TY - JOUR
T1 - Novel solid dispersions of naphthoquinone using different polymers for improvement of antichagasic activity
AU - Oliveira, Verônica da Silva
AU - Dantas, Elen Diana
AU - Queiroz, Anna Thereza de Sousa
AU - Oliveira, Johny Wysllas de Freitas
AU - da Silva, Marcelo de Sousa
AU - Ferreira, Patrícia Garcia
AU - da Siva, Fernando de Carvalho
AU - Ferreira, Vitor Francisco
AU - de Lima, Ádley Antonini Neves
N1 - Funding Information:
Acknowledgments: The authors wish to thank the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) for grants and fellowships. V.d.S.O. and J.W.d.F.O. acknowledge the financial support (PhD and Postdoctoral fellowships) provided by CAPES, Brazil. M.d.S.d.S. acknowledges CNPq, Brazil, for the Research Grant. This work was partially funded by Global Health and Tropical Medicine and Fundação para a Ciência e Tecnologia, FCT, Portugal (Grant number IHMT‐UID/multi/04413/2013 and Grant number PTDC/CVT/CVT/28908/2017).
Publisher Copyright:
© 2020 by the authors.
PY - 2020/11/24
Y1 - 2020/11/24
N2 - IVS320 (3a,10b-dihydro-1H-cyclopenta[b]naphtho[2,3-d]furan-5,10-dione) is a naphthoquinone that has low solubility in aqueous medium, a physical behavior that limits its biological activities, considering that compounds from this class have several activities. In this work, solid dispersions (SDs) prepared between IVS320 and polymers hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP) were developed using physical mixture (PM), kneading (KN), and rotary evaporation (RE) methods. Dispersions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). In addition, in vitro antiparasitic activity in Trypanosoma cruzi Y strains was evaluated. Physical-chemical characterization demonstrated the formation of SDs through the interaction of IVS320 with polymeric matrices. SDs of IVS320-polymer presented a significant potentiation of antichagasic activity, with inhibitory growth around 62% (IVS320-HPMC/RE), 55% (IVS320-PEG/RE), and 85% (IVS320-PVP/RE), while pure IVS320 showed a value of 48% for the highest concentrations evaluated (50 μg/mL).
AB - IVS320 (3a,10b-dihydro-1H-cyclopenta[b]naphtho[2,3-d]furan-5,10-dione) is a naphthoquinone that has low solubility in aqueous medium, a physical behavior that limits its biological activities, considering that compounds from this class have several activities. In this work, solid dispersions (SDs) prepared between IVS320 and polymers hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP) were developed using physical mixture (PM), kneading (KN), and rotary evaporation (RE) methods. Dispersions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). In addition, in vitro antiparasitic activity in Trypanosoma cruzi Y strains was evaluated. Physical-chemical characterization demonstrated the formation of SDs through the interaction of IVS320 with polymeric matrices. SDs of IVS320-polymer presented a significant potentiation of antichagasic activity, with inhibitory growth around 62% (IVS320-HPMC/RE), 55% (IVS320-PEG/RE), and 85% (IVS320-PVP/RE), while pure IVS320 showed a value of 48% for the highest concentrations evaluated (50 μg/mL).
KW - Antichagasic activity
KW - Delivery system
KW - Polymeric carriers
KW - Solid dispersion
UR - http://www.scopus.com/inward/record.url?scp=85096705545&partnerID=8YFLogxK
U2 - 10.3390/pharmaceutics12121136
DO - 10.3390/pharmaceutics12121136
M3 - Article
C2 - 33255502
AN - SCOPUS:85096705545
SN - 1999-4923
VL - 12
SP - 1
EP - 15
JO - Pharmaceutics
JF - Pharmaceutics
IS - 12
M1 - 1136
ER -