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

J Microencapsul

Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto (FFCLRP), Universidade de São Paulo , Ribeirão Preto, São Paulo , Brazil .

Published: May 2016

AI Article Synopsis

  • Synthetic compounds from cinnamic acid significantly reduced Leishmania amazonensis in cultured cells, with a notable 92% decrease after 96 hours using a specific B2 compound.
  • The creation of liposomal systems (about 200 nm in diameter) showed altered thermal properties in the presence of these compounds, suggesting they interacted with the lipid bilayer.
  • When used in negatively charged liposomal systems, these drugs decreased the leishmania count by 50-80% at much lower concentrations than the initial B2 test, indicating that liposomes enhance drug delivery and effectiveness.

Article Abstract

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 ∼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 ΔH, Tm and ΔT1/2, 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.

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Source
http://dx.doi.org/10.3109/02652048.2015.1046518DOI Listing

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