Cinnamic acid derived compounds loaded into liposomes: antileishmanial activity, production standardisation and characterisation

被引:8
作者
Campos Cury, Thuanny Alexandra [1 ]
Yoneda, Juliana Sakamoto [1 ]
Zuliani, Juliana Pavan [2 ,3 ]
Soares, Andreimar Martins [4 ]
Stabeli, Rodrigo Guerino [5 ]
Calderon, Leonardo de Azevedo [4 ,6 ]
Ciancaglini, Pietro [1 ]
机构
[1] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, Dept Quim, BR-14040901 Sao Paulo, Brazil
[2] Univ Fed Rondonia UNIR, Fundacao Oswaldo Cruz Fiocruz, Lab Imunol Celular Aplicada Saude, Fiocruz Rondonia, Porto Velho, Rondonia, Brazil
[3] Univ Fed Rondonia UNIR, Dept Med, Porto Velho, Rondonia, Brazil
[4] Fundacao Oswaldo Cruz Fiocruz, Ctr Estudos Biomol Aplicadas Saude, Fiocruz Rondonia, Porto Velho, Rondonia, Brazil
[5] Ctr Nanotecnol Aplicada Saude Nanosus, Presidencia Fiocruz, Curitiba, Parana, Brazil
[6] Univ Fed Rondonia UNIR, Dept Med, Porto Velho, Rondonia, Brazil
基金
巴西圣保罗研究基金会;
关键词
Antileishmanial activity; drug carrier; Leishmaniasis; liposomes; Leishmania amazonensis; PIPER-TUBERCULATUM JACQ; LEISHMANIA-AMAZONENSIS; MEGLUMINE ANTIMONIATE; IN-VITRO; PHOSPHATIDYLCHOLINE; MACROPHAGE; DIVERSITY; SPP;
D O I
10.3109/02652048.2015.1046518
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Synthetic compounds derived from cinnamic acid were tested in cultures containing the promastigote form of Leishmania amazonensis and the dimethylsulphoxide solution of B2 compound (2.0 mg/mL) led to a 92% decrease of leishmania in 96 h of treatment. Then, different liposomal systems (diameters similar to 200 nm) were prepared by the extrusion method in the presence and absence of compounds studied. DSC thermograms of the liposomes in the presence of these compounds caused changes in Delta H, T-m and Delta T-1/2, compared to controls, indicating that there was an interaction of the compounds with the lipid bilayer. Assays with negatively charged liposomal systems containing these drugs in L. amazonensis cultures led to a 50-80% decrease in the number of leishmanias with a concentration to 100 times lower when compared to the B2 initial test. These liposomal systems are promoting more interaction and delivery of the compounds and proved to be an efficient, stable and promising system.
引用
收藏
页码:467 / 477
页数:11
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