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

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art_MONTEIRO_Buparvaquone_Nanostructured_Lipid_Carrier_Development_of_an_Affordable_2017.PDF (2.21 MB)
Citações na Scopus
31
Tipo de produção
article
Data de publicação
2017
DOI
Scopus
Web of Science
PubMed
Título da Revista
ISSN da Revista
Título do Volume
Editora
HINDAWI LTD
Autores
MONTEIRO, Lis Marie
LOBENBERG, Raimar
ARAUJO, Gabriel Lima Barros de
BOU-CHACRA, Nadia
Citação
BIOMED RESEARCH INTERNATIONAL, article ID 9781603, 11p, 2017
Projetos de Pesquisa
Unidades Organizacionais
Fascículo
Resumo
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 (R) 154 showed highest BPQ solubility in both methods. The BPQ solubility in liquid lipids using HPLC revealed Miglyol (R) 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 (R) P188 and Tween (R) 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.
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URI
https://observatorio.fm.usp.br/handle/OPI/18843
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Coleções
Artigos e Materiais de Revistas Científicas - FM/MIP
Artigos e Materiais de Revistas Científicas - LIM/48
Artigos e Materiais de Revistas Científicas - ODS/03