Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases
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. Soft...
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doaj-1d3b77c33732413693c6c7d5e258ebd62020-11-24T20:40:17ZengHindawi LimitedBioMed Research International2314-61332314-61412017-01-01201710.1155/2017/97816039781603Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of LeishmaniasesLis Marie Monteiro0Raimar Löbenberg1Paulo Cesar Cotrim2Gabriel Lima Barros de Araujo3Nádia Bou-Chacra4Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av 580, Cidade Universitária, 05508-000 São Paulo, SP, BrazilFaculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, 8613 114th St NW, Edmonton, AB, T6G 2H7, CanadaSeroepidemiology, 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, BrazilDepartment of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av 580, Cidade Universitária, 05508-000 São Paulo, SP, BrazilDepartment of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av 580, Cidade Universitária, 05508-000 São Paulo, SP, BrazilBuparvaquone (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.http://dx.doi.org/10.1155/2017/9781603 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Lis Marie Monteiro Raimar Löbenberg Paulo Cesar Cotrim Gabriel Lima Barros de Araujo Nádia Bou-Chacra |
spellingShingle |
Lis Marie Monteiro Raimar Löbenberg Paulo Cesar Cotrim Gabriel Lima Barros de Araujo Nádia Bou-Chacra Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases BioMed Research International |
author_facet |
Lis Marie Monteiro Raimar Löbenberg Paulo Cesar Cotrim Gabriel Lima Barros de Araujo Nádia Bou-Chacra |
author_sort |
Lis Marie Monteiro |
title |
Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases |
title_short |
Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases |
title_full |
Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases |
title_fullStr |
Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases |
title_full_unstemmed |
Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases |
title_sort |
buparvaquone nanostructured lipid carrier: development of an affordable delivery system for the treatment of leishmaniases |
publisher |
Hindawi Limited |
series |
BioMed Research International |
issn |
2314-6133 2314-6141 |
publishDate |
2017-01-01 |
description |
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. |
url |
http://dx.doi.org/10.1155/2017/9781603 |
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