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dc.contributorSistema FMUSP-HC: Faculdade de Medicina da Universidade de São Paulo (FMUSP) e Hospital das Clínicas da FMUSP
dc.contributor.authorSOUZA, Aline de
dc.contributor.authorYUKUYAMA, Megumi Nishitani
dc.contributor.authorBARBOSA, Eduardo Jose
dc.contributor.authorMONTEIRO, Lis Marie
dc.contributor.authorFALOPPA, Ana Cristina Breithaupt
dc.contributor.authorCALIXTO, Leandro Augusto
dc.contributor.authorARAUJO, Gabriel Lima de Barros
dc.contributor.authorFOTAKI, Nikoletta
dc.contributor.authorLOBENBERG, Raimar
dc.contributor.authorBOU-CHACRA, Nadia Araci
dc.identifier.citationCOLLOIDS AND SURFACES B-BIOINTERFACES, v.193, article ID 111097, 8p, 2020
dc.description.abstractHydroxymethilnitrofurazone (NFOH) is a nitrofurazone derivative and has potential use in treating leishmaniasis. However, due to low water solubility and bioavailability, NFOH has failed in in vivo tests. Nanostructured lipid carrier (NLC) is an alternative to overcome these limitations by improving pharmacokinetics and modifying drug delivery. This work is focused on developing a novel NFOH-loaded NLC (NLC-NFOH) using a D-optimal mixture statistical design and high-pressure homogenization, for oral administration to treat leishmaniasis. The optimized NLC-NFOH consisted of Mygliol (R) 840, Gelucire (R) 50/13, and Precirol (R) ATO 5 as lipids. These lipids were selected using a rapid methodology Technobis Crystal 16 T M, microscopy, and DSC. Different tools for selecting lipids provided relevant scientific knowledge for the development of the NLC. NLC-NFOH presented a z-average of 198.6 +/- 5.4 nm, PDI of 0.11 +/- 0.01, and zeta potential of -13.7 +/- 0.7 mV. A preliminary in vivo assay was performed by oral administration of NLC-NFOH (2.8 mg/kg) in one healthy male Wistar rat (341 g) by gavage. Blood from the carotid vein was collected, and the sample was analyzed by HPLC. The plasma concentration of NFOH after 5 h of oral administration was 0.22 mu g/mL. This same concentration was previously found using free NFOH in the DMSO solution (200 mg/kg), which is an almost 100-fold higher dose. This study allowed a design space development approach of the first NLC-NFOH with the potential to treat leishmaniasis orally.eng
dc.description.sponsorshipFundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2017/08332-3]
dc.relation.ispartofColloids and Surfaces B-Biointerfaces
dc.subjectDrug delivery system(s)eng
dc.subjectLipid-based formulation(s)eng
dc.subjectNanostructured lipid carriereng
dc.subject.otherimproved oral deliveryeng
dc.subject.otherskin permeationeng
dc.subject.othergelucire 50/13eng
dc.titleA new medium-throughput screening design approach for the development of hydroxymethylnitrofurazone (NFOH) nanostructured lipid carrier for treating leishmaniasiseng
dc.rights.holderCopyright ELSEVIEReng
dc.subject.wosChemistry, Physicaleng
dc.subject.wosMaterials Science, Biomaterialseng
dc.type.categoryoriginal articleeng
dc.type.versionpublishedVersioneng, Aline de:Univ Sao Paulo, Fac Pharmaceut Sci, Sao Paulo, SP, Brazil, Megumi Nishitani:Univ Sao Paulo, Fac Pharmaceut Sci, Sao Paulo, SP, Brazil, Eduardo Jose:Univ Sao Paulo, Fac Pharmaceut Sci, Sao Paulo, SP, Brazil, Lis Marie:Univ Sao Paulo, Fac Pharmaceut Sci, Sao Paulo, SP, Brazil, Leandro Augusto:Univ Fed Sao Paulo, Inst Environm Chem & Pharmaceut Sci, Dept Exact & Earth Sci, Diadema, SP, Brazil, Gabriel Lima de Barros:Univ Sao Paulo, Fac Pharmaceut Sci, Sao Paulo, SP, Brazil, Nikoletta:Univ Bath, Dept Pharm & Pharmacol, Bath, Avon, England, Raimar:Univ Alberta, Fac Pharm & Pharmaceut Sci, Edmonton, AB, Canada, Nadia Araci:Univ Sao Paulo, Fac Pharmaceut Sci, Sao Paulo, SP, Brazil
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