Lopez, FL;
Shearman, GC;
Gaisford, S;
Williams, GR;
(2014)
Amorphous formulations of indomethacin and griseofulvin prepared by electrospinning.
Molecular Pharmaceutics
, 11
(12)
4327- 4338.
10.1021/mp500391y.
![]() Preview |
PDF
GRW_Mol_Pharm_2014.pdf Download (4MB) |
Abstract
Following an array of optimization experiments, two series of electrospun polyvinylpyrrolidone (PVP) fibers were prepared. One set of fibers contained various loadings of indomethacin, known to form stable glasses, and the other griseofulvin (a poor glass former). Drug loadings of up to 33% w/w were achieved. Electron microscopy data showed the fibers largely to comprise smooth and uniform cylinders, with evidence for solvent droplets in some samples. In all cases, the drug was found to exist in the amorphous physical state in the fibers on the basis of X-ray diffraction and differential scanning calorimetry (DSC) measurements. Modulated temperature DSC showed that the relationship between a formulation's glass transition temperature (Tg) and the drug loading follows the Gordon-Taylor equation, but not the Fox equation. The results of Gordon-Taylor analysis indicated that the drug/polymer interactions were stronger with indomethacin. The interactions between drug and polymer were explored in more detail using molecular modeling simulations and again found to be stronger with indomethacin; the presence of significant intermolecular forces was further confirmed using IR spectroscopy. The amorphous form of both drugs was found to be stable after storage of the fibers for 8 months in a desiccator (relative humidity <25%). Finally, the functional performance of the fibers was studied; in all cases, the drug-loaded fibers released their drug cargo very rapidly, offering accelerated dissolution over the pure drug.
Type: | Article |
---|---|
Title: | Amorphous formulations of indomethacin and griseofulvin prepared by electrospinning |
Open access status: | An open access version is available from UCL Discovery |
DOI: | 10.1021/mp500391y |
Publisher version: | http://dx.doi.org/10.1021/mp500391y |
Language: | English |
Additional information: | This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
Keywords: | amorphous, electrospinning, griseofulvin, indomethacin, modulated-temperature DSC, nanofiber |
UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics |
URI: | https://discovery.ucl.ac.uk/id/eprint/1454625 |
Archive Staff Only
![]() |
View Item |