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BioMed Research International
Volume 2017, Article ID 9781603, 11 pages
https://doi.org/10.1155/2017/9781603
Research Article

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

1Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av 580, Cidade Universitária, 05508-000 São Paulo, SP, Brazil
2Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, 8613 114th St NW, Edmonton, AB, Canada T6G 2H7
3Seroepidemiology, Cellular and Molecular Immunology Laboratory, Institute of Tropical Medicine, University of São Paulo, Dr. Enéas de Carvalho Aguiar 470, Jardim América, 05403-000 São Paulo, SP, Brazil

Correspondence should be addressed to Nádia Bou-Chacra; rb.psu@arcahc

Received 8 September 2016; Accepted 5 January 2017; Published 1 February 2017

Academic Editor: Sanjula Baboota

Copyright © 2017 Lis Marie Monteiro et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

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 -average in the range of 100–300 nm for macrophage delivery. The NLC obtained by high-pressure homogenization showed low -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 -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.