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Development of polymeric nanaparticles and biodegradable systems containing lignans and evaluation its Chagas disease and schistosomiasis activities in vitro and in vivo

Grant number: 09/05049-2
Support type:Regular Research Grants
Duration: July 01, 2009 - June 30, 2011
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Principal researcher:Márcio Luís Andrade e Silva
Grantee:Márcio Luís Andrade e Silva
Home Institution: Reitoria. Universidade de Franca (UNIFRAN). Franca , SP, Brazil


In this project is proposed the development of polymeric nanaparticles to be used in the parenteral administration of two drugs (patented in the INPI), using active principles against Chagas disease and schistosomiasis, which are isolated or obtained by partial synthesis. The importance of this project is on the fact that schistosomiasis may affect more than 220 million people in the world each year, which 10 million people are living in Brazil. Also, about 30% of infected people are resistant to the treatment with available drugs in the market. Regarding Chagas disease there is no available treatment because both nifurtimox and benzonidazol were taken to the market. The active compounds which will be incorporated into nanoparticles are (-)-O-metilcubebin (2) and the (-)-hinoquinin (3) (Figure 1), both from natural occurrence and obtained by partial synthesis from the lignan (-)-cubebin (1), which are isolated from Piper cubeba. These compounds will be used, respectively, to the treatment of schistosomiasis and Chagas disease. It is important to point out that these compounds were active in previous in vitro and in vivo biological assays. Then, these compounds will be encapsulated into pharmaceutical formulations such as PLGA, PLGA-PEG, MCM-41, MCM-41 in order to be used to parenteral administration. (AU)

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Scientific publications (8)
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
NERES, NAYARA B. R.; MONTAGNINI, DANIEL; FERREIRA, DANIELE S.; PARREIRA, RENATO L. T.; ORENHA, RENATO P.; LIMA, THAIS C.; MOLINA, EDUARDO F.; CUNHA, WILSON R.; SILVA, MARCIO L. A.; ESPERANDIM, VIVIANE R.. In Vivo and in Silico Trypanocidal Activity Evaluation of (-)-Cubebin Encapsulated in PLGA Microspheres as Potential Treatment in Acute Phase. CHEMISTRY & BIODIVERSITY, v. 18, n. 6, . (17/24856-2, 13/04880-5, 10/17378-8, 09/05049-2, 11/05952-4, 11/07623-8)
PEREIRA, A. C.; MAGALHAES, L. G.; GONCALVES, U. O.; LUZ, P. P.; MORAES, A. C. G.; RODRIGUES, V.; DA MATTA GUEDES, P. M.; DA SILVA FILHO, A. A.; CUNHA, W. R.; BASTOS, J. K.; et al. Schistosomicidal and trypanocidal structure-activity relationships for (+/-)-licarin A and its (-)- and (+)-enantiomers. Phytochemistry, v. 72, n. 11-12, p. 1424-1430, . (09/05049-2, 09/15207-4)
LUZ‚ P.P.; MAGALHÃES‚ L.G.; PEREIRA‚ A.C.; CUNHA‚ W.R.; RODRIGUES‚ V.; ANDRADE E SILVA‚ M.L.. Curcumin-loaded into PLGA nanoparticles. Parasitology Research, p. 1-6, . (09/05049-2, 09/15207-4)
KAREN C.S. REZENDE; RODRIGO LUCARINI; GUILHERME V. SÍMARO; PATRICIA M. PAULETTI; ANA H. JANUÁRIO; VIVIANE R. ESPERANDIM; CARLOS H.G. MARTINS; MISLAINE A. SILVA; WILSON R. CUNHA; JAIRO K. BASTOS; et al. Antibacterial activity of (-)-cubebin isolated from Piper cubeba and its semisynthetic derivatives against microorganisms that cause endodontic infections. REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY, v. 26, n. 3, p. 296-303, . (08/07089-9, 09/05049-2)
ANDRADE E SILVA, MARCIO LUIS; ESPERANDIM, VIVIANE RODRIGUES; FERREIRA, DANIELE DA SILVA; MAGALHAES, LIZANDRA GUIDI; LIMA, THAIS COELHO; CUNHA, WILSON ROBERTO; NANAYAKKARA, DHAMMIKA N. P.; PEREIRA, ANA CAROLINA; BASTOS, JAIRO KENUPP. Furofuran lignans display schistosomicidal and trypanocidal activities. Phytochemistry, v. 107, p. 119-125, . (11/10179-2, 09/15207-4, 09/05049-2)
LUZ, PRISCILLA P.; MAGALHAES, LIZANDRA G.; PEREIRA, ANA CAROLINA; CUNHA, WILSON R.; RODRIGUES, VANDERLEI; ANDRADE E SILVA, MARCIO L.. Curcumin-loaded into PLGA nanoparticles. Parasitology Research, v. 110, n. 2, p. 593-598, . (09/05049-2, 09/15207-4)
PEREIRA, ANA CAROLINA; MAGALHAES, LIZANDRA G.; JANUARIO, ANA HELENA; PAULETTI, PATRICIA M.; CUNHA, WILSON ROBERTO; BASTOS, JAIRO KENUPP; NANAYAKKARA, DHAMMIKA N. P.; E SILVA, MARCIO LUIS A.. Enantiomeric resolution of (+/-)-licarin A by high-performance liquid-chromatography using a chiral stationary phase. Journal of Chromatography A, v. 1218, n. 39, p. 7051-7054, . (09/05049-2, 09/15207-4)
MELETI, VANDERLISA RITA; ESPERANDIM, VIVIANE RODRIGUES; BOCALON FLAUZINO, LUZIO GABRIEL; PRIZANTELLI, ANNA HELENA; DE LIMA PAULA, LUCAS ANTONIO; MAGALHAES, LIZANDRA GUIDI; CUNHA, WILSON ROBERTO; LAURENTIZ, ROSANGELA DA SILVA; DA ROCHA PISSURNO, ANA PAULA; DHAMMIKA NANAYAKKARA, N. P.; et al. (+/-)-Licarin A and its semi-synthetic derivatives: In vitro and in silico evaluation of trypanocidal and schistosomicidal activities. Acta Tropica, v. 202, . (11/07623-8, 09/05049-2, 17/24856-2)

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