Please use this identifier to cite or link to this item: http://hdl.handle.net/1822/68264

TitleEnhanced dissolution efficiency of tamoxifen combined with methacrylate copolymers in amorphous solid dispersions
Author(s)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
Keywordstamoxifen
solid dispersions
supersaturation
polymer blending
recrystallization
Issue date2020
PublisherMultidisciplinary Digital Publishing Institute (MDPI)
JournalCrystals
CitationT. 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
Abstract(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.
TypeArticle
URIhttp://hdl.handle.net/1822/68264
DOI10.3390/cryst10111046
e-ISSN2073-4352
Publisher versionhttps://www.mdpi.com/journal/crystals
Peer-Reviewedyes
AccessOpen access
Appears in Collections:CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series

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