Present studies are aimed to find out the utility of oil-in-water
emulsions also known as
lipid nanospheres (LN) or fat
emulsions for delivering
piperine for the treatment of
visceral leishmaniasis.
Lipid nanosphere formulations of
piperine were prepared using
soybean oil, egg
lecithin,
cholesterol,
stearylamine and
phosphatidylethanolamine distearylmethoxypolyethyleneglycol (
DSPE-PEG) by homogenization followed by ultrasonication of oil and aqueous phases. Antileishmanial activity of all the formulations was assessed in BALB/c mice infected with Leishmania donovani AG83 for 60 days. A single dose (5 mg/kg) of
piperine, or
lipid nanospheres of
piperine (LN-P), or
lipid nanosphere of
piperine with
stearylamine (LN-P-SA) or pegylated
lipid nanospheres of
piperine (LN-P-PEG) was injected intravenously. Mice were sacrificed after 15 days of treatment with
piperine or formulations and Leishman Donovan Unit (LDU) is counted. Toxicity of formulations and pure
piperine was assessed in normal mice. The size distribution of formulations ranged from 200 to 885 nm.
Piperine reduced the parasite burden in liver and spleen by 38% and 31% after 15 days post
infection respectively. LN-P reduced the parasite burden in liver and spleen by 63% and 52% after 15 days post
infection, respectively. LN-P-PEG reduced the parasite burden in liver and spleen by 78% and 75% after 15 days post
infection, respectively. LN-P-SA reduced the parasite burden in liver and spleen by 90% and 85% after 15 days post
infection, respectively. LN-P, LN-P-PEG, LN-P-SA treated mice did not show any significant changes in the serum levels of
SGOT, ALP,
creatinine and
urea compared to normal mice. Stable and sterile formulations of
lipid nanospheres of
piperine were developed. A single dose of 5 mg/kg of
lipid nanospheres of
piperine could significantly reduce the liver and splenic parasite burden.