Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method

β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (P...

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Veröffentlicht in:Drug development and industrial pharmacy 2018-05, Vol.44 (5), p.750-756
Hauptverfasser: dos Santos, Klecia M., Barbosa, Raquel de Melo, Vargas, Fernanda Grace A., de Azevedo, Eduardo Pereira, Lins, Antônio Cláudio da Silva, Camara, Celso A., Aragão, Cícero F. S., Moura, Tulio Flavio de Lima e, Raffin, Fernanda Nervo
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container_end_page 756
container_issue 5
container_start_page 750
container_title Drug development and industrial pharmacy
container_volume 44
creator dos Santos, Klecia M.
Barbosa, Raquel de Melo
Vargas, Fernanda Grace A.
de Azevedo, Eduardo Pereira
Lins, Antônio Cláudio da Silva
Camara, Celso A.
Aragão, Cícero F. S.
Moura, Tulio Flavio de Lima e
Raffin, Fernanda Nervo
description β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap.
doi_str_mv 10.1080/03639045.2017.1411942
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Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. 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subjects dissolution rate
PEG 6000
PVP K30
solid dispersion
β-Lapachone
title Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method
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