed Estado Rio de Janeiro, Lab Farmacol, Inst Biomed, Rua Frei Caneca 94, BR-20211040 Rio De Janeiro, RJ, Brazil

[8] Univ Fed Fluminense, Dept Quim Organ, Inst Quim, Outeiro Sao Joao Batista S-N, BR-24020141 Niteroi, RJ, Brazil

[9] Univ Fed Fluminense, Fac Farm, Dept Tecnol Farmaceut, Rua Dr Mario Vianna 523, BR-24241002 Niteroi, RJ, Brazil

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2023年 / 636卷

关键词：

Leishmaniaspp; Experimental treatment; Epoxy-?-lapachone; Nanotechnology; Microemulsion; CUTANEOUS LEISHMANIASIS; NEW-WORLD; DELIVERY; DRUG; NAPHTHOQUINONES; STIBOGLUCONATE; MILTEFOSINE; PAROMOMYCIN; ANTIMONIATE; DESIGN;

D O I：

10.1016/j.ijpharm.2023.122864

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Epoxy-alpha-lapachone (ELAP), an oxirane-functionalized molecule synthesized from naturally occurring lapachol, has shown promising activity against murine infection with Leishmania (Leishmania) amazonensis. Herein, we report the successful development of oil-in-water-type (o/w) microemulsions (ME) loaded with ELAP (ELAP-ME) using Capmul MCM, Labrasol, and PEG 400. Stability studies revealed that ELAP-ME (100 mu g/mL of ELAP), which was comprised of globule size smaller than 120.4 +/- 7.7 nm, displayed a good stability profile over 73 days. ELAP-ME had an effect in BALB/c mice infected with L. (L.) amazonensis, causing reductions in paw lesions after two weeks of treatment (similar to 2-fold) when compared to untreated animals. Furthermore, there was also a reduction in the parasite load both in the footpad (60.3%) and in the lymph nodes (31.5%). Based on these findings, ELAP-ME emerges as a promising treatment for tegumentar leishmaniasis.

引用

页数：10

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