Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases

Abstract EN

Buparvaquone (BPQ), a veterinary drug, was formulated as nanostructured lipid carriers (NLC) for leishmaniases treatment.

The formulation design addressed poor water solubility of BPQ and lack of human drug delivery system.

The DSC/TG and microscopy methods were used for solid lipids screening.

Softisan® 154 showed highest BPQ solubility in both methods.

The BPQ solubility in liquid lipids using HPLC revealed Miglyol® 812 as the best option.

Response surface methodology (RSM) was used to identify the optimal Softisan154 : Miglyol 812 ratios (7 : 10 to 2 : 1) and Kolliphor® P188 and Tween® 80 concentration (>3.0% w/w) aiming for z-average in the range of 100–300 nm for macrophage delivery.

The NLC obtained by high-pressure homogenization showed low z-averages (<350 nm), polydispersity (<0.3), and encapsulation efficiency close to 100%.

DSC/TG and microscopy in combination proved to be a powerful tool to select the solid lipid.

The relationship among the variables, demonstrated by a linear mathematical model using RSM, allowed generating a design space.

This design space showed the limits in which changes in the variables influenced the z-average.

Therefore, these drug delivery systems have the potential to improve the availability of affordable medicines due to the low cost of raw materials, using well established, reliable, and feasible scale-up technology.