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Pharmaceuticals 2019, 12(1), 15; https://doi.org/10.3390/ph12010015

Micellisation Mechanism and Behaviour of Soluplus®–Furosemide Micelles: Preformulation Studies of an Oral Nanocarrier-Based System

1
Department of Pharmacy, University of Oslo, 0316 Oslo, Norway
2
Faculty of Health Sciences, OsloMet—Oslo Metropolitan University, N-0130 Oslo, Norway
*
Author to whom correspondence should be addressed.
Received: 22 December 2018 / Revised: 10 January 2019 / Accepted: 10 January 2019 / Published: 19 January 2019
(This article belongs to the Special Issue Nano Drug Carriers)
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Abstract

In this study, self-assembling Soluplus® micelles were examined for inherent properties. Through calorimetric analysis, the critical micelle concentration (CMC) could be determined at 25 and 37 °C, and the influence of three media (Milli-Q water, phosphate-buffered saline (PBS) with a pH of 7.4 and 0.1 M HCl) on the lower critical solution temperature (LCST) was detected. Furthermore, the solubilisation of a poorly soluble drug, furosemide, into the Soluplus® micelles was studied. The concentration-dependent properties of the micellar system were assessed through an examination of the micellar size, polydispersity, morphology, viscosity and solubilising properties, which were all found to be affected by the concentration, but temperature, pH and the composition of the test medium were also found to have an effect. Homogeneity in the estimated micellar size and morphology was shown for monophasic micelle dispersions in lower concentrations and with a shift towards more complex structures or aggregates in higher concentrations. The micelles were further investigated in terms of drug release and biocompatibility with mucus-producing HT29-MTX cells, where no biocompatibility issues were found. In this research, the implications for oral drug delivery are discussed and valuable preformulation information is provided on the micellar properties of a Soluplus® drug system in a liquid or semi-solid form. View Full-Text
Keywords: solubilisation; self-assembling; graft copolymer; furosemide; oral administration; nano drug carrier solubilisation; self-assembling; graft copolymer; furosemide; oral administration; nano drug carrier
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Alopaeus, J.F.; Hagesæther, E.; Tho, I. Micellisation Mechanism and Behaviour of Soluplus®–Furosemide Micelles: Preformulation Studies of an Oral Nanocarrier-Based System. Pharmaceuticals 2019, 12, 15.

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