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

Author(s):Show less -

de Lima, Luiza Ianny ^[1] ; Py-Daniel, Karen Rapp ^[1] ; Guimar, Maria Adelaide ^{[2, 3, 4]} ; Muehlmann, Luis Alexandre ^{[5, 1]} ; 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]

Affiliation

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

^[2] Phytobios Pesquisa Desenvolvimento & Inovacao LTD, Parnaiba, Piaui - Brazil

^[3] Univ Fed Piaui, BIOTEC, Nucl Pesquisa Biodiversidade & Biotecnol, Parnaiba, Piaui - Brazil

^[4] Ponto Focal Univ Fed Piaui, RENORBIO, Programa Pos Grad Biotecnol, Teresina, Piaui - Brazil

^[5] Univ Brasilia, Fac Ceilandia, BR-72220900 Brasilia, DF - 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

• Document type: Journal article
• Source: Nanomedicine; v. 13, n. 7, p. 689-702, APR 2018.
• Web of Science Citations: 8

Abstract

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] . (AU)

• FAPESP's process: 16/22488-3 - Drug repositioning for neglected diseases: identification of novel anthelmintic agents
• Grantee: Josué de Moraes
• Support Opportunities: Regular Research Grants
• FAPESP's process: 14/02282-6 - Structure-activity relationship studies about of Pilocarpus microphyllus (Rutaceae) alkaloid derivatives against Schistosoma mansoni
• Grantee: Ana Carolina Mafud
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 16/18023-5 - Preclinical studies with epiisopiloturine and epiisopilosine and their effect against other helminths
• Grantee: Ana Carolina Mafud
• Support Opportunities: Scholarships abroad - Research Internship - Post-doctor