Loading…

A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo

[Display omitted] •Fexinidazole-loaded self-emulsifying drug delivery systems (FEX-SEDDS) were developed.•SEDDS formed nanoemulsions with small and homogeneous globules after dilution.•No evidence of injury to the intestinal mucosa induced by oral FEX-SEDDS.•Oral SEDDS reduced the parasite burden in...

Full description

Saved in:

Bibliographic Details
Published in:	International journal of pharmaceutics 2023-01, Vol.631, p.122505-122505, Article 122505
Main Authors:	Damasio, Danielle Sóter do Nascimento, Antunes, Patrícia Andrade, Lages, Eduardo Burgarelli, Morais-Teixeira, Eliane de, Vital, Kátia Duarte, Cardoso, Valbert Nascimento, Fernandes, Simone Odılia Antunes, Aguiar, Marta Gontijo, Ferreira, Lucas Antônio Miranda
Format:	Article
Language:	English
Subjects:	Administration, Oral Animals Antiprotozoal Agents - pharmacology Drug Delivery Systems Emulsifying Agents Emulsions Fexinidazole Intestinal permeability Nitroimidazoles Oral treatment Self-emulsifying drug release system Solubility Visceral leishmaniasis
Citations:	Items that this one cites Items that cite this one
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

cited_by	cdi_FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673
cites	cdi_FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673
container_end_page	122505
container_issue
container_start_page	122505
container_title	International journal of pharmaceutics
container_volume	631
creator	Damasio, Danielle Sóter do Nascimento Antunes, Patrícia Andrade Lages, Eduardo Burgarelli Morais-Teixeira, Eliane de Vital, Kátia Duarte Cardoso, Valbert Nascimento Fernandes, Simone Odılia Antunes Aguiar, Marta Gontijo Ferreira, Lucas Antônio Miranda
description	[Display omitted] •Fexinidazole-loaded self-emulsifying drug delivery systems (FEX-SEDDS) were developed.•SEDDS formed nanoemulsions with small and homogeneous globules after dilution.•No evidence of injury to the intestinal mucosa induced by oral FEX-SEDDS.•Oral SEDDS reduced the parasite burden in Leishmania infantum-infected animals.•They can be a promising oral alternative for the treatment of leishmania visceral. The aim of this study was to develop, characterize and evaluate the in vivo oral efficacy of self-emulsifying drug delivery systems (SEDDS) containing fexinidazole (FEX) in the experimental treatment of visceral leishmaniasis (VL). The developed FEX-SEDDS formulation presented as a clear, yellowish liquid, with absence of precipitate. The droplet size, polydispersion index and zeta potential after dilution in water (1:200) was of 91 ± 3 nm, 0.242 ± 0.005 and −16.7 ± 0.2, respectively. In the simulated gastric and intestinal media, the FEX-SEDDS had a size of 97 ± 1 and 106 ± 9 nm, respectively. The FEX retention in droplet after SEDDS dilution in simulated gastrointestinal media was almost 100 %. Antileishmanial efficacy studies showed that FEX-SEDDS was the only treatment able to significantly (p
doi_str_mv	10.1016/j.ijpharm.2022.122505
format	article
fullrecord	<record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_2758102562</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0378517322010602</els_id><sourcerecordid>2758102562</sourcerecordid><originalsourceid>FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673</originalsourceid><addsrcrecordid>eNqFkEFP3DAQha2Kqiy0P6GVj1yytZ04Tk4IIVoqIfXC3XLscXdWdrLYSSD99Q3aLVcuM5f35r35CPnK2ZYzXn_fb3F_2JkUt4IJseVCSCY_kA1vVFmUlarPyIaVqikkV-U5uch5zxirBS8_kfOyllVbMbkh8Yb28EyHZALNEHwBcQoZ_YL9H-rStA4IOENaaF7yCJFiPKRhhkzHHVDTjxgA8y6aHg0F79Eau9DBUw8v2KMzf4cAFHs64zx8Jh-9CRm-nPYlefxx93h7Xzz8_vnr9uahsGuzsZBeKd5KKyUXdacYV10jGK9Uy8vOuppLzqF1rGudNa6RrGlF0zayVZX1tSovydXx7Nr0aYI86ojZQgimh2HKWijZcCZkLVapPEptGnJO4PUhYTRp0ZzpV9B6r0-g9StofQS9-r6dIqYugntz_Se7Cq6PAlj_nBGSzhaht-AwgR21G_CdiH_W75IQ</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2758102562</pqid></control><display><type>article</type><title>A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo</title><source>ScienceDirect Freedom Collection</source><creator>Damasio, Danielle Sóter do Nascimento ; Antunes, Patrícia Andrade ; Lages, Eduardo Burgarelli ; Morais-Teixeira, Eliane de ; Vital, Kátia Duarte ; Cardoso, Valbert Nascimento ; Fernandes, Simone Odılia Antunes ; Aguiar, Marta Gontijo ; Ferreira, Lucas Antônio Miranda</creator><creatorcontrib>Damasio, Danielle Sóter do Nascimento ; Antunes, Patrícia Andrade ; Lages, Eduardo Burgarelli ; Morais-Teixeira, Eliane de ; Vital, Kátia Duarte ; Cardoso, Valbert Nascimento ; Fernandes, Simone Odılia Antunes ; Aguiar, Marta Gontijo ; Ferreira, Lucas Antônio Miranda</creatorcontrib><description>[Display omitted] •Fexinidazole-loaded self-emulsifying drug delivery systems (FEX-SEDDS) were developed.•SEDDS formed nanoemulsions with small and homogeneous globules after dilution.•No evidence of injury to the intestinal mucosa induced by oral FEX-SEDDS.•Oral SEDDS reduced the parasite burden in Leishmania infantum-infected animals.•They can be a promising oral alternative for the treatment of leishmania visceral. The aim of this study was to develop, characterize and evaluate the in vivo oral efficacy of self-emulsifying drug delivery systems (SEDDS) containing fexinidazole (FEX) in the experimental treatment of visceral leishmaniasis (VL). The developed FEX-SEDDS formulation presented as a clear, yellowish liquid, with absence of precipitate. The droplet size, polydispersion index and zeta potential after dilution in water (1:200) was of 91 ± 3 nm, 0.242 ± 0.005 and −16.7 ± 0.2, respectively. In the simulated gastric and intestinal media, the FEX-SEDDS had a size of 97 ± 1 and 106 ± 9 nm, respectively. The FEX retention in droplet after SEDDS dilution in simulated gastrointestinal media was almost 100 %. Antileishmanial efficacy studies showed that FEX-SEDDS was the only treatment able to significantly (p < 0.05) reduce the parasite burden in the liver and spleen of animals experimentally infected with Leishmania infantum. Our intestinal permeability data suggest that FEX-SEDDS showed no evidence of injury to the intestinal mucosa. These findings suggest that FEX-SEDDS can be a promising oral alternative for the treatment of VL caused by L. infantum.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2022.122505</identifier><identifier>PMID: 36549405</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Administration, Oral ; Animals ; Antiprotozoal Agents - pharmacology ; Drug Delivery Systems ; Emulsifying Agents ; Emulsions ; Fexinidazole ; Intestinal permeability ; Nitroimidazoles ; Oral treatment ; Self-emulsifying drug release system ; Solubility ; Visceral leishmaniasis</subject><ispartof>International journal of pharmaceutics, 2023-01, Vol.631, p.122505-122505, Article 122505</ispartof><rights>2022 Elsevier B.V.</rights><rights>Copyright © 2022 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673</citedby><cites>FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/36549405$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Damasio, Danielle Sóter do Nascimento</creatorcontrib><creatorcontrib>Antunes, Patrícia Andrade</creatorcontrib><creatorcontrib>Lages, Eduardo Burgarelli</creatorcontrib><creatorcontrib>Morais-Teixeira, Eliane de</creatorcontrib><creatorcontrib>Vital, Kátia Duarte</creatorcontrib><creatorcontrib>Cardoso, Valbert Nascimento</creatorcontrib><creatorcontrib>Fernandes, Simone Odılia Antunes</creatorcontrib><creatorcontrib>Aguiar, Marta Gontijo</creatorcontrib><creatorcontrib>Ferreira, Lucas Antônio Miranda</creatorcontrib><title>A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted] •Fexinidazole-loaded self-emulsifying drug delivery systems (FEX-SEDDS) were developed.•SEDDS formed nanoemulsions with small and homogeneous globules after dilution.•No evidence of injury to the intestinal mucosa induced by oral FEX-SEDDS.•Oral SEDDS reduced the parasite burden in Leishmania infantum-infected animals.•They can be a promising oral alternative for the treatment of leishmania visceral. The aim of this study was to develop, characterize and evaluate the in vivo oral efficacy of self-emulsifying drug delivery systems (SEDDS) containing fexinidazole (FEX) in the experimental treatment of visceral leishmaniasis (VL). The developed FEX-SEDDS formulation presented as a clear, yellowish liquid, with absence of precipitate. The droplet size, polydispersion index and zeta potential after dilution in water (1:200) was of 91 ± 3 nm, 0.242 ± 0.005 and −16.7 ± 0.2, respectively. In the simulated gastric and intestinal media, the FEX-SEDDS had a size of 97 ± 1 and 106 ± 9 nm, respectively. The FEX retention in droplet after SEDDS dilution in simulated gastrointestinal media was almost 100 %. Antileishmanial efficacy studies showed that FEX-SEDDS was the only treatment able to significantly (p < 0.05) reduce the parasite burden in the liver and spleen of animals experimentally infected with Leishmania infantum. Our intestinal permeability data suggest that FEX-SEDDS showed no evidence of injury to the intestinal mucosa. These findings suggest that FEX-SEDDS can be a promising oral alternative for the treatment of VL caused by L. infantum.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antiprotozoal Agents - pharmacology</subject><subject>Drug Delivery Systems</subject><subject>Emulsifying Agents</subject><subject>Emulsions</subject><subject>Fexinidazole</subject><subject>Intestinal permeability</subject><subject>Nitroimidazoles</subject><subject>Oral treatment</subject><subject>Self-emulsifying drug release system</subject><subject>Solubility</subject><subject>Visceral leishmaniasis</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><recordid>eNqFkEFP3DAQha2Kqiy0P6GVj1yytZ04Tk4IIVoqIfXC3XLscXdWdrLYSSD99Q3aLVcuM5f35r35CPnK2ZYzXn_fb3F_2JkUt4IJseVCSCY_kA1vVFmUlarPyIaVqikkV-U5uch5zxirBS8_kfOyllVbMbkh8Yb28EyHZALNEHwBcQoZ_YL9H-rStA4IOENaaF7yCJFiPKRhhkzHHVDTjxgA8y6aHg0F79Eau9DBUw8v2KMzf4cAFHs64zx8Jh-9CRm-nPYlefxx93h7Xzz8_vnr9uahsGuzsZBeKd5KKyUXdacYV10jGK9Uy8vOuppLzqF1rGudNa6RrGlF0zayVZX1tSovydXx7Nr0aYI86ojZQgimh2HKWijZcCZkLVapPEptGnJO4PUhYTRp0ZzpV9B6r0-g9StofQS9-r6dIqYugntz_Se7Cq6PAlj_nBGSzhaht-AwgR21G_CdiH_W75IQ</recordid><startdate>20230125</startdate><enddate>20230125</enddate><creator>Damasio, Danielle Sóter do Nascimento</creator><creator>Antunes, Patrícia Andrade</creator><creator>Lages, Eduardo Burgarelli</creator><creator>Morais-Teixeira, Eliane de</creator><creator>Vital, Kátia Duarte</creator><creator>Cardoso, Valbert Nascimento</creator><creator>Fernandes, Simone Odılia Antunes</creator><creator>Aguiar, Marta Gontijo</creator><creator>Ferreira, Lucas Antônio Miranda</creator><general>Elsevier B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20230125</creationdate><title>A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo</title><author>Damasio, Danielle Sóter do Nascimento ; Antunes, Patrícia Andrade ; Lages, Eduardo Burgarelli ; Morais-Teixeira, Eliane de ; Vital, Kátia Duarte ; Cardoso, Valbert Nascimento ; Fernandes, Simone Odılia Antunes ; Aguiar, Marta Gontijo ; Ferreira, Lucas Antônio Miranda</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antiprotozoal Agents - pharmacology</topic><topic>Drug Delivery Systems</topic><topic>Emulsifying Agents</topic><topic>Emulsions</topic><topic>Fexinidazole</topic><topic>Intestinal permeability</topic><topic>Nitroimidazoles</topic><topic>Oral treatment</topic><topic>Self-emulsifying drug release system</topic><topic>Solubility</topic><topic>Visceral leishmaniasis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Damasio, Danielle Sóter do Nascimento</creatorcontrib><creatorcontrib>Antunes, Patrícia Andrade</creatorcontrib><creatorcontrib>Lages, Eduardo Burgarelli</creatorcontrib><creatorcontrib>Morais-Teixeira, Eliane de</creatorcontrib><creatorcontrib>Vital, Kátia Duarte</creatorcontrib><creatorcontrib>Cardoso, Valbert Nascimento</creatorcontrib><creatorcontrib>Fernandes, Simone Odılia Antunes</creatorcontrib><creatorcontrib>Aguiar, Marta Gontijo</creatorcontrib><creatorcontrib>Ferreira, Lucas Antônio Miranda</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Damasio, Danielle Sóter do Nascimento</au><au>Antunes, Patrícia Andrade</au><au>Lages, Eduardo Burgarelli</au><au>Morais-Teixeira, Eliane de</au><au>Vital, Kátia Duarte</au><au>Cardoso, Valbert Nascimento</au><au>Fernandes, Simone Odılia Antunes</au><au>Aguiar, Marta Gontijo</au><au>Ferreira, Lucas Antônio Miranda</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2023-01-25</date><risdate>2023</risdate><volume>631</volume><spage>122505</spage><epage>122505</epage><pages>122505-122505</pages><artnum>122505</artnum><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted] •Fexinidazole-loaded self-emulsifying drug delivery systems (FEX-SEDDS) were developed.•SEDDS formed nanoemulsions with small and homogeneous globules after dilution.•No evidence of injury to the intestinal mucosa induced by oral FEX-SEDDS.•Oral SEDDS reduced the parasite burden in Leishmania infantum-infected animals.•They can be a promising oral alternative for the treatment of leishmania visceral. The aim of this study was to develop, characterize and evaluate the in vivo oral efficacy of self-emulsifying drug delivery systems (SEDDS) containing fexinidazole (FEX) in the experimental treatment of visceral leishmaniasis (VL). The developed FEX-SEDDS formulation presented as a clear, yellowish liquid, with absence of precipitate. The droplet size, polydispersion index and zeta potential after dilution in water (1:200) was of 91 ± 3 nm, 0.242 ± 0.005 and −16.7 ± 0.2, respectively. In the simulated gastric and intestinal media, the FEX-SEDDS had a size of 97 ± 1 and 106 ± 9 nm, respectively. The FEX retention in droplet after SEDDS dilution in simulated gastrointestinal media was almost 100 %. Antileishmanial efficacy studies showed that FEX-SEDDS was the only treatment able to significantly (p < 0.05) reduce the parasite burden in the liver and spleen of animals experimentally infected with Leishmania infantum. Our intestinal permeability data suggest that FEX-SEDDS showed no evidence of injury to the intestinal mucosa. These findings suggest that FEX-SEDDS can be a promising oral alternative for the treatment of VL caused by L. infantum.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>36549405</pmid><doi>10.1016/j.ijpharm.2022.122505</doi><tpages>1</tpages></addata></record>
fulltext	fulltext
identifier	ISSN: 0378-5173
ispartof	International journal of pharmaceutics, 2023-01, Vol.631, p.122505-122505, Article 122505
issn	0378-5173 1873-3476
language	eng
recordid	cdi_proquest_miscellaneous_2758102562
source	ScienceDirect Freedom Collection
subjects	Administration, Oral Animals Antiprotozoal Agents - pharmacology Drug Delivery Systems Emulsifying Agents Emulsions Fexinidazole Intestinal permeability Nitroimidazoles Oral treatment Self-emulsifying drug release system Solubility Visceral leishmaniasis
title	A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo
url	http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-02T08%3A04%3A26IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=A%20new%20oral%20self-emulsifying%20drug%20delivery%20system%20improves%20the%20antileishmania%20efficacy%20of%20fexinidazole%20in%20vivo&rft.jtitle=International%20journal%20of%20pharmaceutics&rft.au=Damasio,%20Danielle%20S%C3%B3ter%20do%20Nascimento&rft.date=2023-01-25&rft.volume=631&rft.spage=122505&rft.epage=122505&rft.pages=122505-122505&rft.artnum=122505&rft.issn=0378-5173&rft.eissn=1873-3476&rft_id=info:doi/10.1016/j.ijpharm.2022.122505&rft_dat=%3Cproquest_cross%3E2758102562%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c365t-5f77195c55126b7017b820147913bcd61511e9d0b9dcad8508928985974cf673%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=2758102562&rft_id=info:pmid/36549405&rfr_iscdi=true