Utilize este identificador para referenciar este registo: https://hdl.handle.net/1822/68264

TítuloEnhanced dissolution efficiency of tamoxifen combined with methacrylate copolymers in amorphous solid dispersions
Autor(es)Silva, Dayanne T. C. da
Nadvorny, Daniela
Danda, Lucas J. de A.
Vieira, Amanda C. Q. de M.
Severino, Patricia
Soares, Monica F. La R.
Soares-Sobrinho, José L.
Souto, Eliana B.
Palavras-chavetamoxifen
solid dispersions
supersaturation
polymer blending
recrystallization
Data2020
EditoraMultidisciplinary Digital Publishing Institute (MDPI)
RevistaCrystals
CitaçãoT. C. da Silva, Dayanne; Nadvorny, Daniela; Danda, Lucas J. de A.; Vieira, Amanda C. Q. de M.; Severino, Patricia; Soares, Monica F. La R.; Soares-Sobrinho, José L.; Souto, Eliana, Enhanced dissolution efficiency of tamoxifen combined with methacrylate copolymers in amorphous solid dispersions. Crystals, 10(11), 1046, 2020
Resumo(s)Amorphous solid dispersions (SDs) containing poorly soluble tamoxifen dispersed in a meth(acrylate) copolymer combination were proposed as a controlled release system. The objective of this work was to investigate the characteristics and performance of the tamoxifen–polymer mixture and evaluate the changes in functionality through a supersaturating dissolution study condition while comparing it to a physical mixture at a fixed drug-loading proportion. Two polymers, Eudragit® L 100 and Eudragit® RL 100, were used to prepare SDs with a 1:1 polymer ratio, containing 10%, 20%, or 30% (wt/wt%) of tamoxifen, by the solvent evaporation method. A physical mixture containing 30% of tamoxifen was also prepared for comparison. SDs were characterized by X-ray diffraction, Fourier-transform infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. Dissolution tests were conducted under non-sink conditions to verify the occurrence of drug recrystallization upon its release. Solid-state characterizations confirmed that the drug was in the amorphous state within the polymeric matrix. Tamoxifen release in an acidic medium was mainly affected by the increase in drug concentration caused by the possible loss of interactions that characterize the main polymer functionalities. At pH 7.4, supersaturation was slowly achieved while also contributing to the increase in the kinetic solubility of the drug. The physical mixture demonstrated the best overall performance, suggesting that the polymeric interactions may have negatively affected the drug release. The combination of polymers in the composing SD proved to be a promising strategy to tailor the delivery of poorly soluble drugs. Our study highlights important information on the behavior of tamoxifen as a poorly soluble drug in supersaturating dissolution conditions while released from SD systems.
TipoArtigo
URIhttps://hdl.handle.net/1822/68264
DOI10.3390/cryst10111046
ISSN2073-4352
e-ISSN2073-4352
Versão da editorahttps://www.mdpi.com/journal/crystals
Arbitragem científicayes
AcessoAcesso aberto
Aparece nas coleções:CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series

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