Self-nanoemulsifying drug-delivery systems improve oral absorption and antischistosomal activity of epiisopiloturine

被引：32

作者：

de Lima, Luiza Ianny ^{[1
]}

Py-Daniel, Karen Rapp ^{[1
]}

Guimar, Maria Adelaide ^{[3
,4
,5
]}

Muehlmann, Luis Alexandre ^{[1
,2
]}

Mafud, Ana Carolina ^{[6
,7
]}

Mascarenhas, Yvonne Primerano ^{[6
]}

de Moraes, Josue ^{[8
]}

Roberto de Souza de Almeida Leite, Jose ^{[9
]}

Jiang, Cheng-Shi ^{[10
]}

Azevedo, Ricardo Bentes ^{[1
]}

Figueiro Longo, Joao Paulo ^{[1
]}

机构：

[1] Univ Brasilia, Inst Biol Sci, Genet & Morphol Dept, Brasilia, DF, Brazil

[2] Univ Brasilia, Fac Ceilandia, BR-72220900 Brasilia, DF, Brazil

[3] Phytobios Pesquisa Desenvolvimento & Inovacao LTD, Parnaiba, Piaui, Brazil

[4] Univ Fed Piaui, BIOTEC, Nucl Pesquisa Biodiversidade & Biotecnol, Parnaiba, Piaui, Brazil

[5] Ponto Focal Univ Fed Piaui, RENORBIO, Programa Pos Grad Biotecnol, Teresina, Piaui, Brazil

[6] Univ Saa Paulo, Dept Fis & Ciencia Interdisciplinar, Inst Fis Sao Carlos, BR-13566590 Sao Carlos, SP, Brazil

[7] Swiss Trop & Publ Hlth Inst, Dept Med Parasitol & Infect Biol, CH-4051 Basel, Switzerland

[8] Univ Guarulhos, Nucl Pesquisa Doencas Negligenciadas, Praca Tereza Cristina 88, BR-07023070 Guarulhos, SP, Brazil

[9] Univ Brasilia UnB, Fac Med, Area Morphol, Univ Campus Darcy Ribeiro, BR-70910900 Brasilia, DF, Brazil

[10] Univ Jinan, Sch Biol Sci & Technol, Jinan 250022, Shandong, Peoples R China

来源：

NANOMEDICINE | 2018年 / 13卷 / 07期

基金：

巴西圣保罗研究基金会;

关键词：

antischistosomal activity; oral absorption; self-nanoemulsifying drug-delivery systems; PRAZIQUANTEL; PIPLARTINE;

D O I：

10.2217/nnm-2017-0308

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Aim: To develop a self-nanoemulsifying drug-delivery system (SNEDDS) able to improve oral absorption of epiisopiloturine (EPI), and test the antischistosomal activity in a mice model. Results: SNEDDS had a nanoscopic size and was able to enhance EPI bioavailability after oral administration, and SNEDDS-EPI (40 mg.kg(-1)) improved the in vivo antischistosomal activity of EPI, demonstrating that SNEDDS was able to improve the pharmacokinetics of EPI, and to maintain the pharmacodynamic activity against Schistosoma mansoniin vivo. Conclusion: Taken together, these results indicate that SNEDDS-EPI is efficient in reducing worm burden in comparison to treatment with the free version of EPI. [GRAPHICS] .

引用

页码：689 / 702

页数：14

共 26 条

[1] Nanomedicines for overcoming biological barriers [J].

Alonso, MJ .

BIOMEDICINE & PHARMACOTHERAPY, 2004, 58 (03) :168-172

[2] The adherent gastrointestinal mucus gel layer: thickness and physical state in vivo [J].

Atuma, C ;

Strugala, V ;

Allen, A ;

Holm, L .

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY, 2001, 280 (05) :G922-G929

[3] Self-nano-emulsifying drug delivery systems: an update of the biopharmaceutical aspects [J].

Cherniakov, Irina ;

Domb, Abraham J. ;

Hoffmant, Amnon .

EXPERT OPINION ON DRUG DELIVERY, 2015, 12 (07) :1121-1133

[4] Schistosomiasis control: praziquantel forever? [J].

Cioli, Donato ;

Pica-Mattoccia, Livia ;

Basso, Annalisa ;

Guidi, Alessandra .

MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 2014, 195 (01) :23-29

[5] Human schistosomiasis [J].

Colley, Daniel G. ;

Bustinduy, Amaya L. ;

Secor, Evan ;

King, Charles H. .

LANCET, 2014, 383 (9936) :2253-2264

[6] In Vitro Synergistic Interaction Between Amide Piplartine and Antimicrobial Peptide Dermaseptin Against Schistosoma mansoni Schistosomula and Adult Worms [J].

de Moraes, J. ;

Keiser, J. ;

Ingram, K. ;

Nascimento, C. ;

Yamaguchi, L. F. ;

Bittencourt, C. R. ;

Bemquerer, M. P. ;

Leite, J. R. ;

Kato, M. J. ;

Nakano, E. .

CURRENT MEDICINAL CHEMISTRY, 2013, 20 (02) :301-309

[7]

de Moraes J, 2015, FUTURE MED CHEM, V7, P801, DOI [10.4155/fmc.15.23, 10.4155/FMC.15.23]

[8] Phytol, a Diterpene Alcohol from Chlorophyll, as a Drug against Neglected Tropical Disease Schistosomiasis Mansoni [J].

de Moraes, Josue ;

de Oliveira, Rosimeire N. ;

Costa, Jessica P. ;

Junior, Antonio L. G. ;

de Sousa, Damiao P. ;

Freitas, Rivelilson M. ;

Allegretti, Silmara M. ;

Pinto, Pedro L. S. .

PLOS NEGLECTED TROPICAL DISEASES, 2014, 8 (01) :51

[9]

Fallingborg J, 1999, DAN MED BULL, V46, P183

[10]

Frisch M. J., 2019, Gaussian 16, DOI 10.1159/000348293

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